摘要
目的:比较3种不同类型磷酸川芎嗪鼻用原位凝胶与人工鼻液混合后的胶凝行为,筛选合适的凝胶基质类型,再以星点设计-效应面法确定基质的优选处方配比。方法:以凝胶强度与胶凝速度为指标,选出合适的磷酸川芎嗪原位凝胶基质类型。再以基质处方中主要成分及増黏剂含量为自变量,基质与人工鼻液混合后的胶凝温度为因变量,采用星点设计-效应面法优选制剂处方,并进行处方验证。结果:指标与因素之间采用二项式拟合,r2 =0.978 7,优选处方P407用量为20.11%,P188用量为6.94%,PEG600用量为2.01%,3批验证样品胶凝温度均在32~34℃之间,说明二次模型拟合效果良好。结论:采用优选处方制备的温敏型磷酸川芎嗪鼻用原位凝胶具有理想的胶凝温度,星点设计-效应面法所建立的基质配比影响胶凝温度的数学模型具有良好的拟合精度与数据预测性。
OBJECTIVE To compare the gelation behavior of three different types of ligustrazine phosphate nasal in situ gel mixed with artificial nasal liquid, to screen the suitable gel matrix type and determine the optimal formulation ratio of the matrix by star design-response surface method. METHODS The suitable in situ gel matrix of ligustrazine phosphate was selected by gel strength and gel speed. Then, the formulation was optimized by star design-response surface methodology with the content of main ingredients and viscosity-increasing agent in the matrix formulation as independent variables and the gelation temperature after mixing the matrix and artificial nose fluid as dependent variables, and formulation validation was performed. RESULTS Binomial fitting was used between the indexes and the factors,r^2=0.978 7. The optimal dosage of P407 was 20.11%, P188 was 6.94%, PEG600 was 2.01%. The gelation temperatures of the three batches of validated samples were between 32-34 ℃, which showed the quadratic model had a good fitting effect. CONCLUSION Thermosensitive tetramethylpyrazine phosphate in situ gel prepared by the optimized prescription has an ideal gelation temperature. And the mathematical model of matrix ratio affecting gelation temperature established by star design-response surface method, which has good fitting accuracy and data predictability.
作者
刘新国
舒翔
LIU Xin-guo;SHU Xiang(Department of Pharmacy,The First Hospital of Wuhan,Hubei Wuhan 430022,China)
出处
《中国医院药学杂志》
CAS
北大核心
2019年第21期2168-2171,2197,共5页
Chinese Journal of Hospital Pharmacy
基金
湖北省卫生与计划生育委员会资助项目(编号:WJ2017M180)
关键词
磷酸川芎嗪
鼻用凝胶
温敏凝胶
星点设计-效应面法
ligustrazine phosphate
nasal gel
thermosensitive gel
central composite design-response surface method
