马昔腾坦片体外溶出度试验和生物等效性研究  

In vitro dissolution test and bioequivalence study of Macitentan tablets

作　　者：徐欣 蔡轶君 张静 XU Xin;CAI Yijun;ZHANG Jing(Shanghai Shangyao Rui’er Pharmaceutical Co.,Ltd.,Shanghai 200000,China)

机构地区：[1]上海上药睿尔药品有限公司,上海200000

出　　处：《江苏科技信息》2024年第19期132-136,共5页Jiangsu Science and Technology Information

摘　　要：针对肺动脉高压(PAH)治疗,文章探究了马昔腾坦片剂的体外溶出度与生物等效性关联,旨在确保自制制剂与参比制剂的人体内相似性。通过溶出度试验方法的深入研究,确立了不同pH溶出介质下的检测标准,以更准确地模拟胃肠道环境。自制制剂与参比制剂的溶出曲线在体外表现出高度一致性,证明了自制制剂具备良好的溶出特性。进一步的人体试验显示,无论餐前还是餐后,两制剂间均呈现生物等效性,确认了自制制剂与参比制剂在吸收速率和程度上的相似性,证实了自制制剂具有与参比制剂相当的生物利用度和治疗潜力,为PAH患者提供了新的治疗选择。For the treatment of pulmonary arterial hypertension(PAH),this article explores the correlation between the in vitro dissolution rate and bioequivalence of Macitentan tablets,aiming to ensure the in vivo similarity between the self-made formulation and the reference formulation.Through in-depth research on dissolution test methods,detection standards were established for different pH dissolution media to more accurately simulate the gastrointestinal environment.The dissolution curves of the homemade formulation and the reference formulation showed high consistency in vitro,proving that the homemade formulation has good dissolution characteristics.Further human trials have shown bioequivalence between the two formulations,both before and after meals,confirming the similarity in absorption rate and degree between the homemade formulation and the reference formulation.This confirms that the homemade formulation has comparable bioavailability and therapeutic potential to the reference formulation,providing a new treatment option for PAH patients.

关 键 词：马昔腾坦片 肺动脉高压 溶出曲线 生物等效性 

分 类 号：R944[医药卫生—药剂学]