期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 101, 期 3, 页码 1327-1335出版社
ELSEVIER SCIENCE INC
DOI: 10.1002/jps.23013
关键词
plasma protein binding; brain homogenate binding; equilibrium dialysis; recovery; stability; nonspecific binding; simulation; ADME
Historically, recovery had been used to evaluate the data quality of plasma protein binding or tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative of high nonspecific binding, instability, or low solubility. This study showed that, when equilibrium was fully established in the dialysis assay, low recovery due to nonspecific binding had no impact on the determination of fraction unbound. The conclusion was supported by the principles of the equilibrium dialysis assay, experimental data, and mathematic simulations. The results suggested that the use of recovery as an acceptance criterion for the equilibrium dialysis assay in drug discovery was too restrictive, and introduced the additional burden of repeating studies unnecessarily. (c) 2011 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:13271335, 2012
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