单环单萜烯的经皮吸收促进作用及皮肤刺激性。

Drug design and delivery Pub Date : 1990-09-01
H Okabe, Y Obata, K Takayama, T Nagai
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引用次数: 0

摘要

用大鼠和家兔分别研究了环单萜烯的促皮吸收作用和皮肤刺激性。将酮洛芬(KPF)制成含各种环单萜烯的凝胶软膏,应用于大鼠皮肤。环萜类化合物如反式对甲烷和d-柠檬烯的加入显著提高了KPF的血浆浓度,而其他萜类化合物如l-薄荷醇、l-薄荷酮和1,8-桉树脑的加入对KPF的血浆浓度没有显著的提高作用。增强剂的亲脂性似乎是促进KPF通过皮肤渗透的重要因素。d-柠檬烯的增强活性明显高于氮酮。采用Draize评分法评价了环单萜和氮酮类化合物对家兔皮肤的刺激性。当含有2%碳氢化合物的乙醇应用于背部皮肤时,皮肤表面没有变化,尽管在偶氮酮的情况下观察到轻微的水肿和红斑。特别是氮酮和环单萜化合物在红斑形成上有明显的差异。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Percutaneous absorption enhancing effect and skin irritation of monocyclic monoterpenes.

The percutaneous absorption promoting effect and skin irritancy of cyclic monoterpenes were investigated in rats and with rabbits, respectively. Ketoprofen (KPF) was applied to rat skin in gel ointments containing various cyclic monoterpenes. Plasma concentrations of KPF markedly increased with the addition of the hydrocarbons of cyclic monoterpenes such as trans-p-menthane and d-limonene, whereas no significant enhancing effect was observed in the cases of other terpenes such as l-menthol, l-menthone and 1,8-cineole. The lipophilicity of the enhancers seems the important factor in promoting penetration of KPF through the skin. The enhancing activity of d-limonene was found to be much higher than that of Azone. Irritancy of the hydrocarbons of cyclic monoterpenes and Azone to the skin was evaluated using a Draize scoring method with rabbits. No change was observed on the skin surface when ethanol containing 2% of the hydrocarbons was applied to the dorsal skin, though a slight edema and erythema were observed in the case of Azone. In particular, an obvious difference was observed in the erythema formation between Azone and the hydrocarbons of cyclic monoterpenes.

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