IMPROVEMENT OF ORAL BIOAVAILABILITY OF AZILSARTAN MEDOXOMIL BY LIPID BASED LIQUISOLID COMPACTS: IN VITRO AND IN VIVO EVALUATION

Abstract

The main objective of the current research work is to improve the oral bioavailability of azilsartan medoxomil (BCS Class IV molecule) using lipid based liquisolid approach. Azilsartan liquisolid compacts (ALC) have been prepared using Capmul MCM and Captex as lipid based non-volatile vehicles, Pearlitol SD 200, Avicel PH 102 and Flowlac 90 as carrier’s materials and Syloid® 244FP as a coating material. Carrier to coating material ratio was fixed as 5:1. Percentage of drug in the lipid based non volatile liquid was fixed as 50%w/w. Prepared formulations were evaluated for their micromeritics properties, solubility, dissolution and in vivo bioavailability in selected rats. Among the formulations prepared, formulation (ALC4) containing Capmul MCM as vehicle, Pearlitol SD 200 as carrier has shown enhanced drug release (99.8 ± 1.5 % release in 30 minutes) and solubility (82.54mg/mL) compared to other formulations. Hence, this formulation is evaluated for comparative in vivo bioavailability in rats along with pure drug and marketed formulation (Zilarbi). It was found that relative bioavailability of ALC 4 was increased by 1.29 times compared to pure drug and increased by 1.22 times compared to marketed formulation. Hence, the study demonstrated that lipid based liquisolid technology can lead to improve the bioavailability of poorly soluble drugs like azilsartan medoxomil significantly.