罗替戈汀原位形成植入剂的制备及体内药动学考察

发布时间：2018-04-28 23:10

本文选题：罗替戈汀 + 聚乳酸-羟基乙酸共聚物(PLGA)　；参考：《中国医院药学杂志》2015年07期

【摘要】：目的:制备抗帕金森病药物罗替戈汀原位形成植入剂(R-ISFI),并对其体内长效释药行为进行考察。方法:以N-甲基-二吡咯烷酮(NMP)为溶剂、聚乳酸-羟基乙酸共聚物(PLGA)为载体材料,制备R-ISFI。采用摇床法进行体外释放度的考察,采用大鼠体内药动学实验考察罗替戈汀的体内释药特性。大鼠皮下注射R-ISFI,HPLC法测定不同时间血浆中药物浓度。结果:高分子材料的类型、高分子材料与溶剂比、药物与高分子材料的用量比及ISFI的形状均对药物体外释放有显著的影响。R-ISFI体外释药平缓,30 d可累积释放85%,体内药动学结果表明,R-ISFI在体内缓释效果良好,突释小,可持续释放30 d。结论:制备的R-ISFI可持续平稳释放达一个月,是一种很有开发应用前景的长效缓释制剂。
[Abstract]:Aim: to prepare rotigotin, an in situ implantable drug for Parkinson's disease, and to investigate its long-term drug release behavior. Methods: R-ISFI was prepared with N-methyl-dipyrrolidone (NMP) as solvent and polylactic acid-glycolic acid copolymer (PLGA) as carrier material. The in vitro release of rotigotin was investigated by shaking-bed method, and the in vivo pharmacokinetics of rotigotin was investigated by pharmacokinetics in rats. Drug concentration in plasma was determined by subcutaneous injection of R-ISFI in rats at different time. Results: the type of polymer material, the ratio of polymer material to solvent, The ratio of drug to polymer material and the shape of ISFI had a significant effect on the drug release in vitro. The results of pharmacokinetics in vivo showed that the drug release rate was good, the sudden release was small, and the drug release was sustained for 30 days. Conclusion: the prepared R-ISFI can be released steadily for one month, and it is a kind of long-term sustained release preparation with good prospect of development and application.
【作者单位】：烟台大学药学院;山东绿叶制药有限公司长效和靶向制剂国家重点实验室;
【基金】：国家科技重大专项项目天然药物与新制剂综合大平台(编号:2013ZX09402201) 山东省自然科学基金项目(编号:ZR2013HQ009)
【分类号】：R965

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