盐酸博安霉素注射用温度敏感原位凝胶的研究.pdf

药学学报 Acta Pharmaceutica Sinica 20 11, 46 (6) : 727732 ·727 · 盐酸博安霉素注射用温度敏感原位凝胶的研究 * 丁维明, 李 眉, 李桂玲 , 许鸿章, 陈汝贤 ( 中国医学科学院、北京协和医学院医 生物技术研究所, 北京 100050) 摘要: 本文以泊洛沙姆F 127 为主要基质材料, 复合使用泊洛沙姆F68 和高分子材料羟丙基甲基纤维素K4M, 制备盐酸博安霉素注射用温度敏感原位凝胶。对凝胶的胶凝温度、流变学、质构特性、电镜结构和体外释放等 性能进行了研究, 并考察了该制剂在大鼠体内的药代动 学。结果表明, 制备的盐酸博安霉素注射用温度敏感原 位凝胶在常温下为流动的液体, 在人体温度下能够发生相转变, 成为具有一定胶凝强度的半固体, 方便注射给 , 胶凝后呈现三维网状空间结构, 物的扩散和凝胶材料的溶蚀为控制 物释放的主要因素。该制剂具有明显的 缓释作用, 在大鼠体内可以持续释放48 h 以上。 关键词: 盐酸博安霉素; 温度敏感原位凝胶; 胶凝温度; 流变学; 质构特性; 药代动 学 中图分类号: R943.4 文献标识码:A 文章编号: 0513-4870 (20 11) 06-0727-06 Thermosensitive in situ gel of boanmycin hydrochloride for injection * DING Wei-ming, LI Mei, LI Gui-ling , XU Hong-zhang, CHEN Ru-xian (Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences Peking Union M edical College, Beij ing 100050, China) Abstract: Poloxamer F 127, poloxamer F68 and hydroxypropyl methylcellulose K4M were used to prepare the thermosensitive in situ gel of boanmycin hydrochloride for inj ection. Its gelation temperature, rheological behavior, texture characteristics, scanning electron microscopy, in vitro and in vivo drug release were evaluated. These results showed that the formulation was a fluid solution at room temperature, which could become semisolid at the temperature of 37 ℃, and the thermally induced sol-gel transition allowed to be inj ectable and in situ setting. The formulation was constructed into a tridimensional network at gelation temperature. The drug rel