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经皮吸收:体内实验

Percutaneous absorption: in vivo experiments.

作者信息

Albery W J, Hadgraft J

出版信息

J Pharm Pharmacol. 1979 Mar;31(3):140-7. doi: 10.1111/j.2042-7158.1979.tb13456.x.

Abstract

The percutaneous absorption of esters of nicotinic acid has been studied in vivo in man. The time for erythema to be produced has been measured both when the ester is applied continuously and in 'pulse' experiments when the ester is removed before the erythema develops. The results show that the erythema is produced long before steady state diffusion across the epidermis is established and the penetration of methyl nicotinate is characterized by D/l2 = 2.3 X 10(-4)s-1 where D is the diffusion coefficient and l the thickness of the barrier. Results using glycerol water mixtures in the external phase show that the route of penetration for methyl nicotinate is through the interstitial channels and not through the keratinized cells. Data for absorption from various creams and ointments (Barrett et al 1964) show that the route is independent of the nature of the external phase. Steady state data for the absorption of salicylic acid and carbinoxamine through the abdominal skin of guinea-pigs (Arita et al 1970) show that the route of penetration does not change as the experiment proceeds. Data for the absorption of other substances (Michaels et al 1975) also fit the interstitial route.

摘要

已在人体中对烟酸酯的经皮吸收进行了体内研究。在连续涂抹酯类时以及在“脉冲”实验(即在红斑出现前去除酯类)中,均测量了产生红斑的时间。结果表明,在表皮建立稳态扩散之前很久就会产生红斑,且烟酸甲酯的渗透特征为D/l2 = 2.3×10(-4)s-1,其中D为扩散系数,l为屏障厚度。在外相中使用甘油水混合物的结果表明,烟酸甲酯的渗透途径是通过间质通道而非角质化细胞。来自各种乳膏和软膏的吸收数据(巴雷特等人,1964年)表明,该途径与外相的性质无关。水杨酸和卡比沙明通过豚鼠腹部皮肤吸收的稳态数据(有田等人,1970年)表明,随着实验进行,渗透途径不会改变。其他物质吸收的数据(迈克尔斯等人,1975年)也符合间质途径。

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