Abstract

COMPARISON OF COMPLEXATION, SOLID DISPERSION AND SOLID SMEDDS FOR DISSOLUTION ENHANCEMENT OF OLMESARTAN MEDOXOMIL

Vikas D Kurmi*, Dr.Shreeraj Shah and Abhishek Jain

ABSTRACT

Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The objective of this study is to compare the difference between solid self-microemulsifying drug delivery system (solid-SMEDDS), complexation and solid dispersion technology used to improve the dissolution of Olmesartan medoxomil (OLM).[1] The formulation of OLM-solid SMEDDS was composed of Acrysol K140, Tween 80, PEG 400 and Neusilin US2 which was used as solid absorbent. Olmesartan complexation was prepared using β-cyclodextrin as the carrier in different ratio (1:1, 1:2, 1:3 and 1:4) by kneading method. Olmesartan solid dispersion were prepared with PVP K30, HPMC K4M and HPMC K100M as the carrier in different ratio (1:1, 1:2, 1:3 and 1:4). The prepared formulation of solid dispersion and complexation were evaluated for phase solubility, DSC, drug content and dissolution study. . Prepared SMEDDS was evaluated for its emulsification time, drug content, droplet size, zeta potential. The optimized formulation F2 contained OLM (200 mg), Tween 80 (33%v/v), PEG 400 (33%v/v), and Acrysol K 140 (34%v/v) had shown the smallest particle size. Then it was converted in solid SMEDDS by absorbing it on Neusillin US2, and SEM & dissolution study was carried out. The dissolution of Olmesartan in solid SMEDDS was 4.88 times higher than crude Olmesartan and 1.3 times higher than Olmesartan solid dispersion product and 1.4 times higher than Olmesartan βcyclodextrin complex. In conclusion, solid SMEDDS was more efficient than the traditional solid dispersion and complexation techniques.

Keywords: Olmesartan medoxomil, ?-cyclodextrin, Acrysol K140, solid SMEDDS, Neusillin US2, phase solubility.