Wilding I R, Davis S S, Bakhshaee M, Stevens H N, Sparrow R A, Brennan J
Pharmaceutical Profiles Limited, Nottingham, UK.
Pharm Res. 1992 May;9(5):654-7. doi: 10.1023/a:1015806211556.
Captopril has been administered to eight healthy male subjects by means of a pulsatile delivery system that was designed to release the drug in the colonic region of the intestine. The gastrointestinal transit and pulsatile release were followed using gamma scintigraphy. A pulsatile capsule system with release after a nominal 5-hr period was found to perform reproducibly in vitro and in vivo. In six of the eight subjects, the drug was delivered to the colon, and in the remaining two subjects, to the terminal ileum. Measurable blood levels of free captopril were found in three subjects. Variable instability of the drug in the distal intestine is suggested as a possible reason for the lack of absorption of the drug in the majority of subjects.
已通过一种脉冲式给药系统对8名健康男性受试者施用了卡托普利，该系统旨在将药物释放到肠道的结肠区域。使用γ闪烁显像法追踪胃肠道转运和脉冲释放情况。发现一种标称5小时后释放的脉冲胶囊系统在体外和体内均具有可重复性。在8名受试者中的6名中，药物被输送到结肠，在其余两名受试者中，药物被输送到回肠末端。在3名受试者中发现了可测量的游离卡托普利血药浓度。药物在远端肠道的可变不稳定性被认为是大多数受试者药物吸收缺乏的一个可能原因。
