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稳定同位素在药物生物利用度和生物等效性研究中的应用。

The application of stable isotopes to studies of drug bioavailability and bioequivalence.

作者信息

Wolen R L

出版信息

J Clin Pharmacol. 1986 Jul-Aug;26(6):419-24. doi: 10.1002/j.1552-4604.1986.tb03551.x.

Abstract

The increased availability of chemical intermediates and automated instrumentation has resulted in expanded use of stable isotopes for bioavailability and bioequivalence studies in recent years. Initially, stable isotopes were confined to the labeling of mass internal standard compounds for gas chromatography/mass spectrometry. More recently, their in vivo use has expanded and proved to be a powerful pharmacologic tool. The lack of toxicity of stable isotopes, particularly deuterium and carbon-13, make them ideally suited for human studies. The primary advantage of the isotopic methods is that the drug can be administered concomitantly either by two routes (e.g., parenteral and oral) or in two formulations (e.g., solution and solid dosage). Thus, a single set of blood samples serves to describe the time course of the routes or formulations being compared. The concomitant administration reduces variability inherent in dual administration, the single assay for both forms further reduces variation, and the method minimizes both drug exposure and discomfort to the subject. In addition to single-dose administration, in which two routes or dosage forms are compared, the technique is well suited to "pulse" administration, wherein the kinetics of a single dose, during multiple or chronic dosing regimens, can be compared with single-dose kinetics.

摘要

近年来,化学中间体和自动化仪器的可得性增加,使得稳定同位素在生物利用度和生物等效性研究中的应用得到了扩展。最初,稳定同位素仅限于用于气相色谱/质谱的质量内标化合物的标记。最近,它们在体内的应用得到了扩展,并被证明是一种强大的药理学工具。稳定同位素,特别是氘和碳-13,缺乏毒性,使其非常适合人体研究。同位素方法的主要优点是药物可以通过两种途径(例如,肠胃外和口服)或两种剂型(例如,溶液和固体剂型)同时给药。因此,一组血液样本就可以描述所比较的途径或剂型的时间进程。同时给药减少了双重给药中固有的变异性,两种形式的单一测定进一步减少了变异性,并且该方法使药物暴露和受试者的不适最小化。除了比较两种途径或剂型的单剂量给药外,该技术还非常适合“脉冲”给药,即在多次或长期给药方案期间,单剂量的动力学可以与单剂量动力学进行比较。

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