FormualtionHandbook 12-2007

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(1)FORMULATION HANDBOOK Rev. December/2007. A Guide for R+D.

(2) FORMULATION HANDBOOK Table of Contents Page 1/2. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. Page 02 Page 04 Page 05 Page 08 Page 11 Page 13 Page 15 Page 16 Page 18 Page 20 Page 22 Page 24 Page 25 Page 26 Page 28 Page 29 Page 30 Page 32 Page 34 Page 35 Page 36 Page 37 Page 39 Page 40 Page 41 Page 42 Page 43 Page 44 Page 45 Page 47 Page 49 Page 50 Page 51 Page 52 Page 54 Page 56. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. Table of Contents Introduction Excipients Table of Contents Guide Formulations Acetylsalicylic Acid (High Dosage) [No. 4282-001] Acetylsalicylic Acid (Effervescent) [No. 4282-023] Acetylsalicylic Acid (OD Tablets) [No. 4282-029] Allopurinol [No. 4282-002] Ambroxol Hcl [No. 4282-003] Amoxicillin [No. 4282-024] Atenolol [No. 4282-030] Azitrhomycin 1000 mg Direct Compression [No. 4282-033] Boswellia Serrata [No. 4282-004] Calcium + Vitamin D3 [No. 4282-034] Cefalexin [No. 4282-040] Chromium Picoliante [No. 4282-005] Cimetidin [No. 4282-025] Ciprofloxacin Hcl [No. 4282-006] Citramon Chewable Tablet [No. 4282-041] Citramon Direct Compression [No. 4282-042] Creatine Monohydrate [No. 4282-028] Diazepam [No. 4282-022] Enalapril [No. 4282-007] Enalapril Hydrochlorothiazide [No. 4282-043] Extract of Cartilage [4282-008] Ginkgo Biloba [No. 4282-009] Glucosamine [No. 4282-010] Glucosamine-Chondroitin [No. 4282-035] Guafenesin [No. 4282-011] Ibuprofen (Direct Compression) [No. 4282-012] Ibuprofen (Direct Compression) [No. 4282-013] Ibuprofen (Wet Granulation) [No. 4282-014] Lecithin [No. 4282-031] Liu’wei’di’huang TCM Fluid Bed Drying + Direct Compression [No. 4282-027] Metformin [No. 4282-015] Metformin [No. 4282-026]. Customer Service: +1 (845) 878-3414.

(3) FORMULATION HANDBOOK Table of Contents Page 2/2. Page 58 Page 60 Page 62 Page 63 Page 64 Page 66 Page 68 Page 69 Page 71 Page 73 Page 74 Page 75 Page 76. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. Metoprolol (Direct Compression) [No. 4282-016] Metoprolol (Direct Compression) [No. 4282-017] Multivitamin Chewable Tablets [No. 4282-032] Multivitamin Effervescent Tablet [4282-039] Natural Herbal Laxative Cassia Senna + Melissa off. [No. 4282-018] Paracetamol 500 mg [No. 4282-038] Peppermint Oil (Direct Compression) [No. 4282-037] Piroxicam [No. 4282-019] Ranitidine Hcl [No. 4282-020] Silymarin [No. 4282-036] Simethicone [No. 4282-021] Simethicone Direct Compression [No. 4282-045] Vitamin C + Zink [No. 4282-044]. Customer Service: +1 (845) 878-3414.

(4) FORMULATION HANDBOOK Introduction. Dear Customer, "LEADING THE WORLD IN EXCIPIENTS" summarizes our commitment to the full range of technical services and support that we provide for formulation development. Take advantage of the experience and application know-how available from our JRS PHARMA's Technical Competence Centers in all questions relating to solid dosage forms. This Formulation Handbook provides you with practical examples and ideas together with an understanding of, and guides for diverse applications. Use our suggestions and examples as the first steps (creative ideas) for your own solutions. Further technical details and product information can be found on the Internet under www.jrspharma.com. Our experts will be happy to answer any questions. We look forward to a co-operative discussion with you. JRS PHARMA Technical Competence and Service Centers. USA + CANADA JRS PHARMA LP Patterson, NY 12563-2359. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG D-73494 Rosenberg (Germany). Customer Service: +1 (845) 878-3414.

(5) FORMULATION HANDBOOK JRS Excipients. Product Overview Page 1/3. The High Functionality Excipient. Insoluble Tablet Binders:. PROSOLV SMCC®. VIVAPUR® and EMCOCEL®. Silicified Microcrystalline Cellulose (Microcrystalline Cellulose, Ph.Eur., NF, JP & Silica, Colloidal Anhydrous, Ph.Eur. & Colloidal Silicon Dioxide NF & Light Anhydrous Silicic Acid JP). Microcrystalline Cellulose, Ph.Eur., NF, JP. PROSOLV SMCC® is the most significant innovation in high functionality excipients today. Used with simple direct compression, it emulates the outcome of alternative granulations while significantly reducing the number and quantity of excipients. PROSOLV SMCC® is the high functionality ingredient that offers significant benefits in terms of tablet size, production yield and overall cost. Early use in formulation development can result in early market entry, direct compression formulas and smaller tablets that consumers prefer. PROSOLV SMCC ‘s characteristics are high compactibility, high intrinsic flow, enhanced lubrication efficiency and improved blending properties. Its benefits are proven in formulation, manufacturing, marketing and regulatory approval. ®. Regulatory approvals have been simplified by the recognition that PROSOLV SMCC® is comprised of compendial excipients. Submissions have been approved in the USA, Europe and Japan. It is listed in the Inactive Ingredients Guide (IIG) of the US Food and Drug Administration (FDA) website.. These brands of MCC are preferred excipients in tablet manufacturing due to their high compactibility, inherent flow and ability to initiate disintegration. JRS Pharma has the benefit of multiple manufacturing plants for worldwide availability.. EMCOMPRESS® Calcium Hydrogen Phosphate Dihydrate, Ph.Eur., Dibasic Calcium Phosphate, Dihydrate, USP The first direct compression excipient. Its particles are of a size, shape, and density to maximize flow in high-speed tablet production and to reduce tablet weight variation. ANHYDROUS EMCOMPRESS® : In addition to excellent flow enhancement in direct compression. It does not contain water of crystallization and can be used with moisture sensitive actives. It is very often used in capsule formulations and to accelerate formulation development.. Soluble Tablet Binders: EMDEX® Dextrates, NF. A synergistic co-processing platform resulting in a co-processed API which becomes directly compressible, becomes a highly effective binder/carrier, has maximized flow and content uniformity, stabilizes hygroscopic actives. PROSOLV SMCC® co-processing provides the ultimate deaggregation and dispersion of the API.. Ideal for chewable products, it is the only compendial spherical dextrate available for direct compression that delivers the required flow, compaction and flavor carrying capacity for consumer products. EMDEX® has a great taste masking effect.. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. PROSOLV® TECHNOLOGY:. Customer Service: +1 (845) 878-3414.

