Effect of cyclic monoterpenes on percutaneous absorption in the case of a water-soluble drug (diclofenac sodium).

Drug design and delivery Pub Date : 1990-10-01
Y Obata, K Takayama, H Okabe, T Nagai
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Abstract

The promoting effect of cyclic monoterpenes on the percutaneous absorption of diclofenac sodium (DFS), a water-soluble drug, from gel ointments was investigated in rats. Of five cyclic monoterpenes examined, l-menthol was most effective. Plasma concentrations of diclofenac (DF) increased with increasing amounts of l-menthol in the gel ointment. L-menthol had no effect on the solubility and partition coefficient of DFS, suggesting that the thermodynamic nature of DFS in the formulation was not greatly affected. Plasma concentrations of DF arising from application of ointments containing varying amounts of the terpene were predicted from found pharmacokinetic parameters and the steady-state flux of DFS obtained from in vitro permeation experiments. Experimentally determined plasma concentration of DF agreed well with the predictions, indicating that steady-state flux in vitro well reflects percutaneous absorption in vivo.

环单萜烯对水溶性药物(双氯芬酸钠)经皮吸收的影响。
研究了环单萜对大鼠凝胶软膏中水溶性药物双氯芬酸钠(DFS)经皮吸收的促进作用。在所检测的五种环单萜中,l-薄荷醇最有效。血浆双氯芬酸(DF)浓度随着凝胶软膏中l-薄荷醇含量的增加而增加。l -薄荷醇对DFS的溶解度和分配系数没有影响,说明该配方对DFS的热力学性质影响不大。应用含有不同量萜烯的软膏引起的DF的血浆浓度根据发现的药代动力学参数和从体外渗透实验中获得的DFS的稳态通量进行预测。实验测定的血浆DF浓度与预测结果吻合良好,表明体外稳态通量能很好地反映体内经皮吸收。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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