析因设计优化塞来昔布凝胶中透皮促渗剂用量研究

曾明辉, 熊静悦, 朱九群, 黄娟, 何林, 谭正怀

中国药学杂志 ›› 2017, Vol. 52 ›› Issue (4) : 293-297.

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中国药学杂志 ›› 2017, Vol. 52 ›› Issue (4) : 293-297. DOI: 10.11669/cpj.2017.04.010
论著

析因设计优化塞来昔布凝胶中透皮促渗剂用量研究

  • 曾明辉1, 熊静悦2, 朱九群3, 黄娟1, 何林3, 谭正怀2*
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Optimization of the Dose of Penetration Enhancers in Celecoxib Gel by Factorial Design

  • ZENG Ming-hui1, XIONG Jing-yue2, ZHU Jiu-qun3, HUANG Juan1, HE Lin3, TAN Zheng-huai2*
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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19.35 μg·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27.93 μg·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 optimize the formula of celecoxib gel by studying the effects of different doses of penetration enhancers on the penetration of celecoxib through skin in vitro. METHODS With sodium alginate as the gel base, factorial design method was used to choose the optimal formula of penetration enhancers among four different formulas to prepare celecoxib gels. The release rate of celecoxib in the release media was detected by modified Franz diffusion cells method, and the steady percutaneous speed (J), permeability coefficient (Kp) and the accumulative permeation quantity (Q) in 12 h were calculated. RESULTS The accumulative permeation quantity (Q) in 12 h of celecoxib from the gels made with the four different formulas were 27.93,25.12,18.79 and 19.35 μg·cm-2, respectively. The gel with 1% azone and 1% menthol as penetration enhancers had the maximum Q value, 27.93 μg·cm-2, its penetration process conformed to Higuchi equation, and the steady percutaneous speed (J) and permeability coefficient(Kp)were also higher than the other three experimental groups. CONCLUSION With sodium alginate as the gel base, azone and menthol have a synergistic effect on the percutaneous penetration of celecoxib gels, and the best formula is 1% azone and 1% menthol.

关键词

析因设计 / 塞来昔布 / 凝胶剂 / 月桂氮卓酮 / 薄荷醇 / 促渗剂 / 透皮吸收

Key words

factorial design / celecoxib / gel / azone / menthol / penetration enhancer / percutaneous absorption

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曾明辉, 熊静悦, 朱九群, 黄娟, 何林, 谭正怀. 析因设计优化塞来昔布凝胶中透皮促渗剂用量研究[J]. 中国药学杂志, 2017, 52(4): 293-297 https://doi.org/10.11669/cpj.2017.04.010
ZENG Ming-hui, XIONG Jing-yue, ZHU Jiu-qun, HUANG Juan, HE Lin, TAN Zheng-huai. Optimization of the Dose of Penetration Enhancers in Celecoxib Gel by Factorial Design[J]. Chinese Pharmaceutical Journal, 2017, 52(4): 293-297 https://doi.org/10.11669/cpj.2017.04.010
中图分类号: R944   

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基金

四川省卫生厅科研基金资助项目(090437)
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