壬二酸固体分散体的制备及其表征

Preparation and Characterization of Azelaic Acid Solid Dispersion

目的:制备壬二酸固体分散体,改善壬二酸的溶出度,从而提高其生物利用度。方法:分别以聚乙二醇6000(PEG)、泊洛沙姆188为载体并选取药物与其不同比例(1:3、1:6、1:9),采用熔融法、溶剂-熔融法制备壬二酸固体分散体,并对其进行体外溶出度的考察及比较;采用差示扫描量热法、X射线粉末衍射法鉴别壬二酸在固体分散体中的存在状态。结果:以PEG为载体的固体分散体的药物溶出优于以泊洛沙姆188为载体的固体分散体(90min内溶出分别为100%和80%);且当药物与PEG的比例为1:9时,药物的溶出效果最好,与原料药比较药物溶出50%所需的时间大大缩短(12.65、45.65min)。壬二酸-PEG固体分散体中药物部分呈分子状态分散,部分呈微晶状态分散。结论:壬二酸与PEG(1:9)的固体分散体能显著提高药物的溶出度。

OBJECTIVE：To prepare Azelaic acid（AZA） solid dispersion（SD） and improve the dissolution of azelaic acid to promote the bioavailability of it.METHODS：AZA-SD was prepared using PEG6000（PEG）,poloxamer188（PL188） as carriers by melting or solvent-melting methods with ratio of carriers to drug 1：3,1：6,1：9.The dissolution in vitro was studied,and differential scanning calorimetry（DSC）,X-ray powder diffraction were used to determine the status of azelaic acid in solid dispersion.RESULTS：The dissolution of AZA-SD with PEG as carrier was higher than AZA-SD with PL188 as carrier,and their dissolutions were 100% and 80% within 90 min.The dissolution of AZA-PEG（1：9）-SD was the highest.50% raw material drug dissolved required 45.65 min and that of AZA-PEG-SD required 12.65 min.Drug in AZA-PEG-SD partly existed as molecule and partly as fine crystal.CONCLUSION：AZA-PEG（1：9）-SD can improve the dissolution of azelaic acid.