盐酸氟西汀胃漂浮海藻酸钙缓释微球体内外研究

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.

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

ObjectiveTo prepare fluoxetine hydrochloride incorporated sodium alginate microspheres and explore their retention time and bioavailability in vivo.MethodsThe 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.ResultsThe microspheres released slowly.It could be described by Higuchi model.The retention time of microspheres was more than 8 h.The results showed that floating microspheres released slowly and had longer drug concentration duration; it improved bioavailability.ConclusionThe microspheres can remain floating longer.Results of pharmacokinetics indicates that microspheres have a good sustained release efficacy, with higher bioavailability.