ENHANCED BIOAVAILABILITY OF GLIMEPIRIDE THROUGH MICROEMULSION BASED TRANSDERMAL GELS

摘要

The objective of the present research work was to conduct in vivo pharmacokinetic study of microemulsion based transdermal gel of glimepiride for evaluating the enhanced bioavailability. Saturation solubility studies of the drug were conducted in various solvents and oils. Labrafil M 1944 CS, Tween 80 and Transcutol P were used as oil phase, surfactant and cosurfactants respectively for the preparation of microemulsion based on the results from solubility studies. Surfactant to cosurfactant ratio was fixed as 1:2 in all the formulations. Microemulsion based gel was prepared using carbopol 934 as gelling agent and oil to s_mix ratio of 1:9. In vivo pharmacokinetic studies conducted in rabbits revealed that the bioavailability of microemulsion based gel was increased 5.4 times compared to oral suspension demonstrating avoidance of first pass metabolism and oral degradation. This indicates the effective management of plasma profile of glimepiride when it is administered as microemulsion based gel through transdermal route.