Nokhodchi Ali, Chavan Salonee, Ghafourian Taravat
Lupin Inhalation Research Center, Lupin Pharmaceuticals, 4006 NW 124th Ave., Coral Springs, FL 33065, USA.
Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton BN1 9QJ, UK.
Pharmaceutics. 2023 Mar 18;15(3):983. doi: 10.3390/pharmaceutics15030983.
In vitro dissolution and permeability testing aid the simulation of the in vivo behavior of inhalation drug products. Although the regulatory bodies have specific guidelines for the dissolution of orally administered dosage forms (e.g., tablets and capsules), this is not the case for orally inhaled formulations, as there is no commonly accepted test for assessing their dissolution pattern. Up until a few years ago, there was no consensus that assessing the dissolution of orally inhaled drugs is a key factor in the assessment of orally inhaled products. With the advancement of research in the field of dissolution methods for orally inhaled products and a focus on systemic delivery of new, poorly water-soluble drugs at higher therapeutic doses, an evaluation of dissolution kinetics is proving crucial. Dissolution and permeability testing can determine the differences between the developed formulations and the innovator's formulations and serve as a useful tool in correlating in vitro and in vivo studies. The current review highlights recent advances in the dissolution and permeability testing of inhalation products and their limitations, including recent cell-based technology. Although a few new dissolution and permeability testing methods have been established that have varying degrees of complexity, none have emerged as the standard method of choice. The review discusses the challenges of establishing methods that can closely simulate the in vivo absorption of drugs. It provides practical insights into method development for various dissolution testing scenarios and challenges with dose collection and particle deposition from inhalation devices for dissolution tests. Furthermore, dissolution kinetic models and statistical tests to compare the dissolution profiles of test and reference products are discussed.
体外溶出度和渗透性测试有助于模拟吸入药物产品的体内行为。尽管监管机构对口服剂型(如片剂和胶囊)的溶出度有具体指导原则,但对于口服吸入制剂并非如此,因为目前尚无普遍认可的评估其溶出模式的测试方法。直到几年前,对于评估口服吸入药物的溶出度是否是评估口服吸入产品的关键因素,还没有达成共识。随着口服吸入产品溶出方法领域研究的进展以及对以更高治疗剂量全身递送新的、水溶性差的药物的关注,溶出动力学评估正证明至关重要。溶出度和渗透性测试可以确定研发制剂与创新制剂之间的差异,并作为关联体外和体内研究的有用工具。本综述重点介绍了吸入产品溶出度和渗透性测试的最新进展及其局限性,包括最近基于细胞的技术。尽管已经建立了一些新的溶出度和渗透性测试方法,其复杂程度各不相同,但尚未出现成为标准选择方法的情况。该综述讨论了建立能够密切模拟药物体内吸收的方法所面临的挑战。它为各种溶出度测试场景的方法开发以及溶出度测试中剂量收集和吸入装置颗粒沉积的挑战提供了实际见解。此外,还讨论了用于比较测试产品和参比产品溶出曲线的溶出动力学模型和统计测试。