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Objective: The objective of the present work is to develop a bi-layer tablet consisting of an Immediate Pulse Release [IPR] layer and a sustained release [SR] layer that can produce a distinct biphasic release having two different drug release rates. The IPR layer is intended to release a fraction of the dose rapidly at a faster rate and the SR layer is meant for slow release of the remaining dose at a slower rate for a desired period of time. Methods: The quantitative determination was carried out by UV spectrophotometer. Solid dispersion was prepared by melt method. IPR layer was prepared by direct compression method, SR layer was prepared by wet granulation method. In-vitro drug release study from tablets was carried out in USP II tablet dissolution rate test apparatus. FTIR, DSC, XRD studies were performed. Results: 89% of the incorporated drug was released within 30 min in acid solution of pH 1.2 from the IPR tablet prepared with the highest amount of gelucire due to solid state transformation of the drug. The SR layer (SR8) comprising of SAL, CG and CMC produced prolonged drug release (70% in 10 h). The optimized IPR3 layer and SR layers were compressed to form bi-layer tablets from which 23-37% drug was released immediately in 30 min, and the remaining drug was released slowly for 7 to 10 h depending upon the compositions of the tablets. Conclusion: This study revealed that bi-phasic release of GPZ consisting of an initial quick release and subsequent slow release could be achieved by formulating bi-layer tablets using the existing tablet technology, and such formulation may be able to control hyperglycaemia effectively for a longer period of time © 2015, International Journal of Pharmacy and Pharmaceutical Science. All rights reserved.

World University root node

Department of Chemistry

International Journal of Pharmacy and Pharmaceutical Sciences

Quick/slow biphasic release of a poorly water soluble antidiabetic drug from bi-layer tablets

The study was designed with an aim to evaluate the protective effects of reduced glutathione on cyclophosphamide induced lipid peroxidation and also changes in cholesterol content. Goat liver and white New Zealand rabbit were used as lipid source for the models. Lipid peroxidation study was performed by measuring the malon-dialdehyde, 4-hydroxy-2-nonenal, reduced glutathione and nitric oxide content of tissue homogenates or rabbit blood. In the cholesterol profile total cholesterol and high density lipoprotein cholesterol content of rabbit blood was determined. The data presented in this work demonstrate the lipid peroxidation induction potential of cyclophosphamide and the antiperoxidative potential of reduced glutathione on cyclophosphamide-induced lipid peroxidation. It was also observed that reduced glutathione has protective effect on cyclophosphamide-induced changes in cholesterol content. A significant correlation was also found between malondialdehyde, 4-hydroxy-2-nonenal with total cholesterol as well as between reduced glutathione and nitric oxide with HDL cholesterol. These findings from both in vitro as well as in vivo models indicate the lipid peroxidation induction potential of cyclophosphamide which may be related to its toxic potential. The results also suggest the antiperox-idative effects of reduced glutathione and demonstrate its potential to reduce cyclophosphamide-induced lipid peroxidation and thus to increase therapeutic index of the drug by way of reducing toxicity that may be mediated through free radical mechanisms.

Iranian Journal of Pharmaceutical Sciences

Cyclophosphamide-induced lipid peroxidation and changes in cholesterol content: Protective role of reduced glutathione

The aim of this study was to develop topical hydrogels containing diclofenac potassium (DP) at 1% w/v concentration using conventional hydrophilic hydroxypropyl methyl cellulose (HPMC, 50cPs) and modified hydrophobic hydroxypropyl methyl cellulose (HPMC, 90L grade). The differences between in vitro release profiles of both types of polymer based hydrogels were studied using model dependent equations. Three formulations were prepared from hydrophobic HPMC at 1%, 1.5% and 2% (w/v) concentration. Other two formulations were prepared from hydrophilic HPMC at 12% and 15% (w/v) concentration. Hydrophobic formulations of higher viscosity with small quantity of polymer show higher release compared to hydrophilic formulations of lower viscosity with higher polymer concentration. Combined effect of swelling and erosion leads to anomalous diffusion in case of hydrophobic HPMC based hydrogels whereas only swelling leads to Fickian diffusion in case of hydrophilic HPMC based hydrogels. The formulations follow Higuchi release pattern as well as Weibull model.