(6) FORMULATION HANDBOOK JRS Excipients. Product Overview Page 2/3. CANDEX® Dextrates A plant sourced tablet and capsule dextrate.. SUGARTAB® Compressible Sucrose. Disintegrants: EXPLOTAB® Sodium Starch Glycolate, Type (A) Ph.Eur., NF Sodium Carboxymethyl Starch, JPE. Excellent for chewable products, particularly vitamin formulations. It offers good flow, excellent compressibility and flavor masking.. The classical Super Disintegrant based on starch. The material shows excellent swelling properties and gives fast disintegration times in combination with water insoluble excipients. EXPLOTAB® corresponds to type A (Ph.Eur.), other types are available as well.. COMPACTROL®. VIVASTAR®. Calcium Sulfate Dihydrate, Ph.Eur., NF. Sodium Starch Glycolate, Type (A) Ph.Eur., NF Sodium Carboxymethyl Starch, JPE. A non-hygroscopic and free-flowing product that offers excellent and long-term stability. It can be used as a binder. Super disintegrant having great disintegration power and cost savings.. in wet granulation, especially in combination with starch or powdered cellulose. Due to its high bulk density and flowing characteristics, it imparts a high degree of fluidity which is. VIVASTAR® PSF is innovative in improving stability of certain drugs by removing residual solvents.. essential for high-speed compaction and capsule filling.. VIVASOL® Croscarmellose Sodium, Ph.Eur., NF, JPE. Functional Fillers: ARBOCEL® Powdered Cellulose, Ph.Eur., NF, JP Plant derived unique functional filler for capsules and tablets that shows excellent synergistic effect in hardness when used in combination with lactose and starch.. VIVAPRESS® Calcium Carbonate, Ph.Eur., USP Precipitated Calcium Carbonate, JP. Starch-free super disintegrant that adds excellent results at low use levels.. EMCOSOY® Soy Polysaccharides An all natural super disintegrant, which does not contain starch or sugar. Being a dietary fiber, it has excellent application in nutritional products.. SATIALGINE® A pharmaceutical grade alginic acid that offers rapid swelling in an aqueous medium. It can be moistened and dried without significant loss in disintegration and combines both a wicking and swelling mechanism to promote disintegration in either wet or dry granulations.. 4282_001.GB0.00712pdf. Alginic Acid, NF A direct compressible, calcium containing filler. VIVAPRESS® meets Proposition 65 for lead content..

(7) FORMULATION HANDBOOK JRS Excipients. Product Overview Page 3/3. Lubricants and Modified Release:. Thickener and Stabilizer:. PRUV ®. VIVAPUR® MCG. Sodium Stearyl Fumarate, Ph.Eur., NF, JPE. Microcrystalline Cellulose and Carboxymethylcellulose Sodium, NF. PRUV ® is a unique tablet lubricant that is more hydrophilic than traditional lubricants, less sensitive to blending and relatively inert. This results in tablets with improved disintegration and dissolution, harder tablets and better drug stability. It can be used in all tablet formulations including chewables and effervescent tablets.. An excellent thixotropic gelling agent to stabilize suspensions and emulsions. It is pH stable and could be used in hot and cold medium.. LUBRITAB® Hydrogenated Vegetable Oil, NF, BP Hydrogenated Oil, JP Less chemically reactive than most common lubricants, it can also be used as an auxiliary dry binder and controlled release matrix.. Carriers: NON-PAREIL SEEDS Sugar Spheres, NF Sugar spheres are used in multiple drug units for improved content uniformity, consistent and controlled drug release and high drug stability.. Coating and Sustained Release: VIVAPHARM®. Low viscosity types - the economical coating polymer for protecting tablets against moisture, light oxydation, and increased patients compliance.. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. 4282_001.GB0.00712pdf. Hydroxylpropyl Methylcellulose, Hypromellose, Ph.Eur., USP.

(8) FORMULATION HANDBOOK Table of Contents Guide Formulations. Acetylsalicylic Acid (Effervescent). 4282-001. Acetylsalicylic Acid (High Dosage). 4282-023. Acetylsalicylic Acid (OD Tablets). 4282-029. Allopurinol. 4282-002. Ambroxol HCl. 4282-003. Amoxicillin. 4282-024. Atenolol. 4282-030. Azitrhomycin. 4282-033. Boswellia Serrata. 4282-004. Calcium + Vitamin D3. 4282-034. Cefalexin. 4282-040. Chromium Picoliante. 4282-005. Cimetidin. 4282-025. Ciprofloxacin HCl. 4282-006. Citramon Chewable Tablet. 4282-041. Citramon Direct Compression. 4282-042. Creatine Monohydrate. 4282-028. Diazepam. 4282-022. Enalapril. 4282-007. Enalapril Hydrochlorothiazide. 4282-043. Extract of Cartilage. 4282-008. •. •. • • • •. • • •. • • • •. • • •. •. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. • •. • • • • • • • •. • • • • • • • • • • • • • • • • • • • • • • • • •. WORLDWIDE HEADQUARTERS JRS PHARMA. •. • •. •. • • •. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. No.. ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate. Page 1/3. Customer Service: +1 (845) 878-3414.

(9) FORMULATION HANDBOOK Table of Contents Guide Formulations. Ginkgo Biloba. 4282-009. Glucosamine. 4282-010. Glucosamine-Chondroitin. 4282-035. Guafenesin. 4282-011. Ibuprofen (Direct Compression). 4282-012. Ibuprofen (Direct Compression). 4282-013. Ibuprofen (Wet Granulation). 4282-014. Lecithin. 4282-031. •. • • • • • •. •. • • • • • •. Liu’wei’di’huang TCM Fluid Bed Drying + Direct Compression 4282-027 Metformin. 4282-015. Metformin. 4282-026. Metoprolol (Direct Compression). 4282-016. Metoprolol (Direct Compression). 4282-017. Multivitamin Chewable Tablet V1. 4282-032. Multivitamin Chewable Tablet V2. 4282-039. Natural Herbal Laxative Cassia Senna + Melissa off.. 4282-018. Paracetamol 500 mg. 4282-038. Peppermint Oil (Direct Compression). 4282-037. Piroxicam. 4282-019. • • • •. • • • •. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. • • • • • • • • • •. •. •. • • • • • • • • •. • •. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. No.. ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate. Page 2/3. Customer Service: +1 (845) 878-3414.

