Recent epidemiological studies suggest that postprandial hyperglycemia is an independent risk factor for cardiovascular disease. A human's high carbohydrate diet majorly consists of a high carbohydrate diet and α-glucosidase is a glucosidase located in the brush border of the small intestine is involved in glycosidic cleavage of starch at α-glycosidic bonds. α-glucosidase inhibitors are a unique class of anti-diabetic drugs particularly useful in individuals with a high carbohydrate diet. α-glucosidase inhibitors works by competitively inhibiting the enzyme α-glucosidase at the brush border of the small intestines, thus delaying the digestion of complex carbohydrate and intestinal absorption of glucose. Hence, in the present study, the α-glucosidase inhibition activity of butyl isobutyl phthalate isolated from chloroform fraction of Rubus steudneri leaves investigated and its possible mechanism of action ascertained in silico. The compound was found to exhibit concentration-dependent inhibition of α-glucosidase with half-maximal inhibitory concentration value of 10.68 g/ml. The results of in vitro α-glucosidase inhibition assay for butyl isobutyl phthalate were promising and substantiated by molecular docking and molecular dynamics studies.

Lercanidipine hydrochloride (HCl) is L-type calcium channel blocker widely used in the management of hypertension. According to the BCS classification system, it is classified under BCS class II drugs, showing low solubility and high permeability. The dissolution profile and thus the in vivo performance of this class of drugs widely depend on their solubility and hence their behaviour in dissolution medium. Lercanidipine HCl is not official in any pharmacopeia, so no official dissolution method is available. The present work is mainly focussed on development and validation of a dissolution test that can be used as a quality control test for lercanidipine HCl tablets and formulations. Saturation solubility and sink conditions that can be achieved in different media suggested that 0.1 N HCl, acetate buffer pH 4.5, and phosphate buffer pH 6.8 can be used as a dissolution medium. Dissolution tests of lercanidipine HCl tablets were carried out in these different media at different rotation speeds using a USP type II (paddle) apparatus. The most suitable dissolution conditions were 0.1 N HCl pH 1.2 (900 mL at 37 ± 0.5 °C) as a dissolution medium and a paddle apparatus at 100 rpm for 60 min. The analysis of released lercanidipine HCl was done by ultraviolet spectrophotometry. The developed method was validated according to ICH guidelines. This method showed linearity with an r 2 value of 0.999 within the concentration range of 2-20 µg/mL. The method was found to be accurate with recoveries ranging from 98.50% to 103.72%. The interday and intraday precision was below RSD 2%. The developed method can effectively be used for quality control evaluation of lercanidipine HCl tablets.

Objective: It is always challenging to prepare the floating gastro retentive formulation of the high dose drug. The present research was aimed to prepare gastro retentive controlled release, matrix tablets of metformin, using the combination of different ionic, anionic and polyanionic polymers with HPMC.Methods: Formulations were prepared using sodium alginate, pullulan, kappa carrageenan, xanthan gum, poloxamer 68 in combination with HPMC K15M. All matrix tablets were prepared by direct compression method and evaluated for swelling, floating adhesive period and drug release.Results: All the tablets showed acceptable physicochemical properties. Statistical analyses of data revealed that tablets prepared using HPMC K15M and kappa carrageenan, formulation F2, is best in terms of showing excellent floating properties, extended adhesion periods and sustained drug release characteristics with similarity factor as 92 on comparison with the theoretical release of the drug. Conclusion:The combination of HPMC K15M and kappa carrageenan can be further optimized by applying the appropriate statistical design.

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Introduction: Microsponges provides a proficient drug delivery system for specific delivery in the upper gastrointestinal tract with high drug loading capability. But the formulation is affected by numerous process and design related factors. The intention of the current research work was to formulate and optimize the floating gastroretentive microsponges of glipizide, an antidiabetic drug, with minimum number of experiments, by applying an appropriate experimental design. Methods: The decisive factors affecting formulation were screened by Plackett-Burman design and the final optimization were performed by applying Box-Behnken design. In Plackett-Burman design, Pareto ranking analyses indicated that polymer concentration, stirring speed and temperature significantly affected the formulation of microsponges. The influence of these independent variables was checked on the entrapment efficiency, buoyancy and cumulative drug release (12hr) of the formulation by Box-Behnken design. Results: The results of Box-Behnken design showed that after applying the desirability criteria and looking into overlay plots, formulation GBB-8 with medium drug-polymer ratio and maximum level of the other two variables was found to be optimum with desirability near 1. The formulation gave entrapment efficiency as 90.81%, buoyancy as 92.3% and CDR 12 as 92.3%. Radiographic studies conducted on albino rabbits, indicated the presence of the microsponges in the stomach for 12hr. Conclusion: It could be concluded that application of experimental design is helpful tool for the development of floating microsponges of glipizide. The prepared formulation can offer the sustained release of the drug at its site of absorption which may provide the better control of the diabetes due to less fluctuation in plasma drug concentration.