格列美脲微粉的制备及其对溶出度的影响

Preparation of Ultrafine Glimepiride Powders and Dissolution Improvement of Glimepiride Tablets

为了制备格列美脲微粉,提高格列美脲片的体外溶出度,采用气流粉碎机制备格列美脲微粉,利用高效液相色谱法测定格列美脲微粉片的体外溶出曲线,并以原研格列美脲片亚莫利为参比制剂,用美国食品和药物管理局（FDA）推荐的相似因子f2法进行溶出曲线的相似性比较.结果表明,微粉的中位粒径d50为1.30 μm,粒径范围为0.40～5.85 μm,3批片剂溶出曲线的相似因子分别为54.0、57.7、53.6;微粉化可以提高格列美脲片的体外溶出度,其溶出行为与原研参比制剂的相似.

To prepare ultrafine glimepiride powders and improve the dissolution in vitro of glimepiride tablets, ultrafine glimepiride powders were made by jet mill. The dissolution curve of glimepiride tablets was determined by the method of high performance liquid chromatography. The similarity was evaluated with the reference preparation glimepiride tablets using the similarity factor f2 method referred by the U. S. Food and Drug Administration. The results show that the median diameter d50 of ultrafine powders is 1.30 μm. The distribution of particle size is between 0.40 and 5.85 μm. The similarity factors of dissolution curves of three batches of tablets are respectively 54.0, 57.7 and 53.6. The dissolution in vitro of glimepiride tablets is improved by micronization. The dissolution action is similar with that of the reference preparation.