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脑组织生理药代动力学模型研究进展
引用本文:桑澜, 徐胜, 何华, 柳晓泉. 脑组织生理药代动力学模型研究进展[J]. 药学进展, 2020, 44(12): 942-953.
作者姓名:桑澜  徐胜  何华  柳晓泉
作者单位:1.中国药科大学药物代谢动力学研究中心, 江苏 南京 211198
摘    要:在新药研发过程中,了解药物在脑内的转运与分布情况可以预测药物效应和不良反应。然而,人脑内的药物浓度难以通过现有分析技术直接测定。生理药代动力学(PBPK)模型通过数学建模的方式模拟药物在脑内的转运与分布情况,为预测脑内药物浓度提供帮助。综述影响药物在脑内转运分布的生理因素,以及近年来文献中报道的研究药物脑组织分布的PBPK模型及其在药物研发中的应用。

关 键 词:脑组织  药物转运与分布  生理药代动力学模型
收稿时间:2019-12-30

Advances in Physiologically-Based Pharmacokinetic Models of Brain Tissue
SANG Lan, XU Sheng, HE Hua, LIU Xiaoquan. Advances in Physiologically-Based Pharmacokinetic Models of Brain Tissue[J]. Progress in Pharmaceutical Sciences, 2020, 44(12): 942-953.
Authors:SANG Lan  XU Sheng  HE Hua  LIU Xiaoquan
Affiliation:1.Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 211198, China
Abstract:Characterizing drug transport and distribution within the brain can help predict drug effect and adverse drug reaction during new drug development. However, a major hurdle exists in directly measuring drug concentrations in human brain. Physiologically-based pharmacokinetic (PBPK) modelling of drug transport and distribution in brain tissue is highly beneficial for predicting human brain concentrations. In this article, physiological properties that affect drug transport and distribution within the brain was reviewed. Existing PBPK models of the brain tissue as well as their applications in new drug development were also overviewed.
Keywords:brain tissue  drug transport and distribution  physiologically-based pharmacokinetic modeling
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