运用裂区设计寻找塞来昔布凝胶最佳配方

发布时间：2018-03-08 09:37

本文选题：塞来昔布　切入点：透皮吸收　出处：《中国医院药学杂志》2017年21期 　论文类型：期刊论文

【摘要】：目的:寻找塞来昔布(celecoxib,CLX)凝胶的最佳配方。方法:采用三裂式裂区设计,主区为羟丙基甲基纤维素、海藻酸钠及卡波姆3种基质,副处理为透皮剂月桂氮芯卓酮(氮酮)的两种水平(1.0%和2.0%),亚副处理为透皮剂薄荷醇的两种水平(0.5%和1.0%),重复3次实验。运用改良的Franz扩散池,选用不同配方塞来昔布制剂作促渗性试验,采用HPLC法测定和计算药物12 h累积释放量(Q)。结果:裂区分析发现区组之间并无显著差异,但各种基质之间存在显著差异;透皮剂氮酮及薄荷醇均对CLX透过皮肤起着非常重要的促进作用,氮酮、薄荷醇均与基质存在显著的协同交互作用;薄荷醇与氮酮之间,以及薄荷醇、基质和氮酮三者之间均存在显著的协同交互作用。进一步的析因设计的方差分析发现在以羟丙基甲基纤维素为基质的凝胶中,氮酮在促进CLX透过皮肤的过程中发挥主要作用;薄荷醇则对CLX透过皮肤无明显作用,但氮酮与薄荷醇合用对CLX透过皮肤表现出显著的协同增效作用。在海藻酸钠为基质的凝胶中,氮酮、薄荷醇均可显著促进CLX透过皮肤;两者合用,对CLX透过皮肤表现出显著的协同增效作用。在以卡波姆为基质的凝胶中,氮酮以及薄荷醇均无显著促进CLX透过皮肤的作用;氮酮与薄荷醇合用也无显著的协同或拮抗作用。结论:本研究结果提示,塞来昔布凝胶配方以6号(海藻酸钠+1.0%氮酮和0.5%薄荷醇)为最佳。同时也表明一种化学物质透过皮肤的量,既与其本身的性质有关,也与透皮剂的种类及性质有关,还与凝胶基质的性质有关。
[Abstract]:Objective: to find out the best formula of celecoxibX) gel. Methods: the three fracturing region design was used, the main region was hydroxypropyl methyl cellulose, sodium alginate and carbomer, and the main region was hydroxy propyl methyl cellulose, sodium alginate and carbomer. The secondary treatment was 1.0% and 2.0% of the transdermal agent lauryl azone (azone), and the sub-treatment was 0.5% and 1.0% of the transdermal agent menthol. The experiment was repeated three times. The modified Franz diffusion cell was used. Different formulations of celecoxib were used for promoting permeability test, and HPLC method was used to determine and calculate the cumulative release amount of the drug for 12 h. Results: there was no significant difference between the fracturing zone groups, but there were significant differences among different substrates. Transdermal agents such as azone and menthol play a very important role in promoting the penetration of CLX through the skin. There is a significant synergistic interaction between azone and menthol, and between menthol and azone, as well as between menthol and menthol. There was a significant synergistic interaction between matrix and azone. Further variance analysis of factorial design found that azone played a major role in promoting the penetration of CLX through the skin in the gel based on hydroxypropyl methyl cellulose. Menthol had no obvious effect on the skin penetration of CLX, but the combination of azone and menthol showed a significant synergistic effect on the skin penetration of CLX. In the gel based on sodium alginate, azone and menthol could significantly promote the penetration of CLX through the skin. In the gel with carbomer, azone and menthol did not significantly promote the penetration of CLX through the skin. The combination of azone and menthol has no significant synergistic or antagonistic effect. Celecoxib gel formulation is best with No. 6 (sodium alginate 1.0% azone and 0.5% menthol). It also shows that the amount of a chemical passing through the skin is related both to its own properties and to the types and properties of transdermal agents. It is also related to the properties of gel matrix.
【作者单位】：四川省中医药科学院;四川省人民医院;邛崃市医疗中心医院;
【基金】：四川省中医药管理局科研课题(编号:2010-G-093) 四川省卫生厅科研基金资助项目(编号:090437)
【分类号】：R943

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