硫酸阿托品眼用温敏凝胶的制备及体外释放研究  

Preparation and in vitro Drug Release of Ocular Thermosensitive Gel of Atropine Sulfate

作　　者：周俊[1] 唐蕾[1] 赵伟国[1] 李卓亚[1] 高珊[1] Zhou Jun Tang Lei Zhao Weiguo Li Zhuoya Gao Shan(Zhongshan People＇s Hospital, Guangdong Zhongshan 528403, Chin)

机构地区：[1]中山市人民医院,广东中山528403

出　　处：《中国药师》2017年第2期365-367,共3页China Pharmacist

摘　　要：目的:制备硫酸阿托品眼用温敏凝胶并考察其体外药物释放行为。方法:以泊洛沙姆407(P407)和泊洛沙姆188(P188)的用量为考察因素,模拟泪液稀释前后的胶凝温度为考察指标,采用星点设计-效应面法优化处方并进行验证;采用无膜溶出模型考察凝胶的体外溶蚀与药物释放行为。结果:以处方中含有P407 23%、P188 5%为最佳处方,效应面法优化处方的预测值和实测值偏差均小于5%;凝胶溶蚀速率决定药物释放速率,且两者均符合零级动力学方程。结论:星点设计-效应面法可用于硫酸阿托品眼用温敏凝胶的处方优化,所建立的模型预测性良好;最优处方的制剂体外释放缓慢,符合设计要求。Objective： To prepare the ocular thermosensitive gel of atropine sulfate and study its in vitro release. Methods： The gel formula was optimized by central composite design response surface methodology. The influences of the amounts of poloxamer 407 （P407） and poloxamer 188 （P188） on gelling temperature before and after the dilution with simulated tear fluid were investigated. A membraneless dissolution model was used to determine the gel erosion and in vitro release. Results： The optimized gel formula was as follows： 23% P407 and 5% P188. The deviations between the measured values and predicted values were all lower than 5%. The in vitro release experiment showed that the gel erosion and the drug release fitted zero-order kinetics equations with promising correlation, indicating a dissolutiOn-controlled release mechanism. Conclusion： The optimization of the ocular thermosensitive gel of atropine sul- fate can be achieved by central composite design response surface methodology with good estimation. The thermosensitive gel with sus- tained drug release property meets the design requirements.

关 键 词：硫酸阿托品 眼用温敏凝胶 星点设计-效应面法 凝胶溶蚀 体外释放 

分 类 号：R994.9[医药卫生—毒理学]