(10) FORMULATION HANDBOOK Table of Contents Guide Formulations. No. Ranitidine HCl. 4282-020. Simethicone. 4282-021. Simethicone (Direct Compression). 4282-045. Silymarin. 4282-036. Vitamin C + Zink. 4282-044. ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate. Page 3/3. •. • •. • • • • • • •. •. •. WORLDWIDE HEADQUARTERS JRS PHARMA. GMBH+CO.KG. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312. USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. 4282_001.GB0.00712pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(11) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-001 Acetylsalicylic Acid Direct Compression. High Dosage, Direct Compression. JRS Products: VIVAPUR® 102, VIVASTAR® P. Page 1/2. Comments: Acetylsalicylic acid (ASA) is an old, very well known active substance with analgesic and antipyretic properties. It is a non-steroidal anti-inflammatory drug which also inhibits platelet aggregation.. The common acetylsalicylic acid (ASA) dosage is 500 mg. In the following formulation VIVAPUR ® 102 is used as filler and binder, and VIVASTAR ® P as disintegrant.. Formulation Acetylsalicylic Acid (ASA) VIVAPUR® 102 (Microcrystalline Cellulose) VIVASTAR® P (Sodium Starch Glycolate) Magnesium Stearate Fumed Silica (Aerosil®). Active content (mg) 500.0. mg/tablet 500.0 140.0 23.4 3.3 3.3. Contribution (%) 74.6 20.9 3.5 0.5 0.5. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time:. 670 mg 13 mm 27 - 28 kN 79.1 N 40 sec. Procedure Blending:. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_001.GB0.00709pdf. Acetylsalicylic Acid (ASA), VIVAPUR® 102 and VIVASTAR® P were blended to homogeneity for 15 minutes. Then a sieved mixture of magnesium stearate and Aerosil® were added and mixed for another 5 minutes. The powder mix is ready for direct compression.. Customer Service: +1 (845) 878-3414.

