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用于结肠吸收的临床前模型及其在控释制剂开发中的应用。

Preclinical models for colonic absorption, application to controlled release formulation development.

机构信息

Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University, Spain; Pharmacokinetics, Pharmaceutical Technology and Parasitology, University of Valencia, Spain.

Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University, Spain.

出版信息

Eur J Pharm Biopharm. 2018 Sep;130:247-259. doi: 10.1016/j.ejpb.2018.07.008. Epub 2018 Jul 6.

Abstract

Oral controlled release (CR) formulations have many benefits and have become a valuable resource for the local and systemic administration of drugs. The most important characteristic of these pharmaceutical products is that drug absorption occurs mainly in the colon. Therefore, this review analyses the physiological and physicochemical features that may affect an orally administered CR product, as well as the different strategies to develop a CR dosage form and the methods used to evaluate the formulation efficacy. The models available to study the intestinal permeability and their applicability to colonic permeability determinations are also discussed.

摘要

口服控释(CR)制剂具有许多优点,已成为局部和全身给药的重要药物资源。这些药物制剂最重要的特征是药物吸收主要发生在结肠。因此,本综述分析了可能影响口服 CR 产品的生理和物理化学特性,以及开发 CR 剂型的不同策略和评估制剂功效的方法。还讨论了可用于研究肠道通透性的模型及其在结肠通透性测定中的适用性。

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