长春西汀微乳的优化及其理化性质的考察

目的选择适宜比例的油相、表面活性剂、助表面活性剂和水相制备长春西汀微乳制剂以增加药物的溶解度和经皮渗透量，优化处方，并对其理化性质和刺激性进行研究。方法绘制伪三元相图，确定各相的比例，以经皮稳态渗透流量为指标，利用单纯形网格法优化处方，并考察优化微乳的pH、粘度、电导率、折光率、粒径分布等理化性质。采用MTT法考察微乳制剂对人体皮肤细胞系模型Hacat细胞的毒性。结果O/W微乳在相图中的区域随着表面活性剂和助表面活性剂比例的增加而增加；单纯形网格优化法预测的指标值与实测值相近，所得的优化微乳性质稳定，对Hacat细胞无刺激性，与阴性组无显著性差异。结论长春西汀微乳制剂中药物的溶解度极大提高，经皮稳态渗透流量显著增大，安全稳定，可作为经皮给药的新型载体。

Optimization of microemulsion containing vinpocetine and its physicochemical properties

Aim To prepare the microemulsion of vinpocetine in order to increase solubility and its in vitro transdermal delivery by using appropriate proportion of oil, surfactant (S) , cosurfactant ( CoS) and water. The formulation of proportion was optimized. The physicochemical properties and the skin irritation of the microemulsion was studied. Methods Pseudo-tertiary phase diagrams were prepared to obtain the concentration ratio of components of the microemulsion. Using simplex lattice method, the formulation of microemulsion was optimized and the physicochemical properties including pH, viscosity, refractive index, conductivity and particle size distribution were examined. The MTT method was applied to test the skin irritation of the microemulsion on the Hacat cell. Results The diagrams showed that the areas of O/W microemulsion increased with the increasing ratio of surfactant to cosurfactant ( S/CoS). The predicted values from simplex lattice system were close to that of the experiment. The property of optimized microemulsion showed to be stable behavior and not irritant to Hacat cell. Conclusion The drug solubility and in vitro perscutaneous permeation flux of the optimized microemulsion was improved significantly and the irritation study showed that optimized microemulsion was safe as an ideal transdermal delivery system.