MICHAELIS-MENTEN ABSORPTION KINETICS IN DRUGS - EXAMPLES AND IMPLICATIONS
MICHAELIS-MENTEN ABSORPTION KINETICS IN DRUGS - EXAMPLES AND IMPLICATIONS
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DOI：
10.1007/bf00545976
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发表时间：
1982-01-01
影响因子：
2.9
通讯作者：
THAKKER, KM
中科院分区：
文献类型：
--
作者：
WOOD, JH;THAKKER, KM
保泰松、萘普生和氯噻嗪的吸收受剂量限制机制控制。这种剂量依赖性可以通过数学上服从Michaelis-Menten型动力学的饱和吸收过程来解释。如果假设吸收过程为饱和过程，则可以解释四环素、苯甲酸和相关化合物、苯妥英以及可能的地高辛和洋地黄毒苷的观察到的剂量关系。这种行为可能是由药物化合物的不溶性、胃肠道中有限的吸收窗口或由于载体或所涉及的转运机制而导致的容量受限的吸收产生的。适当设计的新药物化合物的剂量反应研究的需要进行了讨论。
The absorption of phenylbutazone, naproxen and chlorthiazide is governed by a dose-limiting mechanism. This dose-dependency may be explained by a saturation absorption process mathematically obeying Michaelis-Menten type kinetics. Observed dose relationships for tetracycline, fenclozic acid and related compounds, phenytoin and possibly digoxin and digitoxin may be explained if a saturable process in absorption is postulated. This behavior may be produced by isolubility of the drug compound, a limited window of absorption in the gastrointestinal tract, or a capacity limited absorption because of the carrier or the transport mechanism involved. The need for suitably designed dose response studies with new drug compounds is discussed.