BP : Croscarmellose Sodium
JP : Croscarmellose Sodium
PhEur : Croscarmellose Sodium
USP-NF : Croscarmellose Sodium
Synonyms : Ac-Di-Sol; carmellosum natricum conexum; crosslinked carboxymethylcellulose sodium; Explocel; modified cellulose gum; Nymcel ZSX; Pharmacel XL; Primellose; Solutab; Vivasol.
Chemical Name and CAS Registry Number:
Cellulose, carboxymethyl ether, sodium salt, crosslinked [74811- 65-7] Empirical Formula and Molecular Weight:
Croscarmellose sodium is a crosslinked polymer of carboxymethylcellulose sodium. Structural Formula:
91 Functional Category:
Tablet and capsule disintegrant.
Applications in Pharmaceutical Formulation or Technology:
Croscarmellose sodium is used in oral pharmaceutical formulations as a disintegrant for capsules,(1,2) tablets,(3–13) and granules. In tablet formulations, croscarmellose sodium may be used in both direct-compression and wet-granulation processes. When used in wet granulations, the croscarmellose sodium should be added in both the wet and dry stages of the process (intra- and extragranularly) so that the wicking and swelling ability of the disintegrant is best utilized.(11,12) Croscarmellose sodium at concentrations up to 5% w/w may be used as a tablet disintegrant, although normally 2% w/w is used in tablets prepared by direct compression and 3% w/w in tablets prepared by a wet-granulation process.
Use Concentration: (in %) Disintegrant in capsules 10–25 Disintegrant in tablets 0.5–5.0 Description:
Croscarmellose sodium occurs as an odorless, white or grayish white powder. Typical Properties:
Acidity/alkalinity pH = 5.0–7.0 in aqueous dispersions. Bonding index 0.0456
Brittle fracture index 0.1000
92 Stability and Storage Conditions:
Croscarmellose sodium is a stable though hygroscopic material. A model tablet formulation prepared by direct compression, with croscarmellose sodium as a disintegrant, showed no significant difference in drug dissolution after storage at 308C for 14 months.(9) Croscarmellose sodium should be stored in a well-closed container in a cool, dry place.
Incompatibilities:
The efficacy of disintegrants, such as croscarmellose sodium, may be slightly reduced in tablet formulations prepared by either the wet-granulation or direct- compression process that contain hygroscopic excipients such as sorbitol. Croscarmellose sodium is not compatible with strong acids or with soluble salts of iron and some other metals such as aluminum, mercury, and zinc.
Safety:
Croscarmellose sodium is mainly used as a disintegrant in oral pharmaceutical formulations and is generally regarded as an essentially nontoxic and nonirritant material. However, oral consumption of large amounts of croscarmellose sodium may have a laxative effect, although the quantities used in solid dosage formulations are unlikely to cause such problems. In the UK, croscarmellose sodium is accepted for use in dietary supplements. The WHO has not specified an acceptable daily intake for the related substance carboxymethylcellulose sodium, used as a food additive, since the levels necessary to achieve a desired effect were not considered sufficient to be a hazard to health.
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POLYSORBATE 80
Synonym : TWEEN 80; Polyoxyethylene 20 sorbitan monooleate; Polyethylene oxide sorbitan mono-oleate; Polyoxyethylene sorbitan monooleate; Polyoxyethylene sorbitan oleate; Sorbitan mono-9-octadecenoate poly(oxy-1,2-ethanediyl) derivatives; Sorethytan (20) monooleate
Chemical Name : Sorbitan, monooleate polyoxyethylene derivative.
Physical state and appearance: Liquid. (Oily liquid.)
Odor : fatty (Slight.)
Color : Clear Amber. Yellow.
pH (1% soln/water): 7 [Neutral.]
Boiling Point : >100°C (212°F)
Melting Point : -20.556°C (-5°F)
Specific Gravity : 1.06 - 1.10 (Water = 1)
Solubility : Easily soluble in cold water, hot water. Soluble in methanol. Soluble in Toluene, alcohol, cottonseed oil, corn oil, Ethyl Acetate. Insoluble in mineral oil..
Incompatibility with various substances:
Reactive with oxidizing agents.
Corrosivity:
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Structure:
Food use:
Polysorbate 80 is used as an emulsifier in foods, particularly in ice cream. Here, polysorbate is added to up to 0.5% (v/v) concentration and makes the ice cream smoother and easier to handle, as well as increasing its resistance to melting.[4] Adding this substance prevents milk proteins from completely coating the fat droplets. This allows them to join together in chains and nets, which hold air in the mixture, and provide a firmer texture that holds its shape as the ice cream melts.
Medical use:
Polysorbate 80 is an excipient that is used to stabilize aqueous formulations of medications for parenteral administration, and used as an emulsifier in the manufacture of the popular anti-arrhythmic amiodarone.[5] It is also used as an excipient in some European and Canadian influenza vaccines.[6] It is also used in the culture of Mycobacterium tuberculosis in Middlebrook 7H9 broth.
Laboratory use:
Some mycobacteria contain a type of lipase (enzyme that breaks up lipid molecules). When added to a mixture of Tween 80 and phenol red, they cause the solution to change colour, so this is used as a test to identify the phenotype of a strain or isolate.
95 Molecular formula C64H124O26
Molar mass 1310 g/mol
Appearance Amber colored viscous liquid
Density 1.06–1.09 g/mL, oily liquid
Boiling point > 100°C
Solubility in water Very soluble
Solubility in other solvents
soluble in ethanol, cottonseed oil, corn oil, ethyl acetate, methanol, toluene
Viscosity 300–500 centistokes (@25°C) Main hazards Irritant
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6. MATERIALS AND EQUIPMENTS
API, excipients and equipments used for the development of formulation:
S.No. Materials Suppliers
1 Artemether Mangalam drugs Pvt
2 Lumefantrine Mangalam drugs Pvt
3 Hydroxyl propyl cellulose
Welming pharmaceuticals, India
4 Polysorbate 80 Welming chemicals,india
5 Iso propyl alcohol
Loba chemie.,pvt ltd,. Mumbai
6 Microcrystalline cellulose Welming chemicals, India
7 Croscarmelose sodium S.D.Fine-Chemi.,Pvt Ltd., Mumbai
8 Aerosil Amaratal & Co., Chennai
9 Magnesium stearate Loba chemie., Pvt. Ltd., Mumbai
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