本文選題：塞來昔布　切入點(diǎn)：透皮吸收　出處：《中國醫(yī)院藥學(xué)雜志》2017年21期 　論文類型：期刊論文

【摘要】：目的:尋找塞來昔布(celecoxib,CLX)凝膠的最佳配方。方法:采用三裂式裂區(qū)設(shè)計,主區(qū)為羥丙基甲基纖維素、海藻酸鈉及卡波姆3種基質(zhì),副處理為透皮劑月桂氮芯卓酮(氮酮)的兩種水平(1.0%和2.0%),亞副處理為透皮劑薄荷醇的兩種水平(0.5%和1.0%),重復(fù)3次實(shí)驗(yàn)。運(yùn)用改良的Franz擴(kuò)散池,選用不同配方塞來昔布制劑作促滲性試驗(yàn),采用HPLC法測定和計算藥物12 h累積釋放量(Q)。結(jié)果:裂區(qū)分析發(fā)現(xiàn)區(qū)組之間并無顯著差異,但各種基質(zhì)之間存在顯著差異;透皮劑氮酮及薄荷醇均對CLX透過皮膚起著非常重要的促進(jìn)作用,氮酮、薄荷醇均與基質(zhì)存在顯著的協(xié)同交互作用;薄荷醇與氮酮之間,以及薄荷醇、基質(zhì)和氮酮三者之間均存在顯著的協(xié)同交互作用。進(jìn)一步的析因設(shè)計的方差分析發(fā)現(xiàn)在以羥丙基甲基纖維素為基質(zhì)的凝膠中,氮酮在促進(jìn)CLX透過皮膚的過程中發(fā)揮主要作用;薄荷醇則對CLX透過皮膚無明顯作用,但氮酮與薄荷醇合用對CLX透過皮膚表現(xiàn)出顯著的協(xié)同增效作用。在海藻酸鈉為基質(zhì)的凝膠中,氮酮、薄荷醇均可顯著促進(jìn)CLX透過皮膚;兩者合用,對CLX透過皮膚表現(xiàn)出顯著的協(xié)同增效作用。在以卡波姆為基質(zhì)的凝膠中,氮酮以及薄荷醇均無顯著促進(jìn)CLX透過皮膚的作用;氮酮與薄荷醇合用也無顯著的協(xié)同或拮抗作用。結(jié)論:本研究結(jié)果提示,塞來昔布凝膠配方以6號(海藻酸鈉+1.0%氮酮和0.5%薄荷醇)為最佳。同時也表明一種化學(xué)物質(zhì)透過皮膚的量,既與其本身的性質(zhì)有關(guān),也與透皮劑的種類及性質(zhì)有關(guān),還與凝膠基質(zhì)的性質(zhì)有關(guān)。
[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.
【作者單位】： 四川省中醫(yī)藥科學(xué)院;四川省人民醫(yī)院;邛崍市醫(yī)療中心醫(yī)院;
【基金】：四川省中醫(yī)藥管理局科研課題(編號:2010-G-093) 四川省衛(wèi)生廳科研基金資助項(xiàng)目(編號:090437)
【分類號】：R943

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