Preparation and Evaluation of Ursolic Acid Solid Dispersions

Abstract

Abstract: Objective To establish preparation methods of ursolic acid solid dispersions and evaluate the quality in vitro. Methods Ursolic acid solid dispersions (UA-SD) were obtained with different carriers by solvent method. Based on crystal suppression experiment, the carrier materials were screened out. The dissolution rate of UA-SD with different drug loading ratio was compared by dissolution test, and the optimal UA-SD drug loading ratio was screened then the solid dispersion was identified by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (X-RD) and fourier transform infrared spectroscopy (FT-IR). Results Soluplus was selected as the carrier of the preparation UA-SD by crystal suppression experiments. The dissolution in vitro showed that the cumulative dissolution rate of UA-SD at 120 minute was 102.7% with a mass ratio of drug to carrier of 1:11. Solid dispersion displayed a much higher dissolution rate than raw medicine and physical mixture. The SEM, DSC, XRD and FT-IR characterizations showed that UA exist in solid dispersions in amorphous form. Conclusion Preparation of UA-SD with Soluplus as carrier can significantly increase the dissolution rate of ursolic acid.

Key words: ursolic acid, solid dispersions, dissolution rate, phase identification

摘要： 目的制备熊果酸固体分散体,并进行质量评价。方法通过抑晶实验,筛选适宜的载体材料,采用溶剂法制备熊果酸固体分散体（UA-SD）,通过溶出实验比较不同载药比UA-SD的溶出度,筛选最优UA-SD载药比,并运用SEM、DSC、XRD、FT-IR对UA-SD进行物相表征。结果通过抑晶实验,筛选出Soluplus作为载体;选择载药比为1：11,UA-SD在120min时累积溶出度为102.7%,比UA原料药、物理混合物的溶出度明显增加;SEM、DSC、XRD、FT-IR表征显示UA以无定形的形式存在于固体分散体中。结论以Soluplus为载体制备UA-SD,可明显提高UA的体外溶出度。

关键词: 熊果酸, 固体分散体, 溶出度, 表征

CLC Number:

R283

ZHANG Ling, DUAN Li-ying, WU Qian. Preparation and Evaluation of Ursolic Acid Solid Dispersions[J]. Journal of Chengde Medical University, 2022, 39(4): 283-288.

张领, 段丽颖, 武倩. 熊果酸固体分散体的制备与质量评价[J]. 承德医学院学报, 2022, 39(4): 283-288.

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