硫辛酸缓释固体分散体的制备及其体外释放度的考察  

Preparation of sustained release solid dispersion of α-lipoic acid and its dissolution rate in vitro

作　　者：汤伟[1] 庞建国[1] 朱兴一[1,2] 

机构地区：[1]浙江工业大学药学院,杭州310014 [2]长三角绿色制药协同中心,杭州310014

出　　处：《中国新药杂志》2017年第14期1706-1711,共6页Chinese Journal of New Drugs

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。Objective： To prepare sustained release solid dispersion of α-lipoic acid with the intention of extending the release time of α-lipoic acid and improving its bioavailability. Methods： The mechanical chemical technology and microenvironment pH control technology were used to prepare the sustained release solid dispersion. The condition of mechanical milling and the in vitro dissolution of the solid dispersion were investigated, and the changes of crystalline form in the solid dispersion were characterized by XRD. Results： The type and dosage of ethyl cellulose had a certain effect on the release of the sustained release solid dispersion, and EC-N50 was better than other types; HPMC-E3 had better effect on the regulation of the release rate than other types; when the pH regulator was Na2CO3, the solid dispersion had a better sustained release effect, the accumulative drug-release percentage at 12 h in vitro was over 95% ; the optimum mechanical milling process condition was determined to be 100 r-rain-11 h; XRD had proved the formation of solid dispersion. Conclusion： The solid dispersion using ethyl cellulose as the carrier exhibits obvious slow releasing effect in vitro.

关 键 词：硫辛酸 缓释固体分散体 机械球磨 微环境pH调控 释放度 

分 类 号：R945[医药卫生—微生物与生化药学]