氨茶碱栓剂与片剂生物利用度的比较

本文研究了氨茶碱栓剂与片剂的药代动力学参数。经换算后,栓剂360mg与片剂200mg具有相等的血药水平,但栓剂起效慢,维持时间较片剂稍长,临床可根据需要选择使用。氨茶碱栓除对肛门稍有刺激和有排便感外,其他副反应较片剂为轻。

BIOAVAILABILITY OF AMINOPHYLLINE SUPPOSITORY AND TABLET

The parameters of bioavailability for the single administration of aminophylline suppository or aminophylline tablet were investigated in 5 healthy volunteers. The converted values of the maximum blood concentration after administration of a suppository containing 360mg aminophylline or a tablet containing 200mg aminophylline are5.76±0.75ug/ml and 5.72±0.89 ug/ml, respectively. The average time of peak blood concentration for the suppository was found to be 6.71+0.41 hr and for the tablet 1.00±0.19hr. When tablets were used as control, the relative bioavailability of suppository was shown to be 0.82+0.08. These results show that absorption of theophylline from rectal suppositories of aminophylline was slower than that from tablets taken orally. Besides, some irritation on the mucous membrane of the rectum and/or some uncomfortable sensation (tenesmus) were experienced by volunteers who were given suppositories. Its other side-effects were slightly smaller than the tablets.