Saturation solubility

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SATURATION SOLUBILITY OF SCOPOLAMINE IN THIN FILMS OF POLYACRYLATE PRESSURE SENSITIVE ADHESIVES IS TEMPERATURE DEPENDENT

SATURATION SOLUBILITY OF SCOPOLAMINE IN THIN FILMS OF POLYACRYLATE PRESSURE SENSITIVE ADHESIVES IS TEMPERATURE DEPENDENT

Change to the non-cross-linked DURO-TAK 87- 2510 reaches equilibrium after a shorter time, and to a lower value of saturation solubility of the scopolamine at both 25 °C (Fig. 2 a) and 45 °C (Fig. 2 b). The rate of uptake of scopolamine into the acceptor at times up to 2 days is, however, the same with both polymers. With DURO-TAK 2510 this uptake is completed after 2 days, but with DURO-TAK2677 the uptake continues until equilibrium is reached at day 15. This indicates that the diffusivity of the scopolamine is similar in both polymers. The observed shorter time to reach equilibrium in DURO-TAK 2519 is just a result of the higher value of c s * that has to be reached.
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Optimization and Characterization Ezogabine-Loaded Nanosuspension for Enhancement of Bioavailability by “Bottom-Up” Technology Using 32 Factorial Design

Optimization and Characterization Ezogabine-Loaded Nanosuspension for Enhancement of Bioavailability by “Bottom-Up” Technology Using 32 Factorial Design

release was done. The FTIR was used to confirm compatibility and to rule out any possible interactions between drug and carriers. The optimal nanosuspension was obtained with particle size of 510.4 nm, saturation solubility of 557 μg/ml, zeta potential of - 4.49 mV, entrapment efficiency of 96.82%, and in-vitro drug release of 100.14%. Also, the optimal formulation was found to be stable in the accelerated conditions. Data of nanosuspensions were fit in to different equations and kinetic models and found to exhibit first order release kinetics with class II transport mechanism of diffusion. The scanning electron microscopy studies showed elongated nanoparticles with porous surface. The “Bottom up” method can be successfully employed to produce ezogabine nanosuspensions achieving reduced particle size and enhancing dissolution rate by increasing the saturation solubility and remained stable at 25 °C.
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Nanosuspension: Newer Approach for Drug Delivery System

Nanosuspension: Newer Approach for Drug Delivery System

Nanosuspensions are colloidal dispersions of nanosized drug particles stabilized by surfactants. They can also be defined as a biphasic system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1µm in size 7 . Reduction of drug particles to nanometer range leads to an enhanced dissolution rate not only because of increased surface area but also because of saturation solubility. The increase in the saturation solubility and solution velocity of nanoparticle is due to increase of vapour pressure of the particles. Nanosuspension have disclosed the problems associated with the delivery of poorly water soluble and poorly water and lipid soluble drugs and are unequalled because of their simplicity and rewards they confer over other strategies 8 . The particle size distribution of the solid particles in nanosuspensions is usually less than one micron with an average particle size ranging between 200 and 600 nm. An increase in the dissolution rate of micronized particles (particle size < 10 µm) is related to an increase in the surface area and consequently the dissolution velocity 9 . A Nanosuspension is a submicron colloidal dispersion of drug particles. A pharmaceutical
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Characterization of Hydrochloride and Tannate Salts of Diphenhydramine

Characterization of Hydrochloride and Tannate Salts of Diphenhydramine

The pH of 1% solution was within 6 to 6.5 and 6 to 6.2, of DPH HCL and DPH tannate, respectively. The pH saturation solubility profiles for DPH HCl and DPH tannate were showed significantly higher solubility of DPH HCl than DPH tannate at all the determined pH values and in water and organic solvents (Table 3). Both, drugs exhibited high solubility at a pH <2.0. For example, at room temperature, pH 1.2, the solubility of DPH HCl and DPH tannate were 107 and 34 mg/ml, respectively. However, the solubility of DPH HCl, being a weak base, demonstrated a parabolic relationship showing minimum solubility around pH 3.0 to 6.0 and high solubility in both the low acid and alkaline range, appears to dissolve maximally around pH ≤2.0. IR spectra of DPH salts (Þ g. 1) after stability study did not show any signiÞ cant changes in the characteristic peaks of DPH tannate, thus indicating good stability of drug at accelerated conditions and DPH HCl shows extra peak at 3600 to 3700 cm -1 indicating presence
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Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

