Abstract

FORMULATION AND IN VITRO EVALUATION OF IN-SITU GELLING LIQUID SUPPOSITORY OF PROMETHAZINE HCL

Iman S. Jaafar and Ameera A. Radhi*

Abstract

The aim of this study was to formulate and in vitro evaluate a thermogelling mucoadhesive liquid suppositories of promethazine HCl(PMZ HCl) in order to improve the bioavailability, and decreases the side effects as the absorbed drug avoids liver’s first pass metabolism. Poloxamers P407 and P188 were used as thermo- gelling agents and Hydroxypropyl methyl cellulose (HPMCK4M) as mucoadhesive polymer. Thirteen formulas were prepared using cold method and were evaluated for gelation temperature, gel strength, and bioadhesive force and In-vitro release rate. Gelation temperature was significantly increased with incorporation of 12.5 % w/v PMZ HCl while decreased with addition of mucoadhesive polymer. The polymer increased the gel strength and the mucoadhesive force of the prepared solutions but significantly decreased the release rate. Among the formulations examined, the P407/P188/HPMC (16/4/0.5 % w/v) and P407/ P188/ HPMC (16/4/0.75 %w/v) that were used in formulas F9 and F10, respectively, were selected as the bases of choice for PMZ HCl liquid suppository since they exhibited optimum physical properties of gelation temperature, gel strength, high mucoadhesive force and a moderate PMZ HCl in-vitro release. Therefore, these gels represent a promising alternative to conventional suppositories and might be applicable for the development of in situ gelling and mucoadhesive liquid suppository for humans as a more convenient and effective rectal dosage form.

Keywords: Thermogelling mucoadhesive, Poloxamers, Hydroxypropyl.