从体外模型预测药物生物利用度的前景展望

Onyeji Co
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引用次数: 0

摘要

各种药典中都有关于不同溶解介质的描述,但这些介质并不能预测生物利用度。为了解决这个问题,人们开发了生物相关介质和不同的模型作为替代品。本报告旨在重点介绍一些生物相关介质,并评估它们与预测体内药物性能的相关性。显然,生物相关介质比药典介质更能反映胃肠液的内容。此外,生物相关溶解方法与渗透性测量和其他模型以及计算模拟相结合,已被用于预测药物的口服吸收。根据体外数据预测生物利用度需要在溶出率等体外测量数据与生物利用度参数等药物制剂体内性能之间建立体外-体内相关性(IVIVC)。
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Insights on Prospects of Prediction of Drug Bioavailability from in Vitro Models
The various pharmacopoeias contain descriptions of different dissolution media but these are however not predictive of bioavailability. To solve this problem, biorelevant media and different models have been developed as alternatives. The aim of this report was to highlight some of the biorelevant media and appraise their relevance to predict in vivo drug performance. It was apparent that the biorelevant media reflect contents of the gastrointestinal fluids better than the pharmacopoeial media. Also, bio-relevant dissolution methods, combined with permeability measurements and other models along with computational simulations have been used to predict the oral absorption of drug. Prediction of bioavailability from in vitro data involves the establishment of an in vitro-in vivo correlation (IVIVC) between an in vitro measurement such as dissolution rate data and the in vivo performance of the drug formulation such as the bioavailability parameters.
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