Paull P, Day R, Graham G, Champion D
Med J Aust. 1976 Apr 24;1(17):617-9.
The bioavailability of a new enteric-coated tablet of aspirin (Ecotrin, Smith, Kline and French) was evaluated after single doses to eight volunteers. One tablet was administered to each subject on four occasions--twice after a light breakfast, once after a heavy breakfast and once after pretreatment with metoclopramide. The study utilized non-invasive techniques. The rate of absorption of aspirin was estimated by the time course of concentrations of salicylate in saliva, while the total bioavailability was determined by the recovery of total salicylate in urine. The urinary recovery of aspirin from all 32 trials was 575 +/- 25 mg (mean +/- standard error), representing 89% +/- 4% of the administered dose. The different treatments did not significantly alter the urinary recovery. The absorption of aspirin from the enteric-coated tablets was delayed and slow. Absorption was retarded by a heavy meal and hastened by pretreatment with metoclopramide. The effect of metoclopramide is consistent with the release of aspirin in the small intestine. Overall, the single-dose tests indicated satisfactory functioning of the enteric coating.
对8名志愿者单次服用新型肠溶阿司匹林片(益胃平,史克必成公司)后的生物利用度进行了评估。每位受试者在四种情况下各服用一片药:两次在清淡早餐后,一次在丰盛早餐后,一次在服用甲氧氯普胺预处理后。该研究采用了非侵入性技术。通过唾液中水杨酸盐浓度的时间进程来估计阿司匹林的吸收速率,而总生物利用度则通过尿液中总水杨酸盐的回收率来确定。在所有32次试验中,阿司匹林的尿回收率为575±25毫克(平均值±标准误差),占给药剂量的89%±4%。不同的处理方法并未显著改变尿回收率。肠溶片剂中阿司匹林的吸收延迟且缓慢。丰盛的餐食会阻碍吸收,而甲氧氯普胺预处理则会加速吸收。甲氧氯普胺的作用与阿司匹林在小肠中的释放情况一致。总体而言,单剂量试验表明肠溶衣功能良好。