Abstract: This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precip- itation–ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvi- nylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active phar- maceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that .88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the C max were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC 0→24 h ) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption. Keywords: aceclofenac nanocrystals, precipitation–ultrasonication, dissolution rate, in vivo studies
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FORMULATION, CHARACTERIZATION AND IN-VITRO RELEASE STUDY OF SILYMARIN NANOSUSPENSIONSumathi .R *, Tamizharasi.S, Gopinath.K, Sivakumar.TDOWNLOAD/VIEW

FORMULATION, CHARACTERIZATION AND IN-VITRO RELEASE STUDY OF SILYMARIN NANOSUSPENSIONSumathi .R *, Tamizharasi.S, Gopinath.K, Sivakumar.TDOWNLOAD/VIEW

The saturation solubility studies were carried out for both the unprocessed pure drug and different batches of lyophilized nanosuspension.10mg of unprocessed pure drug and nanosuspension equivalent to 10 mg of silymarin was weighed and separately introduced into 25 ml stopper conical flask containing 10 ml distilled water. The flasks were sealed and placed in rotary shaker for 24 hours at 37°C and equivalent for 2 days. The samples were collected after the specified time interval and it is filtered and analyzed. The samples were analyzed using UV spectrophotometer at 287nm [15].
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FORMULATION AND EVALUATION OF NANOSUSPENSION TO IMPROVE SOLUBILITY AND DISSOLUTION OF DIACEREIN

FORMULATION AND EVALUATION OF NANOSUSPENSION TO IMPROVE SOLUBILITY AND DISSOLUTION OF DIACEREIN

Nanosuspension is one of the most important strategies to enhance the oral bioavailability of poorly water soluble drugs 10 . Preparing nanosuspension can be a challenging technique. Various methods which are generally used to prepare nanosuspension are bottom-up including precipitation, and top-down including media milling, emulsion solvent diffusion method, supercritical fluid method, dry co-grinding, high- pressure homogenization, Nano edge 6, 11 . Nanosuspension have two particular advantageous properties, firstly increased saturation solubility and secondly the enlarged surface. Both properties results in an increase in the dissolution rate according to the Noyes-Whitney Law 12 . In general it is advantageous to use nanoparticles that are as small as possible to achieve a maximum improvement in the oral bioavailability or a very rapid dissolution rate 13, 14 .
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“DEVELOPMENT AND EVALUATION OF TOPICAL FORMULATION OF CARBAMAZEPINE”

“DEVELOPMENT AND EVALUATION OF TOPICAL FORMULATION OF CARBAMAZEPINE”

The saturation solubility of Carbamazepine was determined by shaking method. Excess drug was added in 5 ml vial containing 2 ml distilled water and pH 7.4 phosphate buffer. After proper mixing of the mixture, the vial was kept in an orbital shaker at 37±1 0 C for 72 h to reach equilibrium. Then, the sample was removed and centrifuged at 3000 rpm for 15 min and filtered. Filtrate was suitably diluted and absorbance was taken at 284.0 nm using UV- Visible spectrophotometer. The solubility of drug was determined using standard calibration curve of drug in water and pH 7.4 phosphate buffer.
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SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEM FOR COMBINATION OF HYDROPHILIC AND LIPOPHILIC DRUGS

SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEM FOR COMBINATION OF HYDROPHILIC AND LIPOPHILIC DRUGS

ABSTRACT: Improvement in the bioavailability of poorly soluble drugs is one of the challenges faced in the formulation development of the drugs. One of the most admirable and viable formulation approaches for this is self micro emulsifying drug delivery system (SMEDDS). A combination of clarithromycin and amoxicillin has been proved effective for treatment of H. pylori which are available only in tablet dosage form. Hence, the aim of the present study was to prepare SMEDDS of amoxicillin and clarithromycin for better patient compliance. SMEDDS were prepared using Peceol, Cremophor EL and Transcutol as oil, surfactant and co-surfactant respectively. Prepared SMEDDS were evaluated for particle size, zeta potential, water dispersion properties, saturation solubility and in-vitro drug release. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Study concluded that SMEDDS can be an effective alternative for tablet therapy with enhanced dissolution rate and bioavailability .
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Solubility And Dissolution Enhancement Of Bosentan Monohydrate By Solid Dispersion Technique

