硫辛酸缓释固体分散体的制备及其体外释放度的考察

发布时间：2018-06-01 19:33

本文选题：硫辛酸 + 缓释固体分散体　；参考：《中国新药杂志》2017年14期

【摘要】：目的:制备硫辛酸缓释固体分散体,延长药物的释放时间,提高其生物利用度。方法:利用机械化学技术,结合微环境pH调控技术,制备出硫辛酸缓释固体分散体;并对制备条件及其体外释放度的影响进行分析,采用X射线衍射(XRD)技术对缓释固体分散体进行表征。结果:不同型号的乙基纤维素及其用量对缓释固体分散体的释放度有一定的影响,综合考虑,乙基纤维素-N50(EC-N50)的效果较好;羟丙基甲基纤维素E3(HPMC-E3)对释放度的调节效果最好;加入不同的碱化剂做作为pH调节剂对释放度的影响也不尽相同,其中Na_2CO_3能使得释放度在12 h内释放95%以上,药物基本呈一级释放。对机械球磨工艺进行优化,确定最佳的球磨工艺为球磨转速100 r·min~(-1),球磨时间1 h。XRD技术证明固体分散体的形成。结论:以乙基纤维素为载体,采用固体分散技术结合微环境p H调控技术制备的硫辛酸缓释固体分散体的缓释效果明显。
[Abstract]:Aim: to prepare the sustained-release solid dispersion of lipoic acid, prolong the release time and improve its bioavailability. Methods: the sustained release solid dispersion of lipoic acid was prepared by using mechanochemical technology and microenvironment pH control technique, and the effects of preparation conditions and in vitro release rate were analyzed. The sustained release solid dispersion was characterized by X ray diffraction (XRD). Results: different types of ethyl cellulose and its dosage had certain influence on the release rate of sustained release solid dispersion. Considering synthetically, the effect of ethyl cellulose-N50 EC-N50) was better than that of hydroxypropyl methyl cellulose E3HPMC-E3), and the effect of E3HPMC-E3) was the best. The effect of adding different alkali agent as pH regulator on the release was different. Na_2CO_3 could release more than 95% of the release within 12 h, and the drug was basically first-order release. The mechanical ball milling process was optimized. The optimum ball milling technology was determined to be the ball milling speed of 100r / min ~ (-1) and the milling time of 1 h.XRD to prove the formation of the solid dispersion. Conclusion: using ethyl cellulose as carrier and solid dispersion technology combined with microenvironment pH regulation technology, the sustained release effect of lipoic acid slow-release solid dispersion is obvious.
【作者单位】：浙江工业大学药学院;长三角绿色制药协同中心;
【分类号】：R943

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