Combined effect of cyclic monoterpenes and ethanol on percutaneous absorption of diclofenac sodium.

Combined effect of cyclic monoterpenes and ethanol on percutaneous absorption of diclofenac sodium.
复制标题

环状单萜和乙醇对双氯芬酸钠经皮吸收的联合作用。

DOI:
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发表时间:
1991
期刊:
Drug design and discovery
影响因子:
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通讯作者:
Tsuneji Nagai
Tsuneji Nagai
中科院分区:
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文献类型:
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作者:
Y. Obata;K. Takayama;Y. Machida;Tsuneji Nagai

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研究了环单萜类化合物和乙醇对双氯芬酸钠(DFS)凝胶软膏透皮吸收的影响。凝胶软膏中乙醇的浓度对萜烯类化合物的增强活性有显著影响。在较低浓度的乙醇(20%)下,观察到1,8-桉叶素的效果最好。另一方面,当乙醇用量较大(40%)时,d-柠檬烯表现出较强的活性。经方差分析,1,8-桉树脑和L-薄荷脑对DFS的透皮吸收有显著的协同效应。双氯芬酸(DF)游离形式与凝胶软膏配伍后,透皮吸收显著降低。透皮吸收的减少与配方中游离形式的DF使凝胶软膏的pH值降低密切相关。
The combined effect of cyclic monoterpenes and ethanol on the percutaneous absorption of diclofenac sodium (DFS) from gel ointments was investigated in vivo in rats. The enhancing activity of terpenes was significantly affected by the concentration of ethanol formulated in the gel ointments. At a lower concentration of ethanol (20%), 1,8-cineole was observed to be the most effective. On the other hand, d-limonene showed strong activity when the large amount of ethanol was formulated (40%). A synergistic effect between terpenes and ethanol on the percutaneous absorption of DFS was significantly observed in cases of 1,8-cineole and l-menthol using an analysis of variance (ANOVA). When the diclofenac (DF) free form was formulated in gel ointment, the percutaneous absorption was significantly reduced. The reduction of the percutaneous absorption was closely related to the decrease in pH of the gel ointment owing to the free form of DF which was formulated.