Solubility And Dissolution Enhancement Of Bosentan Monohydrate By Solid Dispersion Technique

 Enhancing permeability of poorly permeable drugs. (3) The therapeutic efficacy of a drug product intended to be administered by the oral route mainly depends on its absorption by the gastrointestinal tract. However, for a drug Abstract: Solid dispersions (SDs) are one of the most promising strategies used to improve the solubility of poorly water soluble drugs. This technology is mainly applied to improve the solubility of Class II and Class IV drugs. Bosentan monohydrate is an anti-hypertensive agent used in the treatment of pulmonary arterial hypertension, which has oral bioavailability of 40-50% and it belongs to the BCS class-II. Many attempts are made in the past to increase its solubility by preparing its solid dispersions. However, very few literature reports are available wherein polymers are used for preparation of solid dispersions. In the present work, an attempt is made to increase the solubility of bosentan by preparing its solid dispersions using polymer i.e. gelucire44/14 and poloxamer407 various techniques used for preparing Solid dispersions are by physical mixture, of solvent evaporation methods using different drug-polymer ratio. Thus prepared solid dispersions were evaluated for percentage yield, drug content, saturation solubility and in-vitro dissolution studies. The result obtained from above studies indicated that, the solubility and dissolution of bosentan monohydrate of solid dispersions was improved as compared to pure drug by all the methods employed. Among various methods employed, solvent evaporation method produced good results compared to physical mixture, solvent method. Hence, Solid dispersion technology can be used to improve the solubility of bosentan monohydrate.
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“Design and Characterisation of Nitrendipine Nanocrystals for Solubility and Dissolution Enhancement” by Anilkumar J. Shinde, Monika S. Sankpal, Sujit V. Salokhe, Harinath N. More, India.

“Design and Characterisation of Nitrendipine Nanocrystals for Solubility and Dissolution Enhancement” by Anilkumar J. Shinde, Monika S. Sankpal, Sujit V. Salokhe, Harinath N. More, India.

NTD drug was found to be faint yellow in color, odourless, crystalline solid and melting point 156- 160°C, which complies with E. P. limit. NTD nanocrystals were successfully prepared by the anti- solvent precipitation method. The obtained nanocrystals have been assessed for particle size analysis, zeta potential, saturation solubility and solid-state characterisation by XPRD, DSC, FTIR and SEM analysis. Compatibility studies of NTD and excipients was conducted on FTIR studies. FTIR spectrums revealed that the fundamental peaks of the NTD were retained in the physical mixture indicating absence of any chemical interaction between them.
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Title:  ANTIEPILEPTIC DRUGS: TREATMENT IN ELDERLY PATIENTS. Author:  Callegari C. *, Bianchi L., Vender S Keyword:  Antiepileptic drugs, elderly patients, gabapentinPage No:  96-102Abstract:   Introduction: This study aims to examine qualitatively the use

Title: ANTIEPILEPTIC DRUGS: TREATMENT IN ELDERLY PATIENTS. Author: Callegari C. *, Bianchi L., Vender S Keyword: Antiepileptic drugs, elderly patients, gabapentinPage No: 96-102Abstract: Introduction: This study aims to examine qualitatively the use of AEDs in a population of elderly patients in nursing homes, including the prescription of specialist and monitoring. Methods: This p revalence study was carried out in a state-founded nursing home providing assistance and rehabilitation for elderly people. The first objective of the study is to determine the prevalence of the use of antiepileptic drugs. The second objective is to study the monitoring the dosage modification from the time of admission of the patient until the end of the study. Results: In the period of time that we took into consideration 65 of 402 patient’s monitored patients had at least one anti-epileptic therapy (prevalence of 32%). The antiepileptic drug most prescribed was gabapentin with a frequency of 63.6%. Discussion: The prevalence use of AEDs has beeen 32%. The second objective concerns the drugs monitoring and it has also been achieved and shows how gabapentin is the most prescribed drug (53.8% psychiatrist) and was introduced mainly for anxiety disorders, psychosis, neuropathic pain and mood disorders. Keywords: Antiepileptic drugs, elderly patients, gabapentin Download PDF

