盐酸布替萘芬阴道用温敏水凝胶的制备及体外释放度的考察

目的:制备盐酸布替萘芬阴道用温敏水凝胶并考察其体外释放度。方法:以泊洛沙姆为基质,筛选最佳处方以达到合适胶凝温度,并利用高效液相色谱法(HPLC)建立含量测定方法考察体外释放度。结果:结果显示以1%盐酸布替萘芬、0.1%山梨酸钾、2%甘油、5%聚山梨酯80、12%泊洛沙姆407及5%泊洛沙姆188为配方制备的温敏水凝胶在35℃时产生胶凝,体外释放度考察结果显示8 h可释放超过90%的药物。结论:本研究制备的盐酸布替萘芬阴道用温敏水凝胶具有很好的温度敏感性及黏附性,具有缓释特性且给药方便,是一种值得开发的药物制剂。

Investigation on preparation and release property in vitro of butenafine hydrochloride thermosensitive hydrogel for vagina administration

OBJECTIVE To prepare butenafine hydrochloride thermosensitive hydrogel and investigate its release property in vitro. METHODS Suitable gelling temperature was researched by screening the composition of poloxamer and quantitative analysis method was established by HPLC to investigate release property in vitro. RESULTS Hydrogel was prepared with 1% butenafine hydrochloride, 0.1% potassium sorbate, 2% glycerol, 5% Tween 80, 12% poloxamer 407 and 5% poloxamer 188, which reached suitable gelling temperature and release over 90% of drug in 8 hours in vitro. CONCLUSION Butenafine hydrochloride thermosensitive hydrogel for vagina administration has excellent temperature sensitivity and adhesion which can reach the objective of delayed release and convenient administration. It will be a valuable preparation to develop.