Pharmaceutical Consultant, 11309 Dunleith Place, North Potomac, MD 20878, USA.
Center for Drug Sciences, Faculty of Pharmacy, University of Medicine and Pharmacy Carol Davila Bucharest, 6 Traian Vuia, 020956 Bucharest, Romania.
Int J Pharm. 2022 Oct 15;626:122159. doi: 10.1016/j.ijpharm.2022.122159. Epub 2022 Sep 5.
In vitro drug release test has become one of the most important tools for drug development and approval process of semisolid dosage forms. In vitro release test (IVRT) has the ability to reflect the combined effects of several physicochemical characteristics, particle or droplet size, viscosity, microstructure arrangement of the matter and state of aggregation of dosage form. Genesis of IVRT, its principles and rank order relationship with pharmacodynamic response such as vasoconstriction or dermatopharmacokinetic (skin stripping) results and the evolution of test requirements for regulatory approval is discussed. IVRT reflects various parameters and is an essential part of the stepwise approach to compare topical formulation and its ability to release active in similar quantity at similar rate. Therefore, it is an essential tool, in addition to similar qualitative and quantitative composition (Q1 Q2), to assess the similarity of microstructural arrangement (Q3) as proposed in the Topical drug Classification System (TCS) approach of classes 1 and 3. The TCS system along with evolving concept for topical dermatological drug products from Q1, Q2, Q3 sameness to Q1, Q2, Q3 similar allowing greater permissiveness in formulation changes is discussed.
体外释放试验已成为半固体制剂药物开发和审批过程中最重要的工具之一。体外释放试验（IVRT）能够反映出多种物理化学特性、粒子或液滴大小、黏度、物质的微观结构排列和聚集状态的综合影响。本文讨论了 IVRT 的起源、原理及其与药效反应（如血管收缩或皮肤药代动力学（皮肤剥落）结果）之间的等级关系，以及监管批准的测试要求的演变。IVRT 反映了各种参数，是逐步比较局部制剂及其以相似速率释放活性成分的能力的重要组成部分。因此，除了类似的定性和定量组成（Q1 Q2）之外，它还是评估微观结构排列相似性（Q3）的必要工具，正如在局部药物分类系统（TCS）方法的 1 类和 3 类中所提出的。本文还讨论了 TCS 系统以及从 Q1、Q2、Q3 相同到 Q1、Q2、Q3 相似的局部皮肤科药物产品的不断发展的概念，允许在配方变化方面有更大的宽容度。
