질염 치료제인 클로트리마졸 고체분산체 개발 및 평가

Development and Evaluation of Solid Dispersion of Clotrimazole as a Treatment for Vaginitis

Clotrimazole is used as a treatment for vaginitis and has been developed as an external drug to be administered directly into the vagina. Canesten®Vaginal Tablet is administered directly into the vagina through a device, and has a big tablet weight of approximately 1500 mg. The purpose of this study was to develop a clotrimazole (CTMZ) solid dispersion (SD) with improved solubility and dissolution rate and to ensure stability. The manufacturing method of CTMZ-SD formulations used the solvent evaporation method, and it is a quaternary system composed of CTMZ-organic acid-carrier-polymer. The dissolution results of the final formulation, YE-SD1 (CTMZ:succinic acid:MCM-41:TPGS=1:1:1:1, w/w), were improved by 80.4% (pH 4.5 buffer) and 45.0% (pH 6.8 buffer) compared to those of Canesten®Vaginal Tablet (17.2% in pH4.5 buffer and 0% in pH6.8 buffer). Moreover, all physicochemical properties (melting point, interaction and crystallinity) were changed, and stability for three months was secured. Successful results were obtained for solubilization of CTMZ through organic acids and polymers, and good results are expected in the planned animal experiment.