Aoyagi N, Kaniwa N, Ogata H
National Institute of Hygienic Sciences, Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1990 May;38(5):1338-40. doi: 10.1248/cpb.38.1338.
Two different indomethacin capsules, a commercial one containing fine drug particles and an experimental capsule containing 125-177 microns particles, were employed in this study. The commercial preparation showed faster in vitro dissolution than the experimental one. When administered to humans having normal acidity of the gastric juices, the commercial capsule exhibited higher Cmax and smaller Tmax and mean residence time (MRT) than the experimental one both in fasting and nonfasting states, although the two capsules were equivalent in area under the serum concentration-time curve (AUC). The ingestion of a breakfast delayed the gastrointestinal absorption from both preparations, which resulted in larger Tmax's and MRT's and smaller Cmax's in the nonfasting state. Food, however, did not have any significant effect on the AUC's of the preparations.
本研究使用了两种不同的吲哚美辛胶囊,一种是市售胶囊,其药物颗粒细小,另一种是实验性胶囊,其颗粒大小为125 - 177微米。市售制剂在体外的溶出速度比实验性制剂快。当给胃液酸度正常的人服用时,无论是在禁食还是非禁食状态下,市售胶囊的Cmax均高于实验性胶囊,Tmax和平均驻留时间(MRT)均小于实验性胶囊,尽管两种胶囊的血清浓度 - 时间曲线下面积(AUC)相当。早餐的摄入延迟了两种制剂的胃肠道吸收,导致非禁食状态下Tmax和MRT增大,Cmax减小。然而,食物对制剂的AUC没有任何显著影响。