In vitro-in vivo correlation for complex non-oral drug products: Where do we stand?
In vitro-in vivo correlation for complex non-oral drug products: Where do we stand?
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DOI：
10.1016/j.jconrel.2015.09.052
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发表时间：
2015-12-10
影响因子：
10.8
通讯作者：
Burgess, Diane J.
中科院分区：
文献类型：
--
作者：
Shen, Jie;Burgess, Diane J.
体外-体内相关性 (IVIVC) 是一种预测数学模型，描述药品的体外特性与相关体内反应之间的关系。自1997年美国食品和药物管理局（FDA）发布关于缓释（ER）口服剂型的IVIVC开发、评估和应用的监管指南以来，IVIVC一直是药剂学领域最重要的问题之一。然而，即使在 FDA IVIVC 指南的帮助下，也只有非常有限的 ER 口服药物产品的简化新药申请 (ANDA) 提交包含足够的 IVIVC 数据，以便能够在第一个审评周期内完成生物等效性 (BE) 审评。由于非口服剂型的复杂性以及缺乏能够模拟体内药物释放条件的体外释放方法，建立非口服剂型的 IVIVC 仍然极具挑战性。本综述概述了 IVIVC 复杂非口服剂型（例如肠外聚合物微球/植入剂和透皮制剂）开发的最新进展，并简要总结了过去二十年所获得的知识。最后，本综述讨论了复杂非口服剂型 IVIVC 未来发展的可能方向。 (C) 2015 Elsevier B.V. 保留所有权利。
In vitro-in vivo correlation (IVIVC) is a predictive mathematical model describing the relationship between an in vitro property and a relevant in vivo response of drug products. Since the U.S. Food and Drug Administration (FDA) published a regulatory guidance on the development, evaluation, and applications of IVIVC for extended release (ER) oral dosage forms in 1997, IVIVC has been one of the most important issues in the field of pharmaceutics. However, even with the aid of the FDA IVIVC Guidance, only very limited Abbreviated New Drug Application (ANDA) submission for ER oral drug products included adequate IVIVC data to enable the completion of bioequivalence (BE) review within first review cycle. Establishing an IVIVC for non-oral dosage forms has remained extremely challenging due to their complex nature and the lack of in vitro release methods that are capable of mimicking in vivo drug release conditions. This review presents a general overview of recent advances in the development of IVIVC for complex non-oral dosage forms (such as parenteral polymeric microspheres/implants, and transdermal formulations), and briefly summarizes the knowledge gained over the past two decades. Lastly this review discusses possible directions for future development of IVIVC for complex non-oral dosage forms. (C) 2015 Elsevier B.V. All rights reserved.