以羟丙基甲基纤维素为基质的塞来昔布凝胶中透皮促进剂配方研究

Study on the formula of penetration enhancers in celecoxib gels with hydroxypropyl methylcellulose as vehicle

目的评价不同配方的的透皮促渗剂对塞来昔布凝胶剂皮肤渗透性的影响,为优化透皮促渗剂配方提供实验依据。方法以羟丙基甲基纤维素为基质,采用析因设计的方法选用四种不同配方的透皮促渗剂制备凝胶剂;用改良的Franz扩散池,以高效液相色谱法测定凝胶剂中塞来昔布在12 h内的累积渗透量(Q),并计算其稳态流量(J)和渗透系数(Kp)。结果四个实验组中塞来昔布在12 h内的Q值分别为26.51、13.87、14.92和27.51μg/cm^2,其中促渗剂以2%氮酮和0.5%薄荷醇配方时Q值最大,达27.51μg/cm^2;且塞来昔布的渗透过程符合Higuchi方程,J值及Kp也均高于其它三个实验组。结论以羟丙基甲基纤维素为凝胶基质时,氮酮与薄荷醇联用对塞来昔布透皮特性具有协同增效作用,在实验配方浓度内,两者最佳配方浓度分别为2%氮酮和0.5%薄荷醇。

Objective To evaluate the effect of different formula of penetration enhancers in the celeeoxib gels on skin permeability in order to provide experimental evidence for optimization of transdermal permeability agent formula. Methods With hydroxypropyl methylcellulose as vehicle, four different kinds of formula of penetration enhancers were selected to prepare gels by the factorial design method. The release rate of celdcoxib in release media was detected by modified Franz diffusion ceils. The steady percutaneous speed （J） and permeability coefficient （Kp） and 12-hour accumulative permeation quantity （Q） were calculated. Results The Q values of celecoxib in the four different tests were 26. 51,13.87,14. 92 and 27.51μg/cm^2, respectively. The Q value was 27.51 μg/cm^2when the penetration enhancers with 2% azone and 0. 5% menthol recipes were used. The infiltration process of celecoxib was in accordance with Higuchi equation. The values of J and Kp were also the highest among the four experimental groups. Conclusion With sodium alginate as vehicle,azane and menthol have a synergistic effect on the celecoxib gels. The best formula is 2% azone and 0. 5% menthol.