外用药物制剂体外释放试验技术要求概况

Technical requirements of in vitro release test studies for topical drug products

外用药物制剂具有复杂的药物递送途径,通常局部起效,辅料成分复杂,处方组成和制备工艺参数的微小差异就有可能导致产品的质量特性不同,从而影响药物的安全性和有效性。体外释放试验(IVRT)可用于表征一个产品批次的稳态药物释放速率,表征某些工艺、配方和/或生产的变更对药品的影响,在某些情况下,可用于论证产品批量放大或上市后变更的等效性。尽管IVRT不能模拟体内性能情况,但其仍是一项关键质量属性,应订入产品放行和货架期质量标准。本文参考国内外相关技术指导原则及文献,对皮肤外用制剂的IVRT研究技术要求概况进行综述,以期为业内人士提供参考。

Due to the complex delivery of topical drug products,involving local action,and complexity of certain formulations,small differences in prescription compositions and preparation parameters may lead to different quality characteristics of products,thus affecting the safety and effectiveness of drugs.In vitro release test(IVRT)can be used to characterize the steady-state drug release rate of a product batch,and the influence of certain processes,formulations,and/or manufacturing changes on a drug product.Comparing the steady-state drug release rate of the postchange(test)and prechange(reference)products,typically in the context of scale-up or post-approval changes for an approved drug product,helps demonstrate equivalence of drugs in certain situations.Though IVRT does not simulate the in vivo performance,as a critical quality attribute,the release rate should be specified in the approval of finished products and shelf life specification,unless otherwise justified.This paper reviews the technical requirements of IVRT studies of topical drug products by referring to relevant technical guidelines and literatures.