复方总黄酮聚乳酸-羟基乙酸共聚物微囊的制备及体外释药特性

发布时间：2018-01-18 05:32

本文关键词：复方总黄酮聚乳酸-羟基乙酸共聚物微囊的制备及体外释药特性　出处：《吉林大学学报(医学版)》2017年03期 　论文类型：期刊论文

【摘要】：目的:以聚乳酸-羟基乙酸共聚物(PLGA)作为载体材料制备复合骨碎补总黄酮(TFRD)和野菊花总黄酮(TFC)的TF-PLGA缓释微囊,探讨微囊的最佳制备工艺及其体外缓释特性。方法:以PLGA、TFRD和TFC为原料,采用复乳-溶剂挥发法制备TF-PLGA缓释微囊;以包封产率(EE)为评价指标,通过单因素实验及正交实验进行工艺优化,筛选最佳的工艺参数;光学显微镜(LM)和扫描电子显微镜(SEM)下观察微囊的形态特征、粒径大小和分布情况;采用提取法测定TF-PLGA微囊的体外累计释药率并绘制累计释放曲线。结果:单因素实验和正交实验优化的最佳制备工艺,PLGA浓度为140g·L~(-1),油相体积为1.4mL,乳化速度为1 500r·min~(-1),乳化时间为5min。优化后微囊平均EE为(83.89±2.30)%,平均实际载药量(DL)为(5.90±0.07)%;LM和SEM下观察,微囊形态圆整,平均粒径为(44.34±14.68)μm,粒径分布较窄;体外释放实验检测,24h累计释药率达40%,第50天后累积释药率超过90%。结论:TF-PLGA缓释微囊具有优良的载药及缓释效果,制备工艺简单,重复性良好。
[Abstract]:Objective: to prepare TF-PLGA sustained-release microcapsules of compound total flavonoids of Fructus fragmentae and total flavonoids of Chrysanthemum chrysanthemi by using poly (lactic acid-glycolic acid) copolymers as carrier materials. To investigate the optimum preparation process and in vitro slow-release properties of microcapsules methods: the TF-PLGA sustained-release microcapsules were prepared by the method of compound emulsion and solvent volatilization using PLGAGA-TFRD and TFC as raw materials. The encapsulation yield was used as the evaluation index, and the optimum process parameters were selected by single factor experiment and orthogonal experiment. The morphology, size and distribution of microcapsules were observed under optical microscope (LM) and scanning electron microscopy (SEM). The cumulative release rate of TF-PLGA microcapsules in vitro was determined by extraction method and the cumulative release curve was drawn. Results: the optimal preparation conditions were optimized by single factor experiment and orthogonal experiment. The concentration of PLGA is 140 g 路L ~ (-1), the volume of oil phase is 1.4 mL, and the emulsifying rate is 1 500 r 路min ~ (-1). The emulsification time was 5 min. The average EE of the microcapsules was 83.89 卤2.30 and the average DL was 5.90 卤0.07 after the optimization. Under LM and SEM, the microcapsules were round in shape, the average particle size was 44.34 卤14.68 渭 m, and the particle size distribution was narrow. The cumulative drug release rate of TF-PLGA in vitro was 40% in 24 hours and more than 90% after 50 days. Conclusion: TF-PLGA microcapsules have excellent drug delivery and sustained release effect. The preparation process is simple and reproducible.
【作者单位】：吉林大学口腔医院牙周病科;吉林大学口腔医院急诊科;
【基金】：吉林省中医药管理局科研项目资助课题(2014-Q48)
【分类号】：R943
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