盐酸雷洛昔芬新型给药系统的研究进展  

Research Progress on New Formulations of Raloxifene

作　　者：张雪秋 王润亿 郭琳 黄钛绚 赖金梅 方晓琴 滕希峰[1,3] 何琳 ZHANG Xueqiu;WANG Runyi;GUO Lin;HUANG Taixuan;LAI Jinmei;FANG Xiaoqin;TENG Xifeng;HE Lin(Guangdong Pharmaceutical Universi,Guangzhou,Guangdong 510006,China;Clinical Medieal Collge of Acupuncture,Moxibustion and Rehabilitation,Guangzhou University of Chinese Medicine,Guangzhou,Guangdong 510006,China;State Administration of Traditional Chinese Medicine Key Laboratory for Production and Development of Lingnan Medicinal Material,Guangzhou,Guangdong 510006,China;Guangdong Provincial Cosmetics Engineering and Technology Research Center,Zhongshan,Guangdong 528458,China)

机构地区：[1]广东药科大学,广东广州510006 [2]广州中医药大学针灸康复临床医学院,广东广州510006 [3]国家中医药管理局岭南药材生产与开发重点研究室,广东广州510006 [4]广东省化妆品工程技术研究中心,广东中山528458

出　　处：《今日药学》2023年第2期95-100,共6页Pharmacy Today

基　　金：广东省医学科学技术研究基金项目(B2021071);2021年广东药科大学大学生创新创业训练计划项目(202110571010)。

摘　　要：盐酸雷洛昔芬是由美国FDA批准上市预防和治疗骨质疏松的选择性雌激素受体调节剂,该药水溶性差,首过效应大,导致了口服生物利用度只有2%等问题,限制了其临床应用。但自微(纳米)乳剂、微球、磷脂复合物、固体分散体、固体脂质纳米粒、纳米晶体等新型给药系统,可以提高盐酸雷洛昔芬的溶解度和生物利用度。本文综述了近年来盐酸雷洛昔芬新型给药系统的研究进展,旨在为盐酸雷洛昔芬的新制剂研究提供参考。Raloxifene hydrochloride is a selective estrogen receptor modulators(SERM)for the prevention and treatment of osteoporosis which is approved by FDA.The oral bioavailability of raloxifene hydrochloride is 2%due to its low aqueous solubility and extensive first-pass metabolism which limits its clinical use.The novel drug delivery systems of self-microemulsion,microsphere,phospholipid complex,solid dispersion,solid lipid nanoparticles,nanocrystals have been reported to improve its solubility and bioavailability.In this review,the formulation studies of raloxifene hydrochloride were summarized in order to provide helpful references forits research and development.

关 键 词：盐酸雷洛昔芬 新型给药系统 研究进展 

分 类 号：R94[医药卫生—药剂学]