Abstract

DOUBLE PHASE MODIFIED RELEASE SUPPOSITORY FOR RELIEVING VAGINAL INFECTION: PREPARATION AND IN-VITRO CHARACTERIZATION

Mr. Mehul B. Ranpariya*, Dr. Ramesh B. Parmar

ABSTRACT

Majority of the case of vaginal infection are due to yeast infection are commonly encountered in clinical practice. Clinical manifestation of vaginal infection includes inflammation and associated pain. Hence, the aim of present investigation is to prepare modified release suppository by using the antifungal agent as voriconazole and NSAID as ketorolac tromethamine as a drug to treat vaginal infection. Matrix tablets prepared by direct compression method by using carbopol 971P and HPMC K4M as sustained release polymer. A 32 full factorial design was used to study the effect of polymers on % drug release and swelling index. The responses were analyzed using ANOVA and by polynomial equation. Suppositories were prepared by molding method by using poloxamer 407 and 188 as suppository base. The optimized formulation of matrix tablet (batch F4) has shown 98.99% in vitro drug release at end of 12 hr and 1.8 swelling index at end of 6 hr. Adhesion force was found to be 1.0982 N which is sufficient to retain the tablet in vagina for more than 12 hr. Ex vivo permeation and drug retention studies of modified release suppositories shows voriconazole (%Drug retention 81.23%) gives local effect while ketorolac tromethamine (%CADP 83.56%) reach to the systemic circulation. Stability study shows that there was no significant change in appearance, physical integrity and drug content. Modified release suppository was considered as suitable formulation for sustained release ketorolac tromethamine and conventional release voriconazole.

Keywords: Voriconazole, Ketorolac tromethamine, Modified release suppository, Vaginal infection.