Semi solid matrix formulations of meloxicam and tenoxicam: an in vitro and in vivo evaluation

摘要

The objective of this study was to improve the dissolution and subsequently the therapeutic efficacy of poorly water soluble BCS class-II drugs meloxicam and tenoxicam, by lipid semi solid matrix (SSM) systems filled in hard gelatin capsules by liquid fill technology. The present research involved preparation of SSM formulations using Gelucire 44/14 as a carrier due to its self emulsifying, wetting and hydrophilic properties. The SSM capsules were characterized by assay, in vitro dissolution studies, moisture uptake, FTIR and DSC. The optimized formulations were also evaluated for their in vivo anti inflammatory activity in rat model. Six to ten fold enhancement in vitro drug release, in both acidic and basic media, was obtained with formulations containing drug to carrier in 1: 6 ratio. The absence of drug peak in DSC scans indicated complete dissolution of the drug in carrier, while IR revealed no chemical interaction of pure drug and Gelucire 44/14. The optimized SSM formulations of meloxicam and tenoxicam showed a rapid decrease in paw edema with a significant increase in anti-inflammatory activity. The SSM formulations were successful in providing rapid release of drugs with improved dissolution and in vivo anti-inflammatory activity by liquid fill technology in hard gelatin capsules.