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 Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2011 Jun;46(6):727-32.
Poloxamer F127, poloxamer F68 and hydroxypropyl methylcellulose K4M were used to prepare the thermosensitive in situ gel of boanmycin hydrochloride for injection. 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 degrees C, and the thermally induced sol-gel transition allowed to be injectable and in situ setting. The formulation was constructed into a tridimensional network at gelation temperature. The drug release was controlled by the diffusion of the drug and the erosion of the gelmatrix. The pharmacokinetics indicated that the drug could be released slowly for up to 48 hours after subcutaneous administration in rats.
泊洛沙姆F127、泊洛沙姆F68和羟丙基甲基纤维素K4M用于制备注射用盐酸博安霉素热敏原位凝胶。对其凝胶化温度、流变行为、质地特性、扫描电子显微镜、体外和体内药物释放进行了评估。这些结果表明，该制剂在室温下为流体溶液，在37℃时可变为半固体，热诱导的溶胶-凝胶转变使其可注射并原位凝固。该制剂在凝胶化温度下形成三维网络。药物释放受药物扩散和凝胶基质侵蚀的控制。药代动力学表明，大鼠皮下给药后，药物可缓慢释放长达48小时。
