摘要
近二十年来，稳定同位素示踪技术在临床药代动力学研究中有了快速发展。采用气相色谱一质谱或液相色谱一质谱联机技术检测生物样本中标记药物和未标记药物，具有较高的测试专属性和灵敏度。稳定同位素标记药物的主要作用是作为“分析内标”和“生物内标”，作生物内标时可将标记药物用于人体。本文介绍了稳定同位素标记药物的有关知识及该技术在药物的生物利用度、生物等效性、药物吸收、药物处置及药物相互作用研究中的应用原理与方法。该法具有减少体内药物处置的个体内差异，减少受试者数目，提高药代动力学数据的可信度等优点，但也有一些原因限制了该项技术的广泛应用。
The application of stable isotope tracer technique has rapidly increased in clinical pharmacokinetic studies over the past two decades. The stable isotope labelled (SIL) and labelled drugs in biological samples were measured by GC-MS or LC-MS and higher specificity or sensitivity can be obtained. The major applications of SIL drugs are as analytical internal standard' and as 'biological internal standards'. The latter use is accomplished by administering the SIL drug to man. In this review some knowledge about SIL drugs were introduced and the principle and methods of using SIL tracer technique in bioavailability, bioequivalence, drug absorption, ding disposition and drug interaction studies were concluded. The major advantages of using stable isotope labelled drug are' (a) that intrasubject variability in drug disposition are minimized; (b) a small number of subjects are required; (c) reliability of pharmacokinetic data is increased by substituting administration only once for 2 occasions. However, some reasons limit the use of this methodology.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2000年第1期58-62,共5页
The Chinese Journal of Clinical Pharmacology
