Formulation and Evaluation of Fluconazole Mucoadhisive Vaginal Tablets
Gamal M. Mahours *
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O.Box 2457, Riyadh 11451, Saudi Arabia.
Abdelrahman Y. Ali Sherif
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O.Box 2457, Riyadh 11451, Saudi Arabia.
Diaa Edin Z. Shaaban
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O.Box 2457, Riyadh 11451, Saudi Arabia.
Gamal A. Shazly
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O.Box 2457, Riyadh 11451, Saudi Arabia and Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, 71526, Assiut, Egypt.
*Author to whom correspondence should be addressed.
Abstract
The Mucoadhesive drug delivery system has occupied an important place in the field of pharmaceutical research. Mucoadhesive tablets prolong the residence time of the drug at the site of application and provide extended therapeutic effect. Mucoadhesive tablets have been prepared for various sites thus offering localization as swell as systemic control of drug release. The present study focuses on the concept of formulation of fluconazole as a mucoadhesive vaginal tablet, for improving the sustained release of drug and localized action of the drug. Different polymers, such as Hydoxypropylmethylcellulose M 15, Carbopol71G-NFand Guar Gum were used with different concentrations in order to get the desired sustained release profile over a period of more than12 hrs. The tablets were prepared by direct compression method. All the formulations were evaluated for crushing strength, friability, swelling behavior, adhesion time, drug content and in vitro drug release profile. All the formulation tested showed good physical and adhesive properties. It was found that the controlled release rate of the formulation increases with increasing polymer concentration. Kinetican modeling of release data supports an anomalous non-fickian release behavior. The antimycotic activity of selected formulations containing fluconazole (100 mg) was determined using an agar diffusion technique. Formulations tested showed activity against C. albicans.
Keywords: Fluconazole, mucoadhesion, vaginal tablets, in vitro release, antimycotic activity