氟康唑胶囊体外溶出度的质量评价

Evaluation of Dissolution in Vitro of Fluconazole Capsules

目的比较氟康唑胶囊2个仿制厂家与原研制剂在3种溶出介质的溶出曲线,为评价氟康唑胶囊药品质量提供依据。方法采用《中国药典》2010年版二部附录X C第一法的装置,测定了3个厂家氟康唑胶囊在0.1 mol/L盐酸溶液、水和磷酸盐缓冲液(pH6.8)中的溶出曲线,并用f2因子法进行比较分析。结果在0.1 mol/L盐酸溶液和磷酸盐缓冲液(pH6.8)中,C厂家制剂与原研制剂的溶出曲线一致,B厂家制剂与原研制剂的溶出曲线有明显差异,但在水中仿制制剂与原研制剂的溶出曲线有明显差异,批内均一性的考察结果是C厂家优于B厂家制剂,B和C仿制厂家的批间重复性均良好。结论作为氟康唑胶囊的溶出介质,水比0.1 mol/L盐酸溶液和磷酸盐缓冲液(pH6.8)对制剂质量具有更好的分辨能力,建议修订该溶出度检验方法的溶出介质,与原研药溶出曲线不一致的厂家,建议研究晶型或改进处方工艺。

Objective To compare the dissolution profiles of fluconazole capsules from copy and original manufacturers in 3 dissolution medium, so as to provide basis for comprehensive evaluation of the quality of fluconazole capsules. Methods The dissolution profiles of fluconazole capsules from 3 manufacturers in 0.1 mol/L hydrochloric acid solution, water and phosphoric acid buffer （pH6.8） were determined by the method 1 in appendix X C of Chinese Pharmacopeia 2010, and comparatively analyzed by the f2 similarity factor. Results In 0. 1 mol/L hydrochloric acid solution and phosphoric acid buffer （ pHr. 8）, the dissolution profiles of C manufacturer were similar to that of original manufacturer, but B was different from original manufacturer. In water, the dissolution profiles of fluconazole capsules from 2 copy manufacturers were significant different from that of the original manufacturer. Conclusion As the dissolution medium, water are more suitable for fluconazole capsules than 0. 1 mol/L hydrochloric acid solution and phosphoric acid buffer （ pHr. 8 ）. It is advisable for manufacturers that the dissolution profiles are different from that the original drug to improve their formulation and process of preparation.