Faculty of Pharmaceutical Sciences, Tokyo University of Science, Noda, Japan.
Faculty of Pharmaceutical Sciences, Tokyo University of Science, Noda, Japan.
J Pharm Sci. 2024 Nov;113(11):3137-3144. doi: 10.1016/j.xphs.2024.08.006. Epub 2024 Aug 16.
The present monograph discusses the possibility of BCS-based biowaivers for immediate release pharmaceutical products containing raltegravir potassium, which is used to treat human immunodeficiency virus (HIV) infections. Raltegravir potassium can be assigned to BCS class II or IV since this compound has low solubility and uncertain permeability. Therefore, according to the ICH M9 guideline, it is not recommended to apply BCS-based biowaiver to approval of immediate release solid dosage forms of raltegravir potassium, either for new generic versions or when moderate to major changes in composition and/or the manufacturing method of the product are made.
本专论讨论了基于生物药剂学分类系统（BCS）的豁免生物等效性申请对于含有拉替拉韦钾的即释型药物制剂的可能性，拉替拉韦钾用于治疗人类免疫缺陷病毒（HIV）感染。拉替拉韦钾可被归为 BCS 分类系统 II 类或 IV 类，因为该化合物的溶解度低，渗透性不确定。因此，根据 ICH M9 指南，不建议将基于 BCS 的生物豁免应用于拉替拉韦钾即释固体制剂的批准，无论是新的仿制药版本，还是产品的组成和/或制造方法发生中度至重大变化时。
