glimepiride

The aim of this study is to develop and characterize a solidified self-emulsifying formulation of glimepiride, and to compare its in vitro drug release profile to a commercially available tablets. Several self-emulsifying formulations (SEF) were prepared by selecting different combination from constructed pseudoternary phase diagram. Selected formulations SEF1, SEF2 and SEF3 were solidified using crospovidone and evaluated. Following emulsification, the optimized formula was selected to have the smallest mean particle size and the highest absolute zeta potential, which should yield the formation of a stable emulsion and its superiority in dissolution characteristics. Particle size and distribution of SEF1, SEF2 and SEF3 were 423.36nm, 159.128nm and 115.899nm respectively. Zeta potential analysis revealed  that SEF3 had highest zeta potential – 43.78mV followed by -39.2mV (SEF2) and -39.08mV (SEF1). In vitro drug release in 30 min of formulation SEF1, SEF2 and SEF3 were 75.31%, 83.48% and 93.03% respectively. Which indicated superiority of SEF3. In vitro studies were also performed to compare the optimized formula, SEF3, to a commercially available Betaglim tablet. T50% of glimepiride in SEF3 and betaglim was found to be 7 min and 22 min respectively. Which indicated a significant improvement in glimepiride release characteristics. SEF3 was found to be stable under stressed conditions. However slightly increased globules size of sample stored at accelerated storage condition for 12 weeks was observed.

Gymnema sylvestre has been extensively evaluated for its in vitro and in vivo activity against diabetes mellitus. The leaves of the shrub Gymnema sylvestre contain a complex of pentacyclic triterpenes known as gymnemic acids that have been reported as potential therapeutic agents in the treatment of diabetes. The present study reveals the relationship between the structure and function of the medicinally important constituents of this plant. To understand the binding mechanisms of these active constituents, molecular modelling studies has been performed with dipeptidyl peptidase-4, protein tyrosine phosphatase 1B, sodium potassium ATPase, aldose reductase and glycogen synthase kinase-3β as target proteins using XP docking program of Glide, version 9.2, Schrödinger suit. These constituents showed favourable interactions with the amino acid residues at the active site, their by substantiating their proven efficacy as antidiabetic agents. The present study also gives an insight to the probable herb-drug interaction and reason for sudden hypoglycemic shocks that may occur on concurrent administration of Gymnema extract and synthetic drug, Glimepiride, for the treatment of diabetes.