Kim Yejin, Park Eun Ji, Kim Tae Wan, Na Dong Hee
College of Pharmacy, Chung-Ang University, Seoul 06974, Korea.
G2GBIO, Inc., Daejeon 34054, Korea.
Pharmaceutics. 2021 Aug 23;13(8):1313. doi: 10.3390/pharmaceutics13081313.
Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro-in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.
生物聚合物微粒已被广泛用于半衰期短的化学品或合成肽的长期释放制剂。微粒药物释放的表征对于确保产品质量和预期的药理作用很重要。然而，对于长期释放的肠胃外剂型没有官方方法。已经做了很多工作来开发体外药物释放测试方法，通常分为三大类：取样分离法、透析膜法和连续流动（流通池）法。体外药物释放测试在深入了解产品的体内性能方面也起着重要作用。具有体内相关性的体外释放测试可以降低进行体内研究的成本并加速药物产品开发。因此，体外-体内相关性（IVIVC）的研究越来越成为微粒制剂开发的重要组成部分。本综述结合近期研究文章总结了生物聚合物微粒系统体外释放测试方法的原理，并讨论了它们的特点，包括IVIVC、加速释放测试方法和包封药物的稳定性。
