析因设计优化塞来昔布凝胶中透皮促渗剂用量研究

发布时间：2018-05-28 06:21

本文选题：析因设计 + 塞来昔布　；参考：《中国药学杂志》2017年04期

【摘要】：目的评价不同用量的透皮促渗剂对塞来昔布凝胶剂皮肤渗透性的影响,为优化透皮促渗剂处方提供实验依据。方法以海藻酸钠为基质,采用析因设计的方法选用4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HPLC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 4个实验组中塞来昔布在12 h内的累积渗透量(Q)分别为27.93、25.12、18.79和19.35μg·cm~(-2),其中促渗剂以1%月桂氮酮和1%薄荷醇配方时Q值最大,达27.93μg·cm~(-2);且塞来昔布的渗透过程符合Higuchi方程,稳态流量(J)及渗透系数(Kp)也均高于其他3个实验组。结论以海藻酸钠为基质,月桂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1%月桂氮酮和1%薄荷醇。
[Abstract]:Objective to evaluate the effect of different doses of transdermal permeation enhancers on the skin permeability of celecoxib gel and to provide experimental basis for optimizing the prescription of transdermal permeation enhancers. Methods the gel was prepared with sodium alginate as matrix, four kinds of transdermal permeating agents with different formulations were selected by factorial design, and the modified Franz diffusion cell was used to prepare the gel. The cumulative osmotic capacity of celecoxib in gel was determined by HPLC within 12 h, and the steady flow rate (J) and permeability coefficient (KPX) were calculated. Results the cumulative osmotic capacity of celecoxib in 12 hours was 27.93 渭 g / cm ~ (-1) and 19.35 渭 g / cm ~ (-2) respectively, in which 1% lauroxone and 1% menthol had the highest Q value (27.93 渭 g / cm ~ (-2), and the osmotic process of celecoxib was in accordance with Higuchi equation. The steady-state flow rate (J) and permeability coefficient (Kp) were also higher than those of the other three experimental groups. Conclusion the combination of lauryl azone and menthol has synergistic effect on the transdermal properties of celecoxib with sodium alginate as the matrix. The optimum concentration of the two formulations is 1% lauryl azone and 1% menthol respectively.
【作者单位】：四川邛崃市医疗中心医院;四川省中医药科学院;四川省人民医院;
【基金】：四川省卫生厅科研基金资助项目(090437)
【分类号】：R943

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