盐酸非索非那定磺丁基醚-β-环糊精包合物鼻用温敏凝胶的制备及黏附效果评价

Preparation and Mucoadhesion Evaluation of Fexofenadine Hydrochloride Sulfobutylether-β-Cyclodextrin Clathrate Compound Nasal Thermosensitive Hydrogels

目的:制备盐酸非索非那定磺丁基醚-β-环糊精包合物及其鼻用温敏凝胶,并评价其黏附效果。方法:采用饱和水溶液法制备盐酸非索非那定磺丁基醚-β-环糊精包合物,冷配法制备包合物的鼻用温敏凝胶,以胶凝温度筛选凝胶基质和生物黏附剂;采用靛蓝胭脂红染色法评价所制制剂与盐酸非索非那定混悬液在大鼠鼻腔内的滞留时间。结果:所制包合物易溶于水,包合率为(86.0±2.7)%(n=3);凝胶基质为16%的泊洛沙姆407,生物黏附剂为0.5%的透明质酸钠;所制包合物鼻用温敏凝胶在大鼠鼻腔内的滞留时间约为混悬液的2.8倍。结论:成功制得盐酸非索非那定磺丁基醚-β-环糊精包合物鼻用温敏凝胶,且其鼻腔内黏附效果较好。

OBJECTIVE： To prepare fexofenadine hydrochloride sulfobutylether-β-cyclodextrin clathrate compound and its nasal thermosensitive hydrogels, and to evaluate its mucoadhesion. METHODS： Fexofenadine hydrochloride sulfobutylether-β-cyclodextrin clathrate compound was prepared by saturated aqueous system, and nasal thermosensitive hydrogels were prepared by cold method. Gel matrix and biological adhesive were screened by gelatinization temperature. Indigo carmine staining method was used to evaluate the retention time of prepared preparation and fexofenadine hydrochloride suspension in nasal cavity of rats. RESULTS ： The clathrate was freely soluble in water. Inclusion rate of the clathrate was （86.0 ± 2.7）% （n=3）. Gel matrix was 16% poloxamer 407, biological adhesive was 0.5% sodium hyaluronate, the retention time of prepared nasal thermosensitive hydrogels was 2.8 time as that of fexofenadine hydrochloride suspension. CONCLUSIONS ： Fexofenadine hydrochloride sulfobutylether-β-cyclodextrin clathrate compound nasal thermosensitive hydrogels are prepared successfully and show good mucoadhesion.