盐酸雷洛昔芬新型给药系统的研究进展

Research Progress on New Formulations of Raloxifene

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.