ABSTRACT:
Telmisartan is a biopharmaceutical classification system (BCS) class II drug that has low solubility in biological fluids, which results into poor bioavailability after oral administration.The purpose of this research work was to improve the solubility and therefore the rate of dissolution of telmisartan in pH 1.2, 4.5 and 7.5(FDA recommended) buffers as the dissolution media using spray drying technique. Nanodispersion of telmisartan was prepared by using various proportion of drug: PVP-K30 ratios (1:1 to 1:4). The prepared nanodispersion was subjected to in-vitro dissolution, particle size distribution, FT-IR spectroscopy, and PXRD, DSC and SEM studies. The results indicated that formulation containing drug: PVP-K30 ratio of 1:4, prepared by spray drying technique showed the cumulative release of 99.84% as compared to 9.36% for the pure drug in pH 7.5 phosphate buffers and also significant improvement in pH 1.2, 4.5 and water. Particle size analysis reveals that telmisartan was dispersed in the form of nanoparticles with size 2.5-6.5 r nm in PVP matrix. Absence of significant drug‐carrier interaction was confirmed by FTIR and DSC data. XPRD reveals that crystallinity nature of drug was decreased. In conclusion, the prepared nanodispersion telmisartan with PVP-K30 in ratio of 1:4 was shown higher release profile which may contribute to improved bioavailability of telmisartan.