(12) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-001 Acetylsalicylic Acid Direct Compression. High Dosage, Direct Compression. JRS Products: VIVAPUR® 102, VIVASTAR® P. Page 2/2. Equipment: Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Korsch EK 0, instrumented Type T2A Pharmatest PTB 311, n=6 ERWEKA TAP ERWEKA ZT 3 Pharmatest PTW II, with 6 vessels, flat blade paddle Shimadzu UV-2101 PC. Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml. The determination of the active ingredient is done by an UV-spectrophotometer at = 280 nm.. 120. Dissolved Active Ingredient (%). 110 100 90 80 70 60 50 40 30 20 10 0. 0. 5. 10. 15. 30. 45. 60. Time (min) Diagram 1: Typical Dissolution Profile Diagram of an Acetylsalicylic Acid 500 mg Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_001.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(13) Back to Table of Contents. FORMULATION HANDBOOK. # 4282-023 Acetylsalicylic Acid Effervescent Tablet Direct Compression. Key Words:. Acetylsalicylic Acid, Direct Compression, Effervescent Tablet JRS Products: EMDEX ®, PRUV ®. Page 1/2. Comments: The acetylsalicylic acid is an old and very well known active with analgesic, antipyretic, antiinflammatory and antiaggregant. properties. Its lipophility and low water solubility make the development of an effervescent formulation a big challenge.. Formulation Acetylsalicylic Acid (ASA) PRUV ® (Sodium Stearyl Fumarate) Citric Acid NaHCO3 Glycine HCl Aspartame Flavour EMDEX® (Dextrates). mg/Tablet 500.0 12.0 348.0 400.0 128.0 76.0 36.0 2500.0. Contribution (%) 12.5 0.3 8.7 10.0 3.2 1.9 0.9 62.5. 4000.0. 100.0. Total. Tablet Characteristics Compression Force Hardness Diameter Disintegration Time. 20 kN 10.0 kp 25 mm 176 sec.. Procedure Blending: All ingredients except PRUV ® were blended for 15 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression.. Equipment: Korsch EK 0, instrumented 25 mm, biplane, Schleuniger 2E Pharmatest Standard PTZ Pharmatest PTW 2 Cecil Spektralphotometer, Series 1000. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_023.GB0.00709pdf. Tablet Press: Tablet Diameter: Hardness Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(14) Back to Table of Contents. FORMULATION HANDBOOK. # 4282-023 Acetylsalicylic Acid Effervescent Tablet Direct Compression. Key Words:. Acetylsalicylic Acid, Direct Compression, Effervescent Tablet JRS Products: EMDEX ®, PRUV ®. Page 2/2. Dissolution Test: Dissolutuion Medium: 900 ml 0.1 N HCl, 37 °C, n=6 Samples are taken after 5, 10, 15, 30, 60, 120, 180 and 300 minutes. The sample volume is 3 ml. The probes were diluted if necessary. The determination of the acetylsalicylic acid was done by an UV-spectrophotometer at = 232.0 nm.. 120 110 100. Dissolved Active (%). 90 80 70 60 50 40 30 20 10 0. 0. 20. 40. 60. 80. 100. 120. 140. 160. 180. 200. 220. 240. 260. 280. 300 320. Time (min) Diagram 1: Dissolution Profile of Acetylsalicylic Acid Effervescent Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_001.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(15) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-029. Acetylsalicylic Acid, Direct Compression, Fast Disintegration. JRS Products: PROSOLV SMCC ® 90, PURV ®, EXPLOTAB® , VIVASOL® , EMCOMPRESS ®. Acetylsalicylic Acid OD Tablets; DC Formulations Page 1. Comments: The acetylsalicylic acid is an old and very well known active with analgesic, antipyretic, antiinflammatory and antiaggregant properties. The permanently growing interest on ODT (Orally Disintegrating Tablets) in the last few years stimulate us to create these formulations.. Formulation Formulation Acetylsalicylic Acid PROSOLV SMCC® 90 (Silicified Microcrystalline Cellulose) Adipic Acid Citric Acid Sodium Hydrogencarbonate EMCOMPRESS® (Calcium Hydrogen Phosphate) EXPLOTAB® (Sodium Starch Glycolate) VIVASOL® (Croscarmellose Sodium) PRUV ® (Sodium Stearyl Fumarate). 1 71.43 20.00 4.00 2.86 1.00 0.71. Total. Substance (%) 2 3 70.43 70.43 20.00 14.00 4.00 4.00 2.86 2.86 1.00 5.00 2.00 2.00 0.71 0.71. 4 70.43 14.00 7.50 6.36 1.00 0.71. 100. 100. 100. 100. 29 0.68 13.40 7.10. 27 0.61 14.30 6.80. 28 0.87 20.00 7.10. 40 1.18 22.10 8.10. Tablet Characteristics Disintegration Time (sec) Friability (%) Compression Force (kN) Hardness (kp). Procedure All ingredients except PRUV ® were blended for 15 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression. Note: The mentioned above formulations do not contain taste masking substances!. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_029.GB0.00708pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(16) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-002. Poor Flowability, Direct Compression. JRS Products: VIVAPUR® 102, VIVASTAR® P. Allopurinol Direct Compression Page 1/2. Comments: Allopurinol is used to treat chronic gout (gouty arthritis). This condition is caused by too much uric acid in the blood. It is also used to prevent or treat other medical problems that may occur if too much uric acid is present in the body.. These include certain kinds of kidney stones or other kidney problems. Allopurinol can be directly compressed using VIVAPUR® Microcrystalline Cellulose as a binder.. Formulation Allopurinol VIVAPUR ® 102 (Microcrystalline Cellulose) VIVASTAR ® P (Sodium Starch Glycolate) Magnesium Stearate Fumed Silica (Aerosil® 200). Active content (mg) 100.0. mg/tablet 100.0 72.0 6.2 0.9 0.9. Contribution (%) 55.5 40.0 3.5 0.5 0.5. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time:. 180 mg 9 mm 24 - 25 kN 91.3 N 11 sec. Procedure Blending: Allopurinol, VIVAPUR ® 102 and VIVASTAR ® P were mixed in a Turbula mixer for 15 minutes. Then a sieved mixture of magnesium stearate and Aerosil® were added and mixed for another 3 minutes. The powder mix was ready for direct compression.. Equipment: Korsch EK 0 eccentric press, 9 mm punch,biplane Type T2A Pharmatest PTB 311, n=6 Erweka TAP Erweka ZT 3 Pharmatest PTW II, with 6 vessels, flat blade paddle Shimadzu UV-2101 PC. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_002.GB0.00709pdf. Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(17) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-002. Poor Flowability, Direct Compression. JRS Products: VIVAPUR® 102, VIVASTAR® P. Allopurinol Direct Compression Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml. Samples were diluted if necessary. The determination of the active ingredient is done by an UV-spectrophotometer at = 248.8 nm. 120 100. Dissolved Active Ingredient (%). 90 80 70 60 50 40 30 20 10 0. 0. 5. 10. 15. 20. 25. 30. 35. 40. 45. 50. 55. 60. 65. Time (min) Diagram 1: Typical Dissolution Profile Diagram of a Allopurinol Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_002.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(18) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-003 Ambroxol HCl Direct Compression. Poorly Soluble, Low Dosage, Direct Compression. JRS Products: VIVAPUR® 12, ARBOCEL® A 300, VIVASOL®. Page 1/2. Comments: Ambroxol Hydrochloride is an example for a poorly soluble active substance used in low concentrations. It can be compressed directly by using VIVAPUR ® Microcrystalline Cellulose as a dry binder and ARBOCEL® Powdered Cellulose as a plantderived filler.. Ambroxol HCl is a mucolytic agent which is widely used in chronic bronchitis in Europe. Ambroxol HCl is very popular as an Active Pharmaceutical Ingredient (API) for children.. Formulation Ambroxol HCl VIVAPUR® 12 (Microcrystalline Cellulose) ARBOCEL® A 300 (Powdered Cellulose) VIVASOL® (Croscarmellose Sodium) Magnesium Stearate Fumed Silica (Aerosil® 200). Active content (mg) 30.0. mg/tablet 30.00 69.30 46.20 3.00 0.75 0.75. Contribution (%) 20.0 46.2 30.8 2.0 0.5 0.5. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time: Friability:. 150 mg 8 mm 12.5 kN 64.0 N 13 sec <0.1 %. Procedure Blending: All ingredients were mixed for 4 minutes and compressed at a compaction force of approx. 12.5 kN.. Equipment: Korsch EK 0 eccentric press, 8 mm punch Type T2A Pharmatest PTB 311 ERWEKA TAP ERWEKA ZT 3 Pharmatest PTW II, with 6 vessels, flat blade paddle Shimadzu UV-2101 PC. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_003.GB0.00709pdf. Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(19) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-003 Ambroxol HCl Direct Compression. Poorly Soluble, Low Dosage, Direct Compression. JRS Products: VIVAPUR® 12, ARBOCEL® A 300, VIVASOL®. Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 1, 5, 10, 15, 20, 30, 45, 60, 75 and 90 minutes. The sample volume is 3 ml. Samples were diluted if necessary. The determination of the active ingredient is done by an UV-spectrophotometer at = 223 nm.. 120 110. Dissolved Active Ingredient (%). 100 90 80 70 60 50 40 30 20 10 0. 0. 5. 10. 15. 20. 25. 30. 35. 40. 45. 50. 55. 60. 65. 70. 75. 80. 85. 90. Time (min) Diagram 1: Typical Dissolution Profile Diagram of a Ambroxol Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_003.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(20) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-024 Amoxicillin Direct Compression. High Dosage, Crystalline Active Ingredient, Direct Compression. JRS Products: VIVAPUR® , VIVASTAR® , PRUV ®. Page 1/2. Comments: Amoxicillin is a bactericidal antibiotic with a relatively broad spectrum of activity. It belongs to the penicillin group. Amoxicillin mainly acts against infections caused by amoxicillin-sensitive. micro organisms, i.e. respiratory tract infections, urogenital infections or gastrointestinal infections. It is an example for an easy to compress crystalline substance.. Formulation mg/Tablet 574.0 361.0 36.0 4.5 4.5. Amoxicillin Trihydrate VIVAPUR ® 12 (Microcrystalline Cellulose) VIVASTAR ® P (Sodium Starch Glycolate) Magnesium Stearate Fumed Silica (Aerosil 200). Contribution (%) 58.6 36.8 3.8 0.4 0.4. Tablet Characteristics Diameter of Tablet: Tablet Weight: Compression Force: Hardness: Friability: Disintegration Time (in 200 ml Water):. 20 mm 980 mg 25 - 26 kN 8.8 kp 2.02 % 98 sec. Procedure Blending: Mixing of all ingredients (10 min), compressing at a compaction force of approx. 25 kN. Equipment: Korsch EKO, Nr. 6087/64 , 20 mm punch Schleuniger, Type 2 E Pharmatest, Type PTW 2 , Nr. 6276 Pharmatest Standard, Type PTZ , Nr. 6454 Pharmatest, Typ PTF 1, Nr. 6453 Cecil Spektralphotometer, Series 1000 (CE 1021). WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_024.GB0.00709pdf. Tablet Press: Hardness Tester: Dissolution Tester: Disintegration Tester: Friability Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(21) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-024. High Dosage, Crystallin Active Ingredient, Direct Compression. JRS Products: VIVAPUR® , VIVASTAR® , PRUV ®. Amoxicillin Direct Compression Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0,1 N HCl, 37°C, n=3. Samples were taken after 1, 5, 10, 20, 30, 60, 90 and 120 minutes. The determination of the active ingredient was done by an U.V. spektrophotometer at Lambda =230 nm.. 120 110. Dissolved Active Ingredient (%). 100 90 80 70 60 50 40 30 20 10 0. 0. 20. 40. 60. 80. 100. 120. 140. Time (min). WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_024.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(22) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-030 Atenolol Direct Compression. Atenolol, Direct Compression, Dissolution Profile. JRS Products: VIVAPUR ® 102, PURV ®, EXPLOTAB®. Page 1/2. Comments: Atenolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. Atenolol (trade name Tenormin) can be used to treat cardiovascular diseases such as hypertension, coronary heart. disease, arrhythmias, and treatment of myocardial infarction after the acute event. The drug is also used to treat other conditions, including dysautonomia, anxiety and hyperthyroidism (overfunction of the thyroid gland).. Formulation Atenolol VIVAPUR® 102 (Microcrystalline Cellulose) EXPLOTAB® (Sodium Starch Glycolate) PRUV ® (Sodium Stearyl Fumarate). active content/tablet (mg) 50.0 238.0 9.0 3.0. Contribution (%) 16.7 79.3 3.0 1.0. 300.0. 100.0. Total. Tablet Characteristics Tablet Weight: Tablet Diameter: Tablet Height: Compaction Force: Hardness: Disintegration Friability. 300.0 mg 10 mm 3.4 mm 4.7-4.9 kN 7.1 kp 14 sec 0.22 %. Procedure. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_030.GB0.00709pdf. The Atenolol, VIVAPUR® 102 and the EXPLOTAB® were blended for 15 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression.. Customer Service: +1 (845) 878-3414.

