胡椒酸乙酯固体分散体的制备及体外溶出度研究

Study on Preparation and in vitro Dissolution of Ethyl Pepper Solid Dispersion

目的:研究胡椒酸乙酯固体分散体的制备及体外溶出度。方法:采用溶剂熔融法。选择聚乙二醇6000(PEG-6000)为载体,考察不同药载质量比(1∶1、1∶5、1∶7、1∶10、1∶15、1∶18、1∶20)对胡椒酸乙酯固体分散体溶出度的影响;考察胡椒酸乙酯原料药在85℃时的稳定性;采用差示扫描量热法、X射线粉末衍射表征胡椒酸乙酯在固体分散体中的存在状态。结果:胡椒酸乙酯与PEG-6000药载质量比为1∶15时胡椒酸乙酯的溶出度显著提高,且在85℃制备条件下稳定;胡椒酸乙酯PEG-6000固体分散体中药物以无定形或分子形式存在。结论:胡椒酸乙酯与PEG-6000(1∶15)混合制备固体分散体可显著提高药物溶出度,且在85℃条件下稳定。本研究为胡椒酸乙酯制剂制备工艺研究提供了依据。

OBJECTIVE：To study the preparation and in vitro dissolution of ethyl pepper solid dispersion. METHODS：Solvent-melting method was adopted. Using polyethylene glycol 6000（PEG-6000）as carrier,the effects of different drug-loading ratios（1 ∶ 1,1 ∶ 5,1 ∶ 7,1 ∶ 10,1 ∶ 15,1 ∶ 18,1 ∶ 20）on the dissolution of ethyl pepper solid dispersion was invesigated. The stability of crude drug ethyl pepper at 85 ℃ was determined. Furthermore,differential scanning calorimetry and X-ray powder diffraction method were used to identify the existence of ethyl pepper in the solid dispersion. RESULTS：The dissolution of ethyl pepper could be improved by mixing ethyl pepper and PEG-6000 in a ratio of 1 ∶ 15,and the preparation was maintained stable at 85 ℃. The drugs part of ethyl pepper-PEG-6000 solid dispersions existed in the form of amorphous or molecular. CONCLUSIONS：The dissolution of ethyl pepper solid dispersion can be improved significantly by mixing ethyl pepper and PEG-6000（1 ∶ 15）,and the dispersion keeps stable at 85 ℃. The study can provide reference for further study of the preparation technology of ethyl pepper preparation.