聚乳酸-羟基乙酸共聚物吗啡微球的制备及体外释放模型的建立
Preparation of polyactic-coglycolic acid morphine microspheres and establishment of its in vitro releasing model
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摘要: 目的: 研究以聚乳酸-羟基乙酸共聚物(PLGA)为载体的吗啡生物可降解缓释微球制剂的制备,并测定其体外释放曲线,建立体外释放模型。方法: 采用溶剂挥发法制备吗啡PLGA微球,高效液相色谱法(HPLC)检测微球中吗啡的含量。采用透析释药法测定微球体外释放曲线,并用零级动力学方程、一级动力学方程、Higuchi模型方程进行线性拟合。结果: 吗啡PLGA微球的载药量为11.86%,药物包封产率为33%,体外释放曲线显示吗啡PLGA微球释放时间明显延长至10d以上。结论: 吗啡PLGA微球明显地延长了吗啡释放时间,缓释性好,体外释放遵从零级释放模型。Abstract: Objective: To study the preparation of polyactic-coglycolic acid（PLGA）morphine microspheres and establish its in vitro releasing model. Methods: PLGA morphine microspheres were prepared using the emulsify-solvent evaporation method and observed under a super-microscope.Drug content in morphine microspheres was detected by high performance liquid chromatography（HPLC）.Dialysis method was used to examine the in vitro drug release.The release data fit three model equations. Results: The drug content in morphine microspheres accounted for 11.86%,and the ratio of drug envelopment was 33%.The releasing test in vitro showed that the releasing time of morphine microspheres could last over 10 days and fit the zero-model. Conclusion: PLGA morphine microspheres can obviously prolong the releasing time of morphine.
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