(23) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-030 Atenolol Direct Compression. Atenolol, Direct Compression, Dissolution Profile. JRS Products: VIVAPUR ® 102, PURV ®, EXPLOTAB®. Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37 °C, n=6 Samples are taken after 5, 10, 15, 30, 60 and 120 minutes. The sample volume is 3 ml. The probes were dilueted if necessary. The determination of the atenolol was done by an UV-spectrophotometer at l = 220 nm.. 120 110. Dissolved Active Ingredient (%). 100 90 80 70 60 50 40 30 20 10 0. 0. 10. 20. 30. 40. 50. 60. 70. 80. 90. 100. 110. Time (min) Diagram 1: Dissolution Profile of Atenolol Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_029.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(24) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-033 Azithromycin 1000 mg Direct Compression. Azithromycin, Direct Compression. JRS Products: PROSOLV SMCC ® 50, PRUV ®, VIVASOL®. Page 1/1. Comments: Azithromycin is an antibiotic acting API, which belongs to the class of macrolides. Chemical it is similar to erythromycin. Today, Azithromycin is one of the best selling antibiotics worldwide. It is used against certain bacterial infections, mainly bronchitis, pneumonia, rhinitis and some throat infections.. The formulation of 1.000 mg Azithromycin per tablet is a major challenge. The substance is very good flowing but poor compressible. The monohydrate gives better compression results than the dihydrate.. Formulation Azithromycin PROSOLV SMCC® 5o (Silicified Microcrystalline Cellulose) VIVASOL® (Croscarmellose Sodium) PRUV® (Sodium Stearyl Fumarate) Total. Active content (mg) 1000. mg/tablet 1000.0 256.0 16.0 23.0 1295.0. Contribution (%) 77.22 19.77 1.24 1.77 100. Tablet Characteristics Tablet Weight: Tablet Diameter: Tablet Height: Compaction Force: Hardness: Disintegration Time: Friability:. 1295.0 mg 14 mm, oblong 6.0 mm 16-18 kN 10.3 kp 41 sec 2.3 %. Procedure Blending: The Azithromycin, PROSOLV SMCC® 5o and the VIVASOL® were blended intensive for 15 minutes. The PRUV® was added and the tabletting powder was mixed for another 3 min. Press with compression force 16-18 kN!! A higher compression forces may cause capping.. Equipment: Tablet Press: Hardness Tester: Disintegration Tester: Friability Tester:. Kilian Pressima, 14 mm punch oblong Schleuniger 2E Pharmatest Standard PTZ Pharmatest PTF. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_021.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(25) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-004 Boswellia Serrata Direct Compression. Botanical Extract, Sticky Active, High Dosage, Direct Compression. JRS Products: PROSOLV SMCC ® HD 90, PRUV ®. Page 1/1. Comments: Using PROSOLV SMCC ® HD 90, Boswellia was formulated into a directly compressible tablet. PROSOLV SMCC ® HD 90 not only provided the necessary binding properties required for direct compression tableting, but also served as the tablet disintegrant.. Boswellia has been used historically for various conditions, including arthritis and other inflammation. It is a gum resin, cohesive in nature and, consequently, poorly flowing. Since Boswellia extract is a gum resin, it is also very poorly compactable. Due to its physical characteristics, Boswellia is generally granulated prior to tablet manufacture.. Formulation Boswellia extract PROSOLV SMCC ® HD 90 (Silicified Microcrystalline Cellulose) PRUV ® (Sodium Stearyl Fumarate). Active content (mg) 200.0. mg/tablet 200.0 200.0 2.0. Contribution (%) 49.75 49.75 0.50. Tablet Characteristics Tablet Mass: Hardness: Compaction Force: Tablet Weight Variation: Tablet Disintegration Time:. 402 mg 14.4 kp 15.2 kN 2.3% 225 sec. Procedure Blending: PROSOLV SMCC ® HD 90 and PRUV ® were dispensed to the correct masses and transferred to a Patterson-Kelly twin-shell V-blender. Boswellia was sieved through a twenty mesh and transferred into the V-blender. The powders were blended for five minutes.. Equipment: Blender: Flowability Apparatus: Tablet Press: Hardness Tester: Disintegration Tester: Friability Tester:. Patterson-Kelly twin-shell V-blender Hanson Research Flodex™ Korsch PH-106 instrumented rotary tablet press Erweka TBH-30 Erweka ZT-62 Erweka TA-3. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_004.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(26) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-034. Calcium, Vitamin D3, Effervescent Tablet, Direct Compression. JRS Products: EMDEX ®, VIVAPRESS® , PRUV ®. Calcium+Vit. D3 Effervescent Direct Compression Page 1/2. Comments: Vitamin D is a group of fat-soluble prohormones, the two major forms of which are vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol). Vitamin D regulates the calcium and phosphorus levels in the blood by promoting their absorption from food in the intestines, and by promoting re-absorption of calcium in. the kidneys. It promotes bone formation and mineralization and is essential in the development of an intact and strong skeleton. The combination of calcium supplement and vitamin D3 ist very popular for the prevention and treatment of osteoporosis.. Formulation VIVAPRESS® CA 800 (CaCO3) (Calcium Carbonate) Vitamin C Vitamin D3 Vitamin B6 Sodium Hydrogenphosphate Citric Acid Aspartam Flavour (orange) Beta Carotine 1 % CWS Sodium Chloride EMDEX ® (Dextrate) PEG 6000 PRUV ® (Sodium Stearyl Fumarate) Total. Active content (mg) 670 500 400 IU 10. mg/tablet 670 500 (10 mcg) 10 650 575 70 100 25 10 1310 40 40 4000. Contribution (%) 16.75 12.50 0.00025 0.25 16.25 14.37 1.75 2.50 0.63 0.25 32.75 1.00 1.00 100. Tablet Characteristics 4000.0 mg 25 mm 18 kN 7.5 kp < 2 min. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_034.GB0.00709pdf. Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration. Customer Service: +1 (845) 878-3414.