gm/mole. It is insoluble in water, freely soluble in methanol, soluble in diluted ammonia or sodium hydroxide. 1 According to the Biopharmaceutics Classification System (BCS) aqueous solubility and permeability are the most important variables affecting drug bioavailability. HCT is classified as Class IV, where the drugs have low solubility and low permeability characteristics after oral Abstract: Hydrochlorothiazide (HCT) is a class IV drug which has limited solubility and permeability, for overcome this problems co-crystallization method is used. Co-crystallization is the process to enhance the physical properties of drug molecule especially the solubility. HCT belongs to diuretic category and Propranolol Hydrochloride (PPL) belongs to Beta blocker category they are combined for use in tablet formulation. Co-crystallization was used to combine two drugs in single solid phase and thus to achieve new approach for combination therapy. Using the new approach co- crystals of PPL with HCT were prepared. Co-crystallization of two drugs were carried out by using solvent evaporation and solution co-crystallization method. The saturation solubility was done to evaluate the solubility of co-crystals. Dissolution properties were determined and compared with the marketed tablet formulation. The prepared co-crystals has shown several times faster release than marketed tablet and optimized co-crystals were characterized by using DSC, FTIR and SEM.
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FORMULATION AND DEVELOPMENT OF STABLE METAXALONE NANOSUSPENSION USING 32 FACTORIAL DESIGN

FORMULATION AND DEVELOPMENT OF STABLE METAXALONE NANOSUSPENSION USING 32 FACTORIAL DESIGN

optimization of the formulation variables such as concentration of poloxamer 407 and stirring time as independent variables. The particle size (PS) and maximum saturation solubility (SS) were selected as dependent variables. Formulation thus optimized was subjected to in vitro dissolution test to evaluate improvement of dissolution in comparison to current marketed formulation of metaxalone, SKELAXIN ®

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SOLUBILITY ENHANCEMENT OF BCS CLASS II DRUG USING LYOPHILISATION TECHNIQUE AND DETERMINATION OF BIOAVAILABILITY IN ANIMALS USING CATALEPSY MODEL

SOLUBILITY ENHANCEMENT OF BCS CLASS II DRUG USING LYOPHILISATION TECHNIQUE AND DETERMINATION OF BIOAVAILABILITY IN ANIMALS USING CATALEPSY MODEL

colored powder having very low solubility in water (21.12 mg/L). The main purpose of this study is to enhance the solubility of Ziprasidone HCl using lyophilisation technique. The β-Cyclodextrine and Hydroxy Propyl- β-Cyclodextrine were used as the water soluble carriers for increasing the solubility of Ziprasidone. All the inclusion complexes prepared by lyophilisation technique showed remarkable increase in the solubility compared to the pure Ziprasidone HCl. The saturation solubility analysis demonstrated highest increase in the solubility of drug after complexation with HP-β-CD by lyophilisation technique. The inclusion complexes were characterized using DSC and XRD technique. During in vitro study result obtained that the lyophilized complexes with HPβ-CD showed 100% drug release within 10 min were as the lyophilized complexes with β– CD showed 100% drug release in 25 min. Therefore the freeze dried complex with HP-β-CD was selected for Catalepsy study on Wistar rats. In the catalepsy study the selected inclusion complex showed increase in bioavailability compared to the drug and almost all the data obtained from study was found to be 99.99% significant with the control . INTRODUCTION: 1-7 The way of treating
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DESIGN, DEVELOPMENT AND OPTIMIZATION OF VALSARTAN LIQUISOLID TABLETS USING BOX BEHNKEN DESIGN

