Abstract

PREPARATION & EVALUATION OF EPROSARTAN MESYLATE SOLID DISPERSIONS

Rewar S*, Bansal BK, Shakya.V, Singh CJ, Sharma AK

ABSTRACT

The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique. Solubility and dissolution rate is an important physicochemical factor affecting absorption of drug and its therapeutic effectiveness. Consequences of poor aqueous solubility would lead to failure in formulation development. The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. In the present investigation, an attempt was made to improve the solubility and dissolution rate of a poorly soluble drug, Eprosartan by solid dispersion method using skimmed milk powder as carrier. Four different formulations were prepared with varying drug:carrier ratios viz.1:1, 1:3, 1:5 and 1:9 and the corresponding physical mixtures were also prepared. The formulations were characterized for solubility parameters, drug release studies and drug-polymer interactions by using phase solubility studies, dissolution studies; XRD analysis, FTIR spectrum, TLC analysis and UV overlay spectra. All the formulations showed marked improvement in the solubility behaviour and improved drug release. Formulation containing drug: polymer ratio of 1:9 showed the best release with a cumulative release of 82.67 % as compared to 6.919 % for the pure drug. The interaction studies showed no interaction between the drug and the carrier. It was concluded that skimmed milk powder as a carrier can be very well utilized to improve the solubility of poorly soluble drugs.

Keywords: Solid Dispersion, Skimmed milk powder, solubility, Eprosartan, Dissolution.