(27) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-034. Calcium, Vitamin D3, Effervescent Tablet, Direct Compression. JRS Products: EMDEX ®, VIVAPRESS® , PRUV ®. Calcium+Vit. D3 Effervescent Direct Compression Page 2/2. Procedure Blending: The vitamin mixture was preblended. All substances without the lubricant were mixed for 20 min. Than PRUV ® Sodium Stearyl Fumarate was added and the powder was mixed for another 3 min. DC ready.. Equipment: Tablet Press: Hardness Tester: Disintegration Tester: Friability Tester:. Korsch EK 0 eccentric press, 25 mm punch Schleuniger 2E Pharmatest Standard PTZ Pharmatest PTF. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_034.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(28) Back to Table of Contents. FORMULATION HANDBOOK Key Words :. # 4282-040 Cefalexin 1000 mg Direct Compression. Cefalexin, High Dosage, Direct Compression. JRS Products: PROSOLV SMCC ® 90, PRUV ®. Page 1/1. Comments: Cefalexin (INN) belolongs to the group of cephalosporins, member of the big family of the â-lactam antibiotics. It shows bactericidal activity caused by disruption the synthesis of the peptidoglycan layer of the bacterial cell walls. Cefalexin is so called first generation cephalosporin antibiotic with. predominantly activity against Gram-positive bacterias. Its stability toward hydrochloric acid make this â-lactam antibiotic suitable for oral administration. We developed a direct compression formulation with PROSOLV ® as a binder and PRUV ® as a lubricant.. Formulation Cefalexin PROSOLV SMCC® 50 (Silicified Microcrystalline Cellulose) PRUV ® (Sodium Stearyl Fumarate) Total. Active content (mg) 1000.0. mg/tablet 1000.0 345.0 20.0 1365.0. Contribution (%) 73.26 25.27 1.47 100.00. Tablet Characteristics Tablet Weight Tablet Diameter Compaction Force Tablet Hardness Disintegration Time. 1365.0 mg 20 mm 9.5-10.5 kN 8.5-9.0 kp 123 sec. Procedure Blending: The Cefalexin and the PROSOLV SMCC® 90 were blended for 15 minutes. The PRUV ® was added and the powder was mixed for another 3 min. Ready for direct compression.. Equipment: Tablet Press Hardness Tester Disintegration Tester. Korsch EK 0, instrumented Schleuniger 6D Pharmatest Standard PTZ. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_040.GB0.00711pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(29) FORMULATION HANDBOOK Key Words :. Sticky Active, Low Dosage, Direct Compression. JRS Products: PROSOLV SMCC ®, PRUV ®. Back to Table of Contents. # 4282-005 Chromium Picolinate Direct Compression Page 1/1. Comments: Chromium Picolinate is a poorly flowing, low dose substance. Chromium is an essential trace element. It is reported to play an important role in blood sugar regulation and acts as a cofactor to a number of enzymes involved in energy produc-. tion as well as reducing lipid levels. It can be directly compressed using a combination of PROSOLV SMCC® 50 and PROSOLV SMCC® 90.. Formulation Chromium Picolinate PROSOLV SMCC® 50 (Silicified Microcrystalline Cellulose) PROSOLV SMCC® 90 (Silicified Microcrystalline Cellulose) PRUV ® (Sodium Stearyl Fumarate). Active content (mg) 0.4. mg/tablet 0.4 15.0 135.0 0.3. Contribution (%) 0.27 9.95 89.58 0.20. Tablet Characteristics Tablet Mass: Hardness: Compaction Force: Tablet Disintegration Time:. 150.7 mg 20 kp 23 kN 158 sec. Procedure Blending: Chromium Picolinate, PROSOLV SMCC® 90 and PROSOLV SMCC® 50 added to the V-blender and blended for 30 minutes. PRUV ® was added to the blender and blended for additional three minutes.. Equipment: Blender: Flowability Apparatus: Tablet Press: Hardness Tester: Disintegration Tester: Friability Tester:. Patterson-Kelly 2 qt. twin-shell V-blender Hanson Research Flodex™ Korsch PH-106 rotary tablet press Erweka TBH-30 Erweka ZT-62 Erweka TA-3. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_005.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(30) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-025 Cimetidin 400 mg Direct Compression. High Dosage, Direct Compression. JRS Products: VIVAPUR® 12, VIVASTAR® P, PRUV ®. Page 1/2. Comments: Cimetidin is a histamine H2-receptor antagonist for treatment of ulcus duodeni and ulcus ventriculi. Normally, this active is wet granulated to achieve a better water solubility, because the. cimetidin is only slightly water soluble. But it is not a problem to make tablets by direct compression using VIVAPUR® 12 as a binder, getting good dissolution profiles as well.. Formulation mg/Tablet 400.0 265.0 28.0 3.5 3.5. Cimetidin VIVAPUR ® 12 (Microcrystalline Cellulose) VIVASTAR ® P (Sodium Starch Glycolate) PRUV ® (Sodium Stearyl Fumarate) Fumed Silica (Aerosil 200). Contribution (%) 57.1 37.9 4.0 0.5 0.5. Tablet Characteristics Diameter of Tablet: Tablet Weight: Compression Force: Hardness: Friability: Disintegration Time (in 200 ml Water):. 13 mm 700 mg 14 - 15 kN 9.8 kp 0.79 % 47 sec. Procedure Blending: Mixing of all ingredients (10 min), compressing at a compaction force of approx. 14 - 15 kN. Equipment: Korsch EKO, Nr. 6087/64 , 13 mm punch Schleuniger, Type 2 E Pharmatest, Type PTW 2 , Nr. 6276 Pharmatest Standard, Type PTZ , Nr. 6454 Pharmatest, Typ PTF 1, Nr. 6453 Cecil Spektralphotometer, Series 1000 (CE 1021). WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_025.GB0.00709pdf. Tablet Press: Hardness Tester: Dissolution Tester: Disintegration Tester: Friability Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(31) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-025. High Dosage, Direct Compression. JRS Products: VIVAPUR® 12, VIVASTAR® P, PRUV ®. Cimetidin 400 mg Direct Compression Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0,1 N HCl, 37°C, n=3. Samples were taken after 1, 5, 10, 20, 30, 60 and 120 minutes. The determination of the active ingredient was done by an U.V. spektrophotometer at Lambda = 220 nm.. 120 110. Dissolved Active Ingredient (%). 100 90 80 70 60 50 40 30 20 10 0. 0. 20. 40. 60. 80. 100. 120. 140. Time (min). WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_025.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(32) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-006 Ciprofloxacin HCl Dry Compaction. Very Low Bulk Density, Dry Compaction. JRS Products: VIVAPUR® 12. Page 1/2. Comments: Ciprofloxacin HCl is a material of very low bulk density and has to be precompacted. This can be done with a dry compactor or by “re-processing”. Ciprofloxacin is an antimicrobial agent that stops multiplication of bacteria by inhibiting the reproduction and repair of their genetic material (DNA).. Ciprofloxacin is used to treat infections of the skin, lungs, airways, bones, and joints caused by susceptible bacteria. Ciprofloxacin is also frequently used to treat urinary infections caused by bacteria such as E. Coli.. Formulation Step 1 (Granules) Ciprofloxacin HCl VIVAPUR® 12 (Microcrystalline Cellulose) Magnesium Stearate Fumed Silica (Aerosil® 200). Active content (mg) 500.0. mg/tablet 500.0 75.0 7.5 5.0. Contribution (%) 85.1 12.8 1.3 0.8. mg/tablet 587.5 93.5 5.0 4.0. Contribution (%) 85.1 13.6 0.7 0.6. Step 2 (Tablets) Ciprofloxacin Granules VIVAPUR® 12 (Microcrystalline Cellulose) Magnesium Stearate Fumed Silica (Aerosil® 200). Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time: Friability:. 690 mg 13 mm 8.5 kN 109.7 N 540 sec 0.36 %. Procedure Blending:. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_006.GB0.00709pdf. In the first step tablets were made of 20 mm insize and in the second step the tablets have been crushed by passing them through a dry granulator with a screen size of 19 mesh (800 µm). The resulting granules have been compressed to the final tablet by mixing of all ingredients for 4 minutes and compressing at a compaction force of approx. 8.5 kN.. Customer Service: +1 (845) 878-3414.

