ELSEVIER International Journal of Pharmaceutics 138 (1996) 67 73 international journal of pharmaceutics Preparation and evaluation of bioerodible buccal tablets containing clotrimazole Rajesh Khanna 1, S.P. Agarwal*, Alka Ahuja Department o/' Pharmaceutics, Faculty q[' Pharmacy, Jamia Hamdard, New Delhi, 110 062, bldia Received 26 February 1996; accepted 29 March 1996 Abstract Buccoadhesive erodible tablets for local delivery of clotrimazole (CLT) to the oral cavity were developed using different bio-adhesive polymers along with soluble excipients like mannitol and polyethylene glycol-6000. An apparatus simulating the in vivo conditions of the mouth was designed in order to assess in vitro, the bio-adhesive performance and release characteristics of these tablets. The in vitro adhesion time and release characteristics were found to be a function of the type of polymer and also the total composition of the tablets. In vivo evaluation of placebo tablets in healthy human volunteers indicated a linear and positive correlation between the in vitro and in vivo adhesion time. A2"ywordr: Bio-adhesion; Buccal tablet; Candidiasis; Clotrimazole 1. Introduction Oral candidiasis is an opportunistic infection of the mouth, highly prevalent in a specific group of patients including AIDS patients (Greenspan, 1994). Clotrimazole (CLT) is amongst the first line agents used for the prophylaxis and treatment of this condition (Martin, 1990). As the conven- * Corresponding author. Present Address: Shripati Singhania R and D Centre, JK Pharmaceuticals, Faridabad-121 003, India. tional formulations like mouth paints, rinses, troches, oral gels, etc., have been found to be incapable of maintaining the salivary concentra- tion of drugs for a prolonged period of time (Anders and Merkle, 1989; Collins and Deasy, 1990), it was decided to develop a muco-adhesive buccal tablet which could be stuck on to the inner surface of the cheek and which would maintain the salivary concentration of the drug above the 'minimum inhibitory concentration' (MIC) against Candida albicans (2 mcg/ml) (Holt and Newman, 1972; Sawyer et al., 1975) for a pro- longed period of time. 0378-5173/96/$15.00 © 1996 Elsevier Science B.V. All rights reserved PH S0378-5173(96)04531-0