扎托洛芬凝胶剂的制备及体外研究

目的制备扎托洛芬凝胶剂,考察其体外渗透性、释放性和稳定性。方法采用紫外分光光度法测定扎托洛芬的含量,采用Franz扩散池分别考察载药凝胶剂体外渗透性和释放性,采用正交试验设计筛选处方,探讨了氮酮、卡波姆浓度及丙二醇用量对扎托洛芬凝胶剂经皮渗透的影响,并对凝胶剂初步稳定性进行了考察。结果扎托洛芬的线性范围为16.0~56.0μg/mL,日内日间精密度的RSD均小于0.6%,平均回收率为98.67%,RSD为1.45%;凝胶剂外观细腻,黏度适宜,pH 6.8~7.0,最佳处方含0.75%卡波姆、15%丙二醇、1%月桂氮卓酮,其体外经皮渗透(以小鼠皮为屏障)符合Higuchi方程,体外释放(以赛璐芬膜为屏障)符合零级动力学方程;室温留样3个月稳定性良好。结论扎托洛芬凝胶剂制备工艺简单,体外渗透性良好,制剂稳定性好。

The preparation of zaltoprofen gel and study on its property in vitro

Purpose To prepare zaltoprofen transcutaneous gel and to study its stability,release and permeation ability in vitro.Methods The content of zaltoprofen was determined by UV method.The in vitro permeation and release test were carried out by a twocompartment diffusion cells with mouse skin and cellophane as barriers.Factors such as the concentration of azone,carbomer and propylene glycol were investigated by an orthogonal design,so that the best formula could be obtained.The stability of zaltoprofen gel was also measured.Results The linear of zaltoprofen was 16.0-56.0 μg/mL.RSDs of the inter and intra precison were both less than 0.6%.The average recovery rate was 98.67% and RSD was 1.45%.The gel had suitable viscosity and pH was 6.8-7.0.The optimal formulation of zaltoprofen gel contained 0.75% carbomer,1% azone and 15% propylene glycol.The process of percutaneous permeation of zaltoprofen gel in vitro conformed to Higuchi equation,and its in vitro release conformed to zero order equation.The results of stability test indicated that there were no notable changes in spread and appearance of gel.Conclusion Zaltoprofen transcutaneous gel can be prepared simply and the quality is controllable.The dosage form possessed good permeation and stability.