(33) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-006 Ciprofloxacin HCl Dry Compaction. Very Low Bulk Density, Dry Compaction. JRS Products: VIVAPUR® 12. Page 2/2. Equipment: Granulator: Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Erweka 20240 Korsch EK 0 eccentric press, 13 mm punch Type T2A Schleuniger Type 2 E Pharmatest Type PTF 1, Nr. 6453 Pharmatest Standard, Type PTZ, Nr. 6454 Pharmatest PTW II, with 6 vessels, flat blade paddle Cecil Spectrophotometer, Series 1000 (CE 1021). Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 1, 5, 10, 20, 30, 60, 90, 120, 180, 240 and 300 minutes. The determination of the active ingredient is done by an UV-spectrophotometer at l = 278.7 nm. 120. Dissolved Active Ingredient (%). 110 100 90 80 70 60 50 40 30 20 10 0. 0. 50. 100. 150. 200. 250. 300. 350. Time (min) Diagram 1: Typical Dissolution Profile Diagram of a Ciprofloxacin Tablet, Produced According to the Above Given Formulation.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_006.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(34) Back to Table of Contents. FORMULATION HANDBOOK Key Words :. # 4282-041 Citramon Chewable Tablet. Acetylsalicylic Acid, Paracetamol, Caffein, Direct Compression. JRS Products: EMDEX ® , PRUV ®. Page 1/1. Comments: The acetylsalicylic acid and the paracetamol are two of the widest used pain relief actives world-wide. The combination with caffein is often found in many headache and cold medicinal compositions. A common problem with this. formulation is the unpleasant bitter taste of the paracetamol and the caffein. We developed a direct compression formulation with EMDEX ® as a binder and taste improver, and PRUV ® as a lubricant.. Formulation Acetylsalicylic Acid Paracetamol Caffein Milk Powder EMDEX ® (Dextrates) Cacao Powder Citric Acid Aspartame PRUV ® (Sodium Stearyl Fumarate) Total. Active content (mg) 240.0 200.0 30.0. mg/tablet 240 200 30 199 1150 129 12 10 20 1990.0. Contribution (%) 12.06 10.05 1.51 10.00 57.79 6.48 0.60 0.50 1.01 100.00. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness:. 1990.0 mg 20 mm 16-17 kN 8-9 kp. Procedure Blending: All substances were blended for 20 minutes. Ready for direct compression.. Equipment: Tablet Press Hardness Tester Disintegration Tester. Korsch EK 0, instrumented Schleuniger 6D Pharmatest Standard PTZ. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_041.GB0.00711pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(35) Back to Table of Contents. FORMULATION HANDBOOK Key Words :. # 4282-042 Citramon Direct Compression Chewable Tablet. Acetylsalicylic Acid, Paracetamol, Caffein, Direct Compression. JRS Products: EMDEX ® , PRUV ®. Page 1/1. Comments: The acetylsalicylic acid and the paracetamol are two of the widest used pain relief actives world-wide. The combination with caffein is often found in many headache and cold medicinal compositions. The most of the formulations on the. market are made with microcrystalline cellulose. We developed a direct compression formulation with water soluble matrix using EMDEX ® as a binder and PRUV ® as a lubricant.. Formulation Acetylsalicylic acid Paracetamol Caffein EMDEX ® (Dextrates) Cacao Powder Citric Acid PRUV ® (Sodium Stearyl Fumarate) Total. Active content (mg) 240.0 200.0 30.0. mg/tablet 240.0 200.0 30.0 292.0 20.0 5.0 8.0 795.0. Contribution (%) 30.19 25.16 3.77 36.73 2.52 0.63 1.00 100.00. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Friability. 795.0 mg 13 mm 18-20 kN 8-9 kp 0.8 %. Procedure Blending: All substances except PRUV ® were blended for 15 minutes. The PRUV ® was added and the powder was mixed for another 3 min. Ready for direct compression.. Equipment: Tablet Press Hardness Tester Disintegration Tester Friability Tester. Korsch EK 0, instrumented Scleuniger 6D Pharmatest Standard PTZ Pharmatest Standard PTF. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_042.GB0.00711pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(36) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-028 Creatine Monohydrate Direct Compression. Creatine Monohydrate, Direct Compression, High Dosage. JRS Products: EMDEX® PRUV®. Page 1. Comments: Creatine is a nitrogenous organic acid that naturally occurs in vertebrates and helps to supply energy to muscle cells. Its functions as part of a system based on arginine/ phosphoarginine that operates in many invertebrates. The presence of this energy shuttle keeps the ATP/ADP ratio high which ensures that the free energy of ATP remains high and minimizes the loss of adenosine nucleotides, which would cause cellular dysfunction. Such high energy phosphate. buffers are known as phosphagens. Creatine supplementation has been, and continues to be, investigated as a possible therapeutic approach for the treatment of muscular, neurological and neuromuscular diseases (arthritis, congestive heart failure, disuse atrophy, gyrate atrophy, McArdle's disease, Huntington's disease, miscellaneous neuromuscular diseases, mitochondrial diseases, muscular dystrophy, neuroprotection, etc.).. Formulation Creatine Monohydrate EMDEX ® (Dextrates) PRUV ® (Sodium Stearyl Fumarate). active content/tablet (mg) 1000.0 190.0 10.0. Contribution (%) 83.33 15.83 0.84. 1200.0. 100.00. Total. Tablet Characteristics Diameter of Tablet: Tablet Weight: Compression Force: Hardness:. 17 mm 1200.0 mg 32 kN 6 kp. Procedure The creatine mohohydrate and EMDEX® were blended for 18 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression.. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_028.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(37) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-022 Diazepam. Low Dosage, Direct Compression. JRS Products: VIVAPUR ® 12, EMCOMPRESS® , EXPLOTAB ®/VIVASTAR ® Page 1/2. Comments: Diazepam, better known under the original name Valium™, is a benzodiazepine derivative.. tension and anxiety. Normally the dosage in tablets is between 2 and 10 mg.. It is for short-term management of moderate degrees of anxiety, tension, agitation, fear or aggressiveness. It is often used in certain medical procedures (e.g. surgery ) to reduce. This formulation is an example for a low dosage active ingredient, workable in direct compression.. Formulation mg/Tablet 10,0 59,0 65,5 4,0 0,8 0,7. Diazepam VIVAPUR ® 12 (Microcrystalline Cellulose) EMCOMPRESS® (Calcium Hydrogen Phosphate) VIVASTAR ® (Sodium Starch Glycolate) PRUV ® (Sodium Stearyl Fumarate) Fumed Silica (Aerosil 200). Contribution (%) 7,1 42,1 46,8 2,9 0,6 0,5. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time: Friability:. 140 mg 8 mm 21 - 22 kN 7,3 kp 20 sec 0,1 %. Procedure Blending: Mix all ingredients except PRUV ® for 10 minutes. Add PRUV ® and mix another 3 minutes. The powder is for direct compression.. Equipment: Korsch EK 0, instrumented Schleuniger 2E Pharmatest Standard PTZ Pharmatest PTW 2 Cecil Spektralphotometer, Series 1000. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_022.GB0.00709pdf. Tablet Press: Hardness Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:. Customer Service: +1 (845) 878-3414.

