双载体制备青蒿素速释型固体分散体工艺优化研究

doi:10.16333/j.1001-6880.2021.4.012

天然产物研究与开发 ›› 2021, Vol. 33 ›› Issue (4): 620-629.doi: 10.16333/j.1001-6880.2021.4.012

双载体制备青蒿素速释型固体分散体工艺优化研究

薛昊1,2#，苏婧钰2#，陈文君2，申雨玫2，王可轩1，李鑫1，陈靖2,3*，杨波1*

1哈尔滨商业大学药学院，哈尔滨 150076；2扬州大学医学院（转化医学研究院）；3江苏省中西医结合老年病防治重点实验室，扬州 225001

出版日期:2021-04-28 发布日期:2021-05-10
基金资助:
扬州大学大学生科创基金（X20190733）

Optimized technical conditions of immediate released artemisinin solid dispersion prepared by using dual carriers

XUE Hao1,2#,SU Jing-Yu2,CHEN Wen-jun2,SHEN Yu-mei2,WANG Ke-xuan1,LI Xin1,CHEN Jing2,3*,YANG Bo1*

1College of Pharmacy,Harbin University of Commerce,Harbin 150076,China;2Institute of Translational Medicine,Medical College,Yangzhou University;3Jiangsu Key Laboratory of Integrated Traditional Chinese and Western Medicine for Prevention and Treatment of Senile Disease,Yangzhou University,Yangzhou 225001,China

Online:2021-04-28 Published:2021-05-10

摘要/Abstract

摘要： 对载体类型影响青蒿素固体分散体中药物溶出度进行研究及优化制备工艺。以大豆卵磷脂与PEG 6000或聚乙烯吡咯烷酮为双分散载体，采用溶剂法制备青蒿素速释型固体分散体，以溶出度为考察指标，单因素试验筛选载体类型及最佳制备工艺；并采用红外吸收光谱法（IR）、差示扫描量热法（DSC）进行物相表征，明确载体-药物存在状态。结果表明在50 min内卵磷脂-PVP K30双载体比卵磷脂-PEG 6000药物溶出度更高，制备固体分散体为速释型，50 min内总溶出度87%以上，显著高于原料药和物理混合物，且优化最佳工艺条件为卵磷脂与PVP K30比为1∶7，搅拌时间30 min，无水乙醇用量20 mL。IR及DSC结果显示在固体分散体中药物可能以无定型状态存在。双载体制备青蒿素速释型固体分散体工艺简单可行，可显著提高药物溶出度，为提高青蒿素疗效奠定重要基础。

关键词: 速释型固体分散体, 青蒿素, 双载体, 体外溶出, 制备工艺

Abstract:

This work aimed to study the impact of carriers on artemisinin solubility in solid dispersion and to optimize the technical conditions.Soybean lecithin with polyvinylpyrrolidone (PVP K30) or PEG 6000 were used as dual dispersion carriers to prepare artemisinin solid dispersion by solvent method.Better carriers and the optimal preparation parameters were screened by single factor test,and characterized by infrared absorption spectroscopy (IR) and differential scanning calorimetry (DSC).The results indicated that a higher drug dissolution from immediate released artemisinin solid dispersion was obtained when prepared using lecithin and PVP K30 than lecithin and PEG 6000 as dual carriers.Total dissolution within 50 min for artemisinin was found to be over 87% which was significantly higher than artemisinin alone and physical mixture with raw material and carriers.The optimal conditions were as follows:the ratio between soybean lecithin and PVP K30 was 1∶7,stirring time was 30 min,and solvent volume of anhydrous alcohol was 20 mL.IR and DSC methods demonstrated that artemisinin in solid dispersion exist in an amorphous state.In this study,therefore,the optimal conditions of immediate release artemisinin solid dispersion prepared by using dual carriers is simple and feasible,which can significantly increase its dissolution and lay the basis for the improvement of artemisinin clinical efficacy.

Key words: immediate release solid dispersion, artemisinin, dual carriers, in vitro , dissolution, processing parameters

中图分类号: R944

薛昊#, 苏婧钰#, 陈文君, 申雨玫, 王可轩, 李鑫, 陈靖, 杨波. 双载体制备青蒿素速释型固体分散体工艺优化研究[J]. 天然产物研究与开发, 2021, 33(4): 620-629.

XUE Hao, #, SU Jing-Yu, CHEN Wen-jun, SHEN Yu-mei, WANG Ke-xuan, LI Xin, CHEN Jing, YANG Bo. Optimized technical conditions of immediate released artemisinin solid dispersion prepared by using dual carriers [J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2021, 33(4): 620-629.

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双载体制备青蒿素速释型固体分散体工艺优化研究

Optimized technical conditions of immediate released artemisinin solid dispersion prepared by using dual carriers

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