盐酸博安霉素注射用温度敏感原位凝胶的研究

Thermosensitive in situ gel of boanmycin hydrochloride for injection

本文以泊洛沙姆F127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力学。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,方便注射给药,胶凝后呈现三维网状空间结构,药物的扩散和凝胶材料的溶蚀为控制药物释放的主要因素。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。

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 ℃,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.