NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2021, Vol. 33 ›› Issue (4): 620-629.doi: 10.16333/j.1001-6880.2021.4.012

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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*   

  1. 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

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

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