乳酸环丙沙星温度敏感型原位凝胶的制备及其体外释药评价  

Preparation of the ciprofloxacin lactate thermosensitive in situ gel and its drug releasing performance in vitro

作　　者：曹礼华[1,2] 张东娟[1] 陈辉[1] 莫菲[1] 罗家莹[1] 郭凡溪[1] 江善祥[1] 

机构地区：[1]南京农业大学动物医学院,江苏南京210095 [2]广东广垦畜牧有限公司,广东广州510612

出　　处：《南京农业大学学报》2013年第2期125-131,共7页Journal of Nanjing Agricultural University

摘　　要：以泊洛沙姆407(P407)和泊洛沙姆188(P188)为温敏材料,采用冷溶法制备乳酸环丙沙星(CPFL)温度敏感型原位凝胶,用试管倒转法考察泊洛沙姆溶液的胶凝温度,用紫外分光光度法测定释放介质中的药物含量,经无膜溶出法考察原位凝胶体外释药特性,以胶凝温度和缓释时间为指标筛选组合物。结果显示:最佳组合为0.024 g.mL-1P407+0.02 g.mL-1P188+0.08 g.mL-1 CPFL+0.000 3 g.mL-1 EDTA-2Na+0.001 5 g.mL-1 NaHSO3+0.000 1 g.mL-1苯扎溴铵,对应的胶凝温度为32.5℃;该原位凝胶在室温下为流体,在体温下发生相转变形成凝胶;药物在11 h释放了84.23%,无突释现象,释药规律符合Higuchi动力学方程。结论:乳酸环丙沙星温度敏感型原位凝胶制备工艺简便,载药量高,具有良好的药物缓释作用。The study aimed to prepare the thermosensitive in situ gel of ciprofloxacin lactate （CPFL）and evaluate its sustained in vitro release. The in situ thermosensitive gel of CPFL was prepared with poloxamer 407 （P407） and poloxamer 188 （P188） as thermosensitive materials by using cold method. Gelation temperature（GT） of various concentration poloxamer solutions were all investigated with the method of inversion of test tube. Gel erosion of the in situ gels and release of CPFL from the in situ gels were investigated by membrane free method at 37 ℃ under agitation. The content of CPFL from the thermosensitive in situ gel was determined by ultraviolet spectropho- tometry. The best compositions were selected with release time and GT. The resuhs showed that the best compositions were 0. 024 0.024g·mL^-1P407＋0.02g·mL^-1P188＋0.08g·mL^-1CPFL＋0.0003g·mL^-1EDTA.2Na＋0.0015g·mL^-1NaHSO,＋0.0001g·mL^-1 benza- lkonium bromide. The in situ gel was fluid at room temperature, and gel phase transition occurred at body temperature. The cumulative release of drug achieved 84.23% at 11 h without burst phenomenon. It followed the Higuchi kinetic equation. The results demonstrate that the preparation method of the CPFL thermosensitive in situ gel is appropriate and the drug loading and release in vitro all can reach the expected request.

关 键 词：泊洛沙姆 乳酸环丙沙星 温度敏感型原位凝胶 胶凝温度 体外释药 

分 类 号：S859.5[农业科学—临床兽医学] S859.7[农业科学—兽医学]