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监测游离药物浓度:挑战

Monitoring free drug concentrations: challenges.

作者信息

Musteata Florin Marcel

机构信息

Department of Pharmaceutical Sciences, Albany College of Pharmacy & Health Sciences, Albany, NY 12208, USA.

出版信息

Bioanalysis. 2011 Aug;3(15):1753-68. doi: 10.4155/bio.11.187.

DOI:10.4155/bio.11.187
PMID:21827273
Abstract

Measurement of drug concentrations in biological samples is of utmost importance in many research areas. The information about the amount of drug in a biological sample can be given as either total concentration, which ignores the interaction of the drug with the sample matrix, or as free concentration, which shows the portion of molecules able to diffuse through membranes and exert biological activity. Although the historical trend has been towards determining total concentrations, measurement of free concentrations is becoming more important since it correlates better with pharmacological and toxicological effects. This review will discuss the most popular experimental approaches for monitoring free drug concentrations, based on the type of sample to be investigated and the kind of information to be collected. It is shown that the current challenges in measuring free concentrations are: convenience, accuracy, precision, wide applicability, availability of accurate and precise reference methods, ruggedness, and standardized sample conditions.

摘要

在许多研究领域中,测量生物样品中的药物浓度至关重要。生物样品中药物含量的信息可以表示为总浓度(忽略药物与样品基质的相互作用)或游离浓度(显示能够扩散通过膜并发挥生物活性的分子部分)。尽管历史趋势一直是测定总浓度,但游离浓度的测量变得越来越重要,因为它与药理和毒理效应的相关性更好。本综述将根据待研究的样品类型和要收集的信息类型,讨论监测游离药物浓度最常用的实验方法。结果表明,目前测量游离浓度面临的挑战包括:便利性、准确性、精密度、广泛适用性、准确精密参考方法的可用性、耐用性和标准化的样品条件。

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