目的 将难溶于水的脂溶性青蒿素（artemisinin，Art）通过多孔淀粉（porous starch，PS）负载后形成青蒿素多孔淀粉微球（Art-PSM），使其理化性质优于Art原药，从而改善Art的水溶性。方法 采用物理吸附方法使PS微粒对Art原药进行负载，通过单因素法优化制备Art-PSM的最佳条件。通过扫描电镜检测（SEM）、比表面积的测定（BET）、红外光谱检测（FTIR）、X射线衍射检测（XRD）、差示扫描量热（DSC）和热重分析（TG）检测分别对Art-PSM的理化性质进行表征与分析。分别检测Art-PSM在水、人工胃液和人工肠液中的溶解度。结果 通过对理化性质的表征验证了在最佳制备条件下，PS已成功负载Art形成微球，其载药量为（20.37±0.61）%，包封率为（81.86±3.06）%。PS负载Art的过程中只发生了物理变化，Art原药已完全被PS所吸附，体现出和PS一样具有无定形态结构，从而提高了Art原药的水溶性。Art-PSM的溶解度显著提高，在水、人工胃液、人工肠液中分别是Art原药的3.77、1.64和1.72倍。结论 Art-PSM显著提高了Art原药的水溶性，为解决难溶性药物的临床应用提供了重要的研究依据。

Objective The fat-soluble artemisinin (Art), which is poorly soluble in water, was loaded with porous starch to form Art microspheres, and its physical and chemical properties were better than the original powder, so as to improve the water solubility of Art. Methods The porous starch particles were loaded on Art powder by physical adsorption method. The physical and chemical properties of Art microspheres loaded with porous starch were characterized and analyzed by SEM, BET, FTIR, XRD, DSC, and TG respectively. The saturated solubilities of porous starch loaded Art microspheres in water, artificial gastric juice and artificial intestinal fluid were determined. Results In the characterization test, we found that under the optimal preparation conditions, porous starch had successfully loaded Art to form microspheres with drug loading of (20.37 ±0.61)% and entrapment efficiency of (81.86 ±3.06)%. In the process of loading Art with porous starch, only physical changes happened. The original Art powder had been completely loaded by porous starch, showing that it had the same amorphous structure as porous starch, thus improving the water solubility of the original Art powder. The saturated solubility of the porous starch loaded Art microspheres was significantly improved, and the water, artificial gastric juice and artificial intestinal fluid were 3.77, 1.64, and 1.72 times higher than the original Art powder, respectively. Conclusion This paper significantly improved the water solubility of Art powder and provided important research basis for solving the clinical application of insoluble drugs.

R283.6

黑龙江省林业科技项目（逊克）（HLJXK01）；中央高校基本科研业务费专项资金资助（2572016AA37）