盐酸氟西汀胃漂浮海藻酸钙缓释微球体内外研究  

A Study on Fluoxetine Hydrochloride Floating Calcium Alginate Microspheres in Vitro And in Vivo

作　　者：沈龙华[1] 邓艳平[1] 汪效英[1] 吴宏霞[1] 余祥彬[1] 

机构地区：[1]福建医科大学药学院,福州350108

出　　处：《福建医科大学学报》2016年第2期82-87,102,共7页Journal of Fujian Medical University

基　　金：福建省科技厅高校产学合作科技重大项目(2015Y4005)

摘　　要：目的制备盐酸氟西汀海藻酸钙胃漂浮微球,考察胃漂浮制剂的体内滞留及生物利用度。方法采用离子凝胶-烘干法制备海藻酸钙胃漂浮微球,以百忧解为参比制剂,测定微球体外释放情况,并采用残余药量法考察微球胃肠转运行为,建立柱前衍生-HPLC荧光检测法测定胃漂浮微球大鼠体内血药浓度,计算药代动力学参数和生物利用度。结果胃漂浮微球体外释放较慢,释放曲线符合Higuchi方程,在胃中的滞留时间>8h,血药浓度更平稳,生物利用度明显提高。结论所制胃漂浮微球具有缓释的效果,可以延长胃中滞留时间,提高药物的生物利用度。Objective To prepare fluoxetine hydrochloride incorporated sodium alginate microspheres and explore their retention time and bioavailability in vivo. Methods The ion gel method was used to prepare microspheres. Ultraviolet spectrophotometry（UV）test was introduced for releasing rate in vitro. The residual quantity method was used to study gastrointestinal tract transfer behavior. The drug concentration in blood was assayed by HPLC with pre-column derivatization and fluorescence detection. The pharmacokinetic parameters and bioavailability were calculated. Results The microspheres released slowly. It could be described by Higuchi model. The retention time of microspheres was more than 8h. The results showed that floating microspheres released slowly and had longer drug concentration duration;it improved bioavailability. Conclusion The microspheres can remain floating longer.Results of pharmacokinetics indicates that microspheres have a good sustained release efficacy,with higher bioavailability.

关 键 词：胃 药用制剂 微球体 剂量效应关系 药物 生物利用度 

分 类 号：R943[医药卫生—药剂学]