阿司匹林固体分散体及其胶囊的制备与体外溶出度研究

目的:制备阿司匹林固体分散体及其胶囊,并研究其体外溶出度。方法:以聚乙烯吡咯烷酮为载体,采用喷雾干燥法制备阿司匹林固体分散体,比较阿司匹林原料药、阿司匹林与载体不同比例的物理混合物和固体分散体的溶出度;采用X-射线衍射和扫描电镜考察药物在载体中的分散状态,测定比表面积;考察阿司匹林固体分散体胶囊的体外溶出度。结果:与阿司匹林原料药、阿司匹林物理混合物比较,阿司匹林固体分散体中药物的溶出度均有提高,且载体比例越大,药物溶出越快,但药物-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;药物-载体在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。

Preparation and Dissolution in vitro of Aspirin Solid Dispersion and Capsules

OBJECTIVE： To prepare Aspirin solid dispersion （SD） and capsules, and to study its dissolution in vitro. METHODS： Using polyvi-nylpyrrolidone （PVP K30） as carrier, Aspirin SD was prepared by spray-drying method. The dissolution rates of aspirin, Aspirin-carrier physical mixture and Aspirin-carrier solid dispersion were determined. X-ray diffractometer and SEM were used to investigate the dispersion status of aspirin in the carriers, and specific surface area was determined. The in vitro dissolution of Aspirin SD and capsules were investigated. RESULTS ： The solubility of aspirin in Aspirin SD was increased to some ex- tent, compared with raw material and Aspirin-carrier physical mixture. The higher the proportion of carrier was, the rapider drug dissolved; when the ratio of drug and 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 to 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 min. CONCLUSIONS ： The preparation technology of SD is feasible, and the quality of capsules is controllable.