Gourishankar Institute of Pharmaceutical Education and Research

Sātāra, India

Gourishankar Institute of Pharmaceutical Education and Research

Sātāra, India
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Ghorpade V.S.,YSPMs Yashoda Technical Campus | Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research | Dias R.J.,YSPMs Yashoda Technical Campus
Carbohydrate Polymers | Year: 2017

Citric acid crosslinked β-cyclodextrin–carboxymethylcellulose (βCD-CMC) hydrogel films were prepared by esterification-crosslinking method for the controlled release of ketoconazole (model drug). The hydrogel films were evaluated for active βCD content, carboxyl content, swelling ratio, drug loading and release, and hemolytic activity. The structural characterization was carried out using solid state 13C NMR, ATR-FTIR, TGA and DSC analysis. The βCD-CMC hydrogel films showed increase in active βCD content swelling ratio and drug loading with increase in the concentration of βCD in the feed. The βCD helped to minimize the burst effect and retarded the release of ketoconazole. The hydrogel films were found to be biocompatible and capable of controlling the release of ketoconazole for long duration. © 2017 Elsevier Ltd


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research | Murthy S.M.,Vignan Institute of Pharmaceutical Sciences
DARU, Journal of Pharmaceutical Sciences | Year: 2012

Background and the purpose of the study. Carvedilol nonselective β-adrenoreceptor blocker, chemically (±)-1-(Carbazol-4-yloxy)-3-[[2- (o-methoxypHenoxy) ethyl] amino]-2-propanol, slightly soluble in ethyl ether; and practically insoluble in water, gastric fluid (simulated, TS, pH 1.1), and intestinal fluid (simulated, TS without pancreatin, pH 7.5) Compounds with aqueous solubility less than 1% W/V often represents dissolution rate limited absorption. There is need to enhance the dissolution rate of carvedilol. The objective of our present investigation was to compare chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol. Methods. The different formulations were prepared by different methods like solvent change approach to prepare hydrosols, solvent evaporation technique to form solid dispersions and cogrind mixtures. The prepared formulations were characterized in terms of saturation solubility, drug content, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), electron microscopy, in vitro dissolution studies and stability studies. Results: The practical yield in case of hydrosols was ranged from 59.76 to 92.32%. The drug content was found to uniform among the different batches of hydrosols, cogrind mixture and solid dispersions ranged from 98.24 to 99.89%. There was significant improvement in dissolution rate of carvedilol with chitosan chlorhdyrate as compare to chitosan and explanation to this behavior was found in the differences in the wetting, solubilities and swelling capacity of the chitosan and chitosan salts, chitosan chlorhydrate rapidly wet and dissolve upon its incorporation into the dissolution medium, whereas the chitosan base, less water soluble, would take more time to dissolve. Conclusion: This technique is scalable and valuable in manufacturing process in future for enhancement of dissolution of poorly water soluble drugs. © 2012 Shete et al.


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research | Murthy M.S.,Vignan Institute of Pharmaceutical Sciences
Indian Journal of Pharmaceutical Education and Research | Year: 2012

The objectives of present investigations were to enhance dissolution rate of irbesartan by using chitosan and chitosan chlorhydrate and optimize an effective concentrations of both. Cocrystals of irbesartan (IB) were prepared by solvent change technique.Chitosan solution was prepared by soaking chitosan and chitosan chlorhydrate in glacial acetic acid. A weighed amount of drug was dispersed in chitosan solution by stirring. The dispersion was added to sodium citrate solution to precipitate chitosan on drug crystals. The precipitate obtained was filtered through Whatmann No. 1 filter paper using vacuum filtration unit and dried at 45° C for 24 h. The prepared cocrystals were characterized in terms of saturation solubility, drug content, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), in vitro dissolution studies and stability studies. The considerable improvement in the dissolution rate of drug from optimized co-crystal formulation was attributed to the decreased drug crystallinity, altered surface morphology and reduction in particle size. The 0.2% chitosan and 0.4% chitosan chlorhydrate were found to be optimized concentrations for enhancement of dissolution rate of irbesartan. The technique is scalable and mayprove valuable in manufacturing process in futureforenhancement of dissolution of poorly watersoluble drugs.


