星点设计-效应面法优化盐酸川芎嗪眼用温度敏感型原位凝胶的处方

探讨星点设计-效应面法优化盐酸川芎嗪眼用温度敏感型原位凝胶的处方。采用泊洛沙姆407和泊洛沙姆188为温敏材料,以模拟泪液稀释前后的溶液-凝胶相转变温度为考察指标,采用星点设计-效应面法对处方进行优化并进行验证。经过优化的处方组成为22.5%泊洛沙姆407和5%泊洛沙姆188;优化处方制备的凝胶在26.9℃为自由流动的液体,经模拟泪液稀释后在32.5℃转变为凝胶。星点设计-效应面法适用于盐酸川芎嗪眼用温度敏感型原位凝胶的处方优化,所建立的模型预测性良好,该眼用温敏凝胶符合眼部应用要求。

Optimization of the Rmosensitive in Situ Gel System Containing Ligustrazine Hydrochloride for Ocular Use by Central Composite Design - Response Surface Methodology

To optimize the thermosensitive in situ gel system containing ligustrazine hydrochloride for ocular use by central composite design - response surgace methodology. The in situ thermosensitive gel system containing ligustrazine hydrochloride was prepared by Poloxamer 407（P407）and Poloxamer 188（ P188）as thermosensitive materials. The phase transition temperature of the solution - gel before and after the simulated tear fluid（STF）dilution was used as index. The mathematic relation of the factors and indicators were descirbed using binomial mode1 and the formulation was optimized and validated by supeirmposed contour plot. Optimized fomrulation of in situ thermosensitive gel system containing ligustrazine hydrochloride consisted of 22. 5% of P407 and 5% of P188,which was a free - flowing liquid at room temperature and converted to gel after STF dilution. The central composite design - response surface methodology is useful for optimization and the estimation of stablished model is good. The thermo - sensitive in situ gel system satisfied the requirement of ophthalmic application.