蒿甲醚纳米结构脂质载体的制备及体外释放

发布时间：2018-01-17 15:21

本文关键词：蒿甲醚纳米结构脂质载体的制备及体外释放　出处：《中国医药工业杂志》2017年05期 　论文类型：期刊论文

【摘要】：采用伪三元相图法筛选蒿甲醚纳米结构脂质载体的处方组成,分别采用微乳法和高压乳匀法进行制备,通过单因素试验和正交设计进行工艺及处方优化。结果显示,优化条件下,微乳法所得纳米粒粒径为(30.0±2.3)nm,ζ电位为(-40.9±1.1)m V,包封率为(92.8±2.4)%;高压乳匀法所得纳米粒粒径为(61.5±1.9)nm,ζ电位为(-28.4±0.5)m V,包封率为(83.8±0.2)%。二者体外释放规律均符合一级动力学方程,48 h累积释放率为80.6%和83.9%。两种方法制备的纳米粒粒径均达到预期值(小于80 nm)并显示缓释特性。由于高压乳匀法工艺参数更易控制,适合放大批量生产,将在后续研究中用于蒿甲醚纳米结构脂质载体的制备。
[Abstract]:Composition screening of artemether nanostructured lipid carrier prescription using pseudo three element phase diagram method, respectively using microemulsion method and high pressure homogenization method of preparation, process and formulation optimization by single factor test and orthogonal design. The results showed that under the optimum conditions, the microemulsion nanoparticles diameter was (30 + 2.3) nm. The zeta potential was m V (-40.9 + 1.1), encapsulation efficiency (92.8 + 2.4)%; the high pressure homogenization method for the particle size (61.5 + 1.9) nm, the zeta potential was m V (-28.4 + 0.5), encapsulation efficiency (83.8 + 0.2)%. The two release in vitro accord with the kinetic equation, the cumulative release rate was 48 h two and 83.9%. 80.6% method of making nano particle size reached the expected value (less than 80 nm) and showed sustained release characteristics. Because of the high pressure homogenization method of process parameters can be easily controlled, suitable for amplification of mass production, will be used to artemether nanostructured lipid carriers the preparation in the follow-up study.

【作者单位】：山西医科大学药学院;
【基金】：国家自然科学基金(81373364) 山西省回国留学人员科研资助项目(2009-47)
【分类号】：R943
【正文快照】： 蒿甲醚(artemether,1)是目前治疗疟疾的一线药物,其临床应用有油溶液注射剂、片剂、胶丸等制剂[1]。前期研究表明,1口服吸收快,但存在自身诱导代谢作用,且主要诱导首过代谢[2]。油溶液注射剂通过肌肉注射给药,虽无自身诱导作用,但起效较慢。研制静脉给药制剂则可避开首过代谢

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