(38) Back to Table of Contents. FORMULATION HANDBOOK Key Words:. # 4282-022 Diazepam. Low Dosage, Direct Compression. JRS Products: VIVAPUR ® 12, EMCOMPRESS® , EXPLOTAB ®/VIVASTAR ® Page 2/2. Dissolution Test: Dissolution Medium: 900 ml 0,1 N HCl, 37°C, n = 6 Samples were taken after 1, 5, 10, 20, 30, 60 and 120 minutes. The determination of the active ingredient was done by an UV spectrometer at é= 242 nm.. 120 110. Dissolved Active Ingredient (%). 100 90 80 70 60 50 40 30 20 10 0. 0. 5. 10. 15. 20. 25. 30. 35. 40. 45. 50. 55. 60. 65. 70. Time (min). WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_023.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

(39) FORMULATION HANDBOOK Key Words:. Poor Flowability, Low Dosage, Direct Compression. JRS Products: PROSOLV SMCC ® 90, EMCOMPRESS® , VIVASTAR® P, PRUV ®. Back to Table of Contents. # 4282-007 Enalapril Direct Compression Page 1/1. Comments: Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure.. Enalapril which is a poor flowing API can be directly compressed using PROSOLV SMCC® 90 and EMCOMPRESS® as binders.. Formulation Enalapril Maleate PROSOLV SMCC® 90 (Silicified Microcrystalline Cellulose) EMCOMPRESS® (Calcium Hydrogen Phosphate) VIVASTAR® P (Sodium Starch Glycolate) PRUV ® (Sodium Stearyl Fumarate). Active content (mg) 10.0. mg/tablet 10.0 93.7 85.4 5.9 1.0. Contribution (%) 5.1 47.8 43.6 3.0 0.5. Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Friability: Disintegration Time:. 196 mg 8 mm 17 - 18 kN 10.8 kp 0.03 % 14 sec. Procedure Blending: Enalapril maleate, PROSOLV SMCC® 90, EMCOMPRESS® and VIVASTAR® P were blended to homogeneity for 10 minutes. Then PRUV ® was added and mixed for another 3 minutes. The powder-mix was ready for direct compression.. Equipment: Tablet Press: Hardness Tester: Friability Tester: Disintegration Tester:. Korsch EK 0 eccentric press, 8 mm punch Schleuniger 2E Pharmatest PFT Pharmatest Standard PTZ. WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG. USA + CANADA JRS PHARMA LP. Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail: [email protected] www.jrspharma.de www.jrs.de. 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail: [email protected] www.jrspharma.com. Customer Service: +49 (0) 7967 / 152-312. 4282_007.GB0.00709pdf. Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.. Customer Service: +1 (845) 878-3414.

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