喷雾干燥法制备阿司匹林固体分散体及其胶囊制备与体外特性研究

Preparation of Aspirin Solid Dispersions by Spray Drying and Characterization of Its Capsules in Vitro

目的制备阿司匹林固体分散体及其胶囊,提高其溶出度。方法以聚乙烯吡咯烷酮(PVP K 30)为载体,采用喷雾干燥法制备阿司匹林固体分散体,测定溶出度,采用X-射线衍射和扫描电镜(SEM)考察药物在载体中的分散状态,测定比表面积;制备阿司匹林固体分散体胶囊,考察胶囊的体外溶出度。结果与阿司匹林原料药、阿司匹林物理混合物相比,阿司匹林固体分散体中药物的溶出度均有显著提高,且载体比例越大,药物溶出越快,但药物和载体比例达1∶6以上时,溶出度增加不再明显。阿司匹林以无定型或分子形式高度分散在载体中,药辅比在l∶6时,阿司匹林固体分散体比阿司匹林原料药的比表面积增大3.2倍;制成固体分散体胶囊后,30 min时药物累积溶出度达99.8%。结论该固体分散体制备工艺可行,制备的胶囊质量可控。

OBJECTIVE To prepare aspirin solid dispersion（SD） and capsules, and to improve its dissolution. METHODS Using polyvi-nylpyrrolidone（PVP K 30） as carrier, aspirin SD was prepared by spray-drying method. The dissolution in vitro was determined. X-ray diffractometer and Scanning electron microscope were used to investigate the dispersion status of aspirin in the carriers, and specific surface area was determined. Aspirin solid dispersion capsules were prepared, the dissolution in vitro of aspirin SD and capsules were investigated. RESULTS The solubility of aspirin in aspirin SD was significantly increased compared with raw material and aspirin-carrier physical mixture. The higher the proportion of carrier, the rapider drug was dissolved. When the ratio of drug to carrier was above 1 ： 6, the increase of dissolution was no longer significant. Aspirin were highly dispersed in the carrier in amorphous or molecular form. Compared with raw material, the specific surface area of aspirin SD with drug-carrier ratio of 1 ： 6 increased by 3.2 folds; the cumulative release of aspirin in aspirin SD capsule achieved about 99.8% within 30 rain. CONCLUSION The preparation technology of SD is feasible, and the quality of capsules is controllable.