FORMULATION AND EVALUATION OF THERMOREVERSIBLE IN SITU GELLING AND MUCOADHESIVE DILTIAZEM HYDROCHLORIDE LIQUID SUPPOSITORY

2010 
Objective of the present study was to develop and e valuate thermoreversible in situ gelling and mucoadhesive liquid suppositories to improve patien t compliance and systemic absorption of diltiazem hydrochloride. Thermoreversible mucoadhesive liquid suppositories were prepared by adding mucoadhesive polymers to a formulation that contained pluronic F -127, pluronic F-68 and diltiazem hydrochloride. Mucoadhesive polymers such as Carbopol 974P, Polyox WSR-301, hydroxypropyl methylcellulose, polycarbophil and polyvinylpyrrolidone were investi gated to modulate the gel strength and mucoadhesive force for diltiazem hydrochloride liquid suppositor y. Addition of these polymers reinforced the gel st rength and the mucooadhesive force of the prepared liquid suppository formulation. Increasing the concentrati on of mucoadhesive polymers retarded the release of dilti azem hydrochloride from the pluronic gel. Carbopol and polycarbophil showed highest retardation of drug re lease than other polymers investigated. Diltiazem hydrochloride formulated as mucoadhesive thermoreversible poloxamer solution for rectal administration can have potential to avoid first-pass effect through o ral route, improve the bioavailability of drug and it can be used as a safe and sustained release rectal deliver y system to control severe post-operative pain.
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