Dissolution of poorly water-soluble drugs in biphasic media using USP 4 and fiber optic system

Clinical Research and Regulatory Affairs Pub Date : 2009-06-01 DOI:10.1080/10601330902905887

S. Vangani, Xiaoling Li, Peter Zhou, M. Del-Barrio, R. Chiu, Nina S. Cauchon, P. Gao, Cesar Medina, B. Jasti

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引用次数: 46

Abstract

A novel in-vitro dissolution system based on the principle of flow-through technique has been designed to evaluate the in-vitro release rate of poorly water-soluble compounds. The flow through apparatus (USP 4) has been coupled with the compendial dissolution apparatus (USP apparatus 2). A bi-phasic dissolution medium is used to achieve sink conditions. The dissolved drug is continuously removed from the aqueous phase into the organic phase of the dissolution medium, mimicking the process of absorption in the systemic circulation. The in vitro release profiles obtained from this dissolution model was able to distinguish the formulation changes of several poorly water-soluble drugs from their dosage forms. For AMG 517, the model drug, excellent rank order correlation has been obtained between the in-vitro release and the in-vivo absorption of the drug from several different dosage forms and their formulations. In addition, for several commercial formulations, the model successfully discriminated between the bioequivalent and non-bioequivalent formulations.

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使用usp4和光纤系统在双相介质中溶解水溶性差的药物

本文设计了一种基于流动技术原理的体外溶出体系，用于评价难水溶性化合物的体外释放速度。通过装置(USP 4)与药典溶解装置(USP装置2)耦合。使用双相溶解介质来达到沉淀条件。溶解后的药物连续地从水相中析出，进入溶解介质的有机相，模拟体循环中的吸收过程。利用该溶出度模型获得的体外释放曲线能够区分几种水溶性较差药物的剂型变化。以模型药物AMG 517为例，不同剂型及其制剂的体外释放度与体内吸收具有良好的秩序相关性。此外，对于几种商业制剂，该模型成功地区分了生物等效性和非生物等效性制剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Clinical Research and Regulatory Affairs

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