Abstract

FORMULATION AND EVALUATION OF SUSTAINED RELEASE FLOATING MICROBALLOONS OF EPROSARTAN MESYLATE

PJ. Prasuna Sundari*, Raju Gangadhari, Dr. Prathima Srinivas

Abstract

Eprosartan mesylate is an anti-hypertensive drug. It has low solubility and 13% of oral bioavailability. The objective of the present study was to improve the oral bioavailability by formulating floating microballoons of Eprosartan mesylate to prolong its gastric residence time. Microballoon formulations were prepared by solvent evaporation technique and were optimized for polymer composition and concentration, solvent systems and temperature. All formulations were evaluated for percentage yield, particle size, incorporation efficiency, buoyancy percentage and in vitro drug release. F4 was optimized and the results indicated as of incorporation efficiency 85.25 ± 0.61%, and % drug release 99.074 ± 1.29. In vivo pharmacokinetic studies were conducted in male wistar rats and the drug was assayed by HPLC. The AUC0-t and Cmax of API and microballoon formulation was 746.151±0.29ng.hr/ml, 2958.91±0.14ng.hr/ml, 164.64 ±0.23ng, 446.72±0.76ng respectively. The results indicated that F4 exhibited increased oral bioavailability due to increase in gastric residence time. The release data was fitted to different kinetic models and the drug obeys zero order kinetics and the drug release was diffusion controlled.

Keywords: Microballoons, Eprosartan, Solvent evaporation technique, Bioavailability.