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research | Murthy M.S.,Vignan Institute of Pharmaceutical Sciences | Sakhare S.,Gourishankar Institute of Pharmaceutical Education and Research
Indian Journal of Pharmaceutical Education and Research | Year: 2011

Stability testing is the primary tool used to assess expiration dating and storage conditions for pharmaceutical products. Many protocols have been used for stability testing, but most in the industry are now standardizing on the recommendations of the International Conference on Harmonization (ICH). These guidelines were developed as a cooperative effort between regulatory agencies and industry officials from Europe, Japan, and United States. Proper design, implementation, monitoring and evaluation of the studies are crucial for obtaining useful and accurate stability data. Stability studies are linked to the establishment and assurance of safety, quality and efficacy of the drug product from early phase development through the lifecycle of the drug product. Liposomes have been extensively investigated for drug delivery, drug targeting, controlled release and enhancing solubility. However the major limitation in the widespread use of this versatile drug delivery system is its instability. In present review the methods like control of the particle size, lipid composition, method of drug loading, prodrug, pro-liposomes, lyophilization and electrosteric stabilization are reviewed to enhance the physical, chemical and biological stabilities of the liposomes collectively because all are inter-related.


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research
Indian Journal of Pharmaceutical Education and Research | Year: 2010

Liquisolid compacts were used to formulate water insoluble drugs in non-volatile solvents and converting into acceptably flowing and compressible powders. The objectives of present investigations were formulation and evaluation orodispersible liquisolid compacts of aceclofenac by using different dissolution enhancers and study the effect of way of addition of superdisintegrants on rate dissolution of aceclofenac. Liquisolid compacts of aceclofenac were prepared by dispersing the drug in various dissolution enhancing agents(Propylene glycol, Polyethylene glycol 400 and Tween 80 in 1:1 ratio with drug), then addition of diluents, superdisintegratns (like Cross carmelose Sodium, Cross povidone and Sodium starch glycolate) in various ways and in combinations finally addition of glidants and lubricants. Before compactions powdered mass were evaluated for flow properties. Compacts were evaluated for disintegration test, weight variation test, in vitro dissolution study, friability Test, wetting time, hardness Test and data was analyzed statistically. All liquisolid compacts being orodispersible rapidly disintegrate within 3 minutes with enhanced dissolution properties over the conventional tablet of aceclofenac. Among all formulations, Tween 80 liquisolid compact containing cross carmelose sodium showed highest dissolution. The combination of superdisintegrants enables us to study the effect of combined disintegrating action on drug release. Among this, compacts with Sodium starch glycolate added intragranularly and cross povidone extra granularly showed highest dissolution rate. Aceclofenac release from tablets followed Peppas model. Orodispersible liquisolid compacts prepared with Tween 80 enhance the dissolution rate of aceclofenac to a greater extent. Hence liquidsolid compacts and way of addition of superdisintegratns is useful technique in enhancement of dissolution rate of aceclofenac. © APTI All rights reserved.


Sakhare S.,Gourishankar Institute of Pharmaceutical Education and Research
Indian Journal of Pharmaceutical Education and Research | Year: 2010

In this work, the dissolution-absorption studies were conducted on marketed tablets of acyclovir (ACIVIR-200mg) and the mucoadhesive tablets of acyclovir using varying concentration of sodium lauryl sulfate as a permeation enhancer. The purpose of this study was to improve the absorption of acyclovir using sodium lauryl sulfate as permeation enhancer. The everted and perfused intestine model was used to study the permeation of mucoadhesive tablets of acyclovir. The studies yielded dissolution-absorption relationship that can be used to predict dissolution or permeation-rate-limited absorption for formulated and marketed formulations. The results showed that marketed tablets of acyclovir had less permeability coefficient (0.778 × 10 cm/sec) as compared to mucoadhesive tablets with varying concentrations of sodium lauryl sulfate. The permeability increased with increasing concentration of sodium lauryl sulfate and permeability coefficient for mucoadhesive tablets with 4% sodium lauryl sulfate was found to be 5.231x 10 cm/sec Amongst the varying concentrations of sodium lauryl sulfate used, 4% of sodium lauryl sulfate in the dissolution medium of mucoadhesive tablet of acyclovir showed highest increase in permeation of acyclovir therapy increasing the bioavailability of acyclovir. © APTI All rights reserved.