DESIGN, DEVELOPMENT AND OPTIMIZATION OF VALSARTAN LIQUISOLID TABLETS USING BOX BEHNKEN DESIGN

Saturation Solubility Studies: The solubility of Valsartan in different non-volatile liquid vehicles that are commonly used for the formulation of liquisolid com pacts, namely, propylene glycol, polyethylene glycol 200 (PEG 200), and PEG 400, Tween 20, Tween 40 and Tween 80 was determined by preparation of saturated solutions of the drug in these solvents and measuring the solubilized drug concentration. Excess Valsartan was stirred in the above mentioned solvents for 48 h at 25˚C. Accurately weighed quantities of the filtered supernatants were further diluted with methanol and analyzed spectrophotometrically at 250 nm for their drug content. From these results, the solubility of Valsartan in the respective liquid vehicle was calculated. Each experiment was carried out in triplicate 9, 10 .
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ENHANCEMENT OF BIOAVAILABILITY OF NORFLOXACIN MUCOADHESIVE SUSPENSION BY USING DIFFERENT GRADES OF CARBOPOL

ENHANCEMENT OF BIOAVAILABILITY OF NORFLOXACIN MUCOADHESIVE SUSPENSION BY USING DIFFERENT GRADES OF CARBOPOL

Formulation of mucoadhesive suspension: Best suspension was selected on the basis of optimum particle size, surface area, saturation solubility and zeta potential.. Suspension prepared w[r]

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SOLUBILITY ENHANCEMENT OF ATORVAQUONE USING SOLID DISPERSION TECHNIQUEM. Rajeev Kumar, Dr.Y.Ankamma Chowdary, B.Satyanarayana, Sk. Vajid PashaDOWNLOAD/VIEW

SOLUBILITY ENHANCEMENT OF ATORVAQUONE USING SOLID DISPERSION TECHNIQUEM. Rajeev Kumar, Dr.Y.Ankamma Chowdary, B.Satyanarayana, Sk. Vajid PashaDOWNLOAD/VIEW

all the solid dispersions as the ratio of carrier is increased. Highest solubility was observed with lipophilic carrier gelucire 44/14 and it was also observed that the solubility was slightly higher with solvent evaporation method than melting method. Table 12: Saturation solubility studies of solid dispersions prepared with Kollidon VA 64 S. No.

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Preparation and In vitro Evaluation of Solid Dispersion of Finasteride

Preparation and In vitro Evaluation of Solid Dispersion of Finasteride

Saturation Solubility is the extreme amount of a solute that dissolved in a specified solvent; such solution were prepared by adding extra quantities of FNS in distilled water and chloroform and shacked by shaker water bath for 10 min at 30°C. Filtration of solution was performed to exclude any unsolvable particles that might disturb the results. The results of saturation solubility study are shown in Table 3.

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DESIGN AND DEVELOPMENT OF FAST DISSOLVING TABLETS OF HYDROCHLOROTHIAZIDE AND ATENOLOL CO CRYSTALS

DESIGN AND DEVELOPMENT OF FAST DISSOLVING TABLETS OF HYDROCHLOROTHIAZIDE AND ATENOLOL CO CRYSTALS

ABSTRACT: Hydrochlorothiazide (HCT) is a class IV drug which has limited solubility and permeability, for overcome this problems co-crystallization method is used. Co-crystallization is the process to enhance the physical properties of drug molecule especially the solubility. HCT belongs to diuretic category and Atenolol (ATL) belongs to Beta blocker category they are combined for use in tablet formulation. Co-crystallization was used to combine two drugs in single solid phase and thus to achieve new approach for combination therapy to treat hypertension. Using the new approach co-crystals of ATL with HCT was prepared. Co-crystallization of two drugs were carried out by using solvent evaporation and solution co-crystallization method. The saturation solubility was done to evaluate the solubility of co-crystals. Comparative drug release study was carried out between co-crystals and marketed formulation. The prepared co- crystals have shown several times faster release than marketed tablet and co-crystals were characterized by using DSC, FTIR and SEM. INTRODUCTION: Hydrochlorothiazide (HCT) is
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An Alkali Activated Binder for High Chemical Resistant Self Leveling Mortar

An Alkali Activated Binder for High Chemical Resistant Self Leveling Mortar

The sodium hydroxide concentration of over 5.5 mol/l did not further increase the 3-point bending tensile strength, because the saturation point with respect to the solubility of the bin[r]

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