甲氨蝶呤皮下注射用原位凝胶的研制

Preparation of Methotrexate-loaded in situ Gel for Subcutaneous Injection

以壳聚糖-甘油磷酸钠温敏水凝胶为载体,构建甲氨蝶呤皮下注射用原位凝胶。以壳聚糖和甘油磷酸钠的用量为自变量,黏度和胶凝时间为因变量,通过星点设计-效应面法优化处方。结果表明,壳聚糖和甘油磷酸钠的优化用量为1.69%和13.03%。此条件下制得的凝胶黏度为(184.0±12.5)mPa·s,胶凝时间为(6±2)min,pH值为7.01±0.05,并且冻干后能在30 d内保持稳定。

The methotrexate-loaded in situ gel for subcutaneous injection based on thermo-sensitive chitosan/ glycerophosphate （CS/GP） hydrogel was prepared. The formulation was optimized by central composite design and response surface methodology with amounts of CS and GP as independent variables and the time of gelation and the viscosity as dependent variables. The compositions of the optimal formulation were determined as 1.69 % CS and 13.03 % GE The observed optimized formulation had viscosity of （184.0±12.5）mPa.s, gelation time of （6±2） min and pH value of 7.01±0.05. Moreover, the product could maintain stable within 30 d after lyophilization.