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research
Indian Journal of Pharmaceutical Sciences | Year: 2015

The present investigation deals with formulation of nicotinamide-based co-crystals of fenofibrate by different methods and solid-state characterization of the prepared co-crystals. Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods. The prepared molecular complexes were characterized by powder X-ray diffractometry, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy and in vitro dissolution study. Considerable improvement in the dissolution rate of fenofibrate from optimized co-crystal formulation was due to an increased solubility that is attributed to the super saturation from the fine co-crystals is faster because of large specific surface area of small particles and prevention of phase transformation to pure fenofibrate. In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate. Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.


Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research
Artificial Cells, Blood Substitutes, and Biotechnology | Year: 2012

To have advantages of reduced dosing frequency, improved bioavailability and effective delivery system of Cefuroxime Axetil, a Chitosan based intragastric sustained release microbead formulation of Cefuroxime Axetil was developed. The drug delivery system was prepared by ionotropic gelation of Chitosan in presence of sodium tripolyphosphate as polyanion and optimized by box-behnken experimental design. Response surface methodology was applied to evaluate various vitro characteristics of prepared mucoadhesive microbeads. Multiple independent variables were optimized to achieve responses of interest, thereby to get the desired sustained release profile of Cefuroxime Axetil in gastric environment. © 2012 Informa Healthcare USA, Inc.


Shete A.,TAL Group | Murthy S.,Vignan Institute of Pharmaceutical Sciences | Korpale S.,TAL Group | Yadav A.,Gourishankar Institute of Pharmaceutical Education and Research | And 3 more authors.
Journal of Drug Delivery Science and Technology | Year: 2015

Itraconazole (ITZ) is an antifungal compound and a weak base with log P of 6.2 with an extremely low aqueous solubility 5 μg/ml, and high permeability, and consequently belonging to Biopharmaceutical Classification System Class II. The objectives of present investigation were to determine Hansen solubility parameters, synthesis, solid state characterization, in vitro drug release and antifungal activity of itra-conazole cocrystals. The different formulations were prepared by neat and cocktail cogrinding with different amino acids like aspartic, glycine, proline, serine and succinic acid as a coformer. The prepared formulations were characterized in terms of saturation solubility, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), in vitro dissolution studies and in vitro antifungal activity. In DSC studies ITZ amino acids cocrystals showed depression in melting point, whereas difference in δ values were below 5 and the prepared complex can be called as cocrystals. The results revealed considerable changes in the IR peaks of Itraconazole in the prepared co-crystals when compared to pure drug thereby indicating the presence of hydrogen bonding and π-π bonding in the newly formed cocrystals. Cocrystallization of Itraconazole resulted in five novel cocrystal forms including four cocrystals and one cocktail cocrystal with improved in vitro antifungal activity. © 2015 Elsevier B.V. All rights reserved.


Ghorpade V.S.,YSPMs Yashoda Technical Campus | Yadav A.V.,Gourishankar Institute of Pharmaceutical Education and Research | Dias R.J.,YSPMs Yashoda Technical Campus
International Journal of Biological Macromolecules | Year: 2016

The present communication deals with preparation of β-cyclodextrin (βCD) grafted hydroxypropylmethylcellulose (HPMC) hydrogel films using citric acid as crosslinking agent with the aim of improving the loading and achieving controlled release of hydrophobic weak base (ketoconazole). The hydrogel films were characterized by attenuated total reflectance-fourier transform infrared (ATR-FTIR) spectroscopy, solid state 13C-nuclear magnetic resonance (13C NMR) spectroscopy, thermal analysis and scanning electron microscopy (SEM). The films were evaluated for βCD content, carboxyl content, swelling ratio, drug loading, drug release and hemolytic assay. ATR-FTIR spectra indicated crosslinking via ester formation whereas 13C NMR, thermal analysis and SEM confirmed βCD grafting. The βCD grafted hydrogel films with high carboxyl content showed maximum swelling and high drug loading. The presence of grafted βCD helped to retard the release of ketoconazole from the hydrogel films. The hemolytic assay suggested the biocompatible nature of the hydrogel films. Altogether, βCD grafted HPMC hydrogel films were found to be suitable for delivery of poorly soluble weak bases. © 2016 Elsevier B.V.

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