静脉注射和口服给药后血药浓度或血浆浓度-时间曲线下面积之比的通用方程及其在药物消除个体间差异中的应用。
A general equation for the ratio of the areas below the blood or plasma concentration time-curves following intravenous and oral drug administration and its application to inter-subject variations in drug elimination.
作者信息
Vaughan D P, Trainor A
出版信息
Br J Clin Pharmacol. 1975 Jun;2(3):239-50. doi: 10.1111/j.1365-2125.1975.tb01582.x.
Abstract
1 When a drug is metabolized in the liver the total area under the plasma or blood concentration-time curve following oral drug administration is less than the area obtained after intravenous drug administration. This difference has been termed the 'first-pass effect'. 2 General equations for the areas below the blood or plasma concentration-time curve of a drug following intravenous and oral drug administration are derived. 3 An explicit expression for the ratio of areas below the blood or plasma concentration-time curves following intravenous and oral drug administration is derived. 4 By the application of the derived equations it is shown that the relative contribution of hepatic drug metabolism and urinary excretion to inter-subject variation in drug elimination can be easily ascertained.
摘要
- 当一种药物在肝脏中代谢时，口服给药后血浆或血液浓度-时间曲线下的总面积小于静脉给药后获得的面积。这种差异被称为“首过效应”。2. 推导了药物静脉给药和口服给药后血液或血浆浓度-时间曲线下面积的一般方程。3. 推导了静脉给药和口服给药后血液或血浆浓度-时间曲线下面积之比的显式表达式。4. 通过应用推导的方程表明，可以很容易地确定肝脏药物代谢和尿液排泄对药物消除个体间差异的相对贡献。
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A general equation for the ratio of the areas below the blood or plasma concentration time-curves following intravenous and oral drug administration and its application to inter-subject variations in drug elimination.静脉注射和口服给药后血药浓度或血浆浓度-时间曲线下面积之比的通用方程及其在药物消除个体间差异中的应用。
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本文引用的文献
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Concept of a volume of distribution and possible errors in evaluation of this parameter.分布容积的概念以及该参数评估中可能存在的误差。
J Pharm Sci. 1968 Jan;57(1):128-33. doi: 10.1002/jps.2600570125.
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Influence of first-pass effect on availability of drugs on oral administration.首过效应对口服给药时药物可利用度的影响。
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Oral absorption and disposition kinetics of lidocaine hydrochloride in dogs.盐酸利多卡因在犬体内的口服吸收及处置动力学
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Pharmacokinetics of pentazocine in the rhesus monkey.
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An analysis of the inter-subject variation in the metabolism of pentazocine.喷他佐辛代谢的个体间差异分析。
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