Ozaksun Nihal Tugce, Incecayir Tuba
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Etiler, 06330 Ankara, Turkey.
Pharmaceutics. 2025 Aug 28;17(9):1126. doi: 10.3390/pharmaceutics17091126.
: Reflecting the interaction between dissolution and absorption, the biphasic dissolution system is an appealing approach for estimating the intestinal absorption of drugs in humans. The study aims to characterize the suitability of the biphasic in vitro dissolution testing to set up an in vitro-in vivo correlation (IVIVC) for the original and generic immediate-release (IR) tablets of a Biopharmaceutics Classification System (BCS) Class II drug, bicalutamide (BIC). : USP apparatus II paddle was used to conduct dissolution testing. A level A IVIVC was obtained between in vitro partitioning and in vivo absorption data of the original drug. The single-compartmental modeling was used for pharmacokinetic (PK) analysis. The generic product's plasma concentrations were estimated. : There was a good correlation between in vitro and in vivo data ( = 0.98). The area under the concentration-time curve () and maximum plasma concentration () ratios for generic/original were 1.04 ± 0.01 and 0.951 ± 0.026 (mean ± SD), respectively. : The biphasic dissolution testing may present an in vivo predictive tool for developing generic products of poorly soluble and highly permeable drugs such as BIC, which are characterized by pH-independent poor solubility.
双相溶出系统反映了溶出与吸收之间的相互作用，是一种用于评估人体药物肠道吸收的有吸引力的方法。本研究旨在表征双相体外溶出试验对于建立生物药剂学分类系统（BCS）II类药物比卡鲁胺（BIC）的原研和仿制药速释（IR）片剂的体外-体内相关性（IVIVC）的适用性。使用美国药典（USP）II型桨法进行溶出试验。在原研药物的体外分配与体内吸收数据之间获得了A级IVIVC。采用单室模型进行药代动力学（PK）分析，估算了仿制药的血浆浓度。体外和体内数据之间存在良好的相关性（ = 0.98）。仿制药/原研药的浓度-时间曲线下面积（）和最大血浆浓度（）比值分别为1.04±0.01和0.951±0.026（平均值±标准差）。双相溶出试验可能为开发像BIC这样的难溶性和高渗透性药物的仿制药提供一种体内预测工具，这类药物的特点是pH无关的难溶性。
