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Auti P.B.,Maharashtra Institute of Pharmacy
Mini-Reviews in Medicinal Chemistry | Year: 2014

The 1, 4-dihydropyridines (DHPs), a class of drugs possess a wide variety of biological and pharmacological actions. It represents one of the most important groups of calcium-channel modulating agents and has experienced widespread use in the treatment of cardiovascular disease which includes antihypertensive, antianginal, vasodilator and cardiac depressants activities. It also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, CFTR, antimalarials, neuroprotection properties, HIV-1 protease inhibitors, antifertility activities and many more. There are many drugs available in market which contains 1, 4-dihydropyridines ring as basic scaffold. Basic motive of this review is to disclose various therapeutic applications of 1, 4-dihydropyridine derivatives reported by other researchers during their research work in 2001 to 2011. ©2014 Bentham Science Publishers.

Sangshetti J.N.,Dr. Babasaheb Ambedkar Marathwada University | Chabukswar A.R.,Maharashtra Institute of Pharmacy | Shinde D.B.,Dr. Babasaheb Ambedkar Marathwada University
Bioorganic and Medicinal Chemistry Letters | Year: 2011

Sodium bisulfite has been reported first time for the synthesis of 2,5-disubstituted 1,3,4-oxadiazole using microwave and conventional method in ethanol-water. The yields obtained are in the range of 90-95% using microwave and 87-91% using conventional method. All the synthesized compounds (8a-8s) are novel and were evaluated for their in vitro antifungal activity. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Some of the compounds from the series like 8k was equipotent with miconazole against Candida albicans and Fusarium oxysporum. Also compound 8n was equipotent with miconazole against F. oxysporum. © 2010 Elsevier Ltd. All rights reserved.

Pangarkar P.A.,Maharashtra Institute of Pharmacy
International Journal of Pharmacy and Technology | Year: 2013

More than one third of drug in pharmaceutical industry show polymorphism. These polymorphic or crystalline drugs have their stringent and specific physicochemical properties. These stringencies regarding physicochemical properties make it difficult for the formulation of such drugs into suitable dosage form. Various methods are available for the improvement of physiochemical properties of these medicinal agents, but most of the time they fail to give the satisfied results. To resolve all these complications, the prior study of polymorphic properties can be very helpful. Crystalline drugs always have their thermodynamic as well as kinetic properties. As such these properties make them crystalline but at the same time these drugs get it difficult for ideal formulation. This review covers the information regarding drug polymorphism as detail as possible. The methods, newer techniques in the field of crystallization, sophisticated techniques for the characterization of crystal forms and the regulatory consideration have been discussed in detailed. The role of crystallization processes in pharmaceutical science and technology can be associated, both, with its influence on the solid-state properties of the drug substances and with an effect on drug product stability and performance. The concept of crystal and particle engineering applied to pharmaceutical substances requires, first of all, reproducibility and consistency of the solid-state properties.

Jagdale S.,Maharashtra Institute of Pharmacy
Current drug delivery | Year: 2013

Simvastatin is a hypolipidemic drug used in atherosclerosis. It has short elimination half life (2-3 hours) and narrow absorption window. It is mainly absorbed from stomach. The objective of this research was to develop gastroretentive floating tablets of Simvastatin using combination of release retardant polymers like Polyox WSR 205, Polyox WSR N12K and HPMC K4M. Material and methods: 3(2) full Factorial design was applied to design the experiments and tablets were prepared by direct compression. Prepared floating tablets were evaluated for hardness, floating time, friability, % drug content, swelling index, in-vitro drug release study and mean gastric retention period by invivo X-ray study. Statistical analysis was done using design expert software and model fitting was carried out using PCP DISSO. Design expert software was validated by comparing predicted results with observed results. Statistical analysis data revealed that tablets from formulation batch D3 (containing HPMC K4M 10% and POLYOX WSR 205 35%) and formulation batch E2 (HPMC K4M 10% and Polyox WSR N12K 25%) were promising system exhibiting excellent floating properties and drug release pattern. Stability studies revealed that all formulations were physically and chemically stable. In-vivo X-ray imaging of formula D3 and formula E2 shows mean gastric retention time of 6 ± 0.5 hours.

Thombre N.A.,Maharashtra Institute of Pharmacy | Gide P.S.,Maharashtra Institute of Pharmacy
Carbohydrate Polymers | Year: 2013

The galactomannan from the seeds of Caesalpinia pulcherrima L. was isolated and purified by precipitation method using alcohol to get C. pulcherrima (CP) gum. CP gum was studied for its physicochemical and rheological properties. The composition of CP gum was found to contain mannose:galactose:glucose:xylose in a proportion of 2.8:1:0.1:0.08, with M/G ratio 2.80. The molecular weight (M w) for CP gum was obtained to be approximately 2.72 × 10 6 Da by static light scattering measurements and 2.79 × 10 6 Da using Mark-Houwink relationship. The intrinsic viscosity by Huggins and Kraemer plots using capillary viscometry was obtained as 12-12.5 dl/g. The rheological behavior of aqueous galactomannan solutions was studied at 25 °C, using steady-shear and dynamic oscillatory measurements. The various concentrations of CP gum exhibits shear thinning non Newtonian behavior at high shear rate and Newtonian flow at low shear rate. Experimental data in steady shear has been correlated and found a better fitting with the Cross and Carreau models. A graph of the specific viscosity at zero shear rate (ηsp0) against coil overlap parameter (C[η]) was plotted and the slope of the lines in dilute and semi-dilute regions were found to be 1.23 and 4.1 respectively. The critical concentration (C*) was found to be about 3.8/[η]. The linear viscoelastic region for CP gum solutions presented nature as that of macromolecular solutions. At all shear rates and frequencies, ηap and η* had almost similar magnitudes, which shows its reasonable agreement with the Cox-Merz rule. The present investigation shows the suitability of CP gum as a pharmaceutical aid application like viscosity modifier, release retardants, binders. © 2013 Elsevier Ltd. All rights reserved.

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