DRUG ABSORPTION .I. AN IN SITU RAT GUT TECHNIQUE YIELDING REALISTIC ABSORPTION RATES

DRUG ABSORPTION .I. AN IN SITU RAT GUT TECHNIQUE YIELDING REALISTIC ABSORPTION RATES
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DOI:
10.1002/jps.2600581006
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发表时间:
1969-01-01
影响因子:
3.8
通讯作者:
SWINTOSKY, JV
SWINTOSKY, JV
中科院分区:
医学3区
文献类型:
--
作者:
DOLUISIO, JT;BILLUPS, NF;SWINTOSKY, JV

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本文报道了一种研究麻醉大鼠离体肠段胃肠药物吸收的方法。该实验技术简单,利用了现成的实验室设备。结果重复性好,吸收速率与已知药物在人体和完整动物体内的吸收行为比较接近。药物在肠腔内的消失遵循表观一级动力学,在pH值为6的条件下测得的半衰期如下:氨基比林32分钟;巴比妥钠19分钟;氟哌啶醇24分钟;丙氯哌嗪23分钟;水杨酸8分钟;磺胺乙咪唑32分钟。这些吸收速率比通常在肠道制剂中观察到的要快得多。此外,还提供了大鼠胃原位吸收速率以及禁食时间与大鼠肠道吸收速率之间关系的初步数据。
A method is reported for studying gastrointestinal drug absorption from isolated gut segments of the anesthetized ratin situ. The experimental technique is simple and utilizes readily available laboratory equipment. The results are closely reproducible and yield absorption rates which are realistic in terms of the known absorption behavior of drugs in humans and intact animals. Disappearance of the drugs from the lumen of the small intestine followed apparent first-order kinetics; and the following half-lives were determined at pH 6: aminopyrine, 32 min.; barbital, 19 min.; haloperidol, 24 min.; prochlorperazine, 23 min.; salicylic acid, 8 min,; and sulfaethidole, 32 min. These absorption rates are much faster than those normally observed inin situintestinal preparations. Absorption rates from rat stomachin situ, and preliminary data showing a relationship between fasting time and intestinal absorption rates in the rat are also presented.