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[14C]-左旋薄荷醇在皮肤中的吸收、分布及代谢

[Absorption, distribution and metabolism of [14C]-levomenol in the skin].

作者信息

Hahn B, Hölzl J

机构信息

Institut für Pharmazeutische Biologie, Fachbereich Pharmazie und lebensmittelchemie der Philipps-Universität, Marburg/Lahn.

出版信息

Arzneimittelforschung. 1987 Jun;37(6):716-20.

PMID:3663271
Abstract

The purpose of the present investigations was to study the cutaneous absorption of sesquiterpenic alcohol, the major active principle of chamomile. For these investigations 14C-labelled levomenol ((-)-6-methyl-2-(4-methyl-3-cyclohexen-1-yl)-5-hepten-2-ol; (-)-alpha-bisabolol) was prepared by biochemical incorporation of [14C]-acetate into the molecule. 5 h after topical application of the radiolabelled substance onto nude mice half of the radioactivity was found in the skin. The other part was measured in tissue and organes. 90% of this radioactivity was analysed as intact levomenol. To demonstrate the distribution of the substance in the skin a part of this tissue was cutted into horizontal slices by a cryotome. From the slices autoradiograms were produced. The densitometric measuration showed that there was a fast penetration of levomenol into the skin. 5 h after the topical application the substance was displaced from outermost to innermost areas. From these results a fast cutaneous absorption and a long therapeutical effect of the antiphlogistic and spasmolytic levomenol in the skin can be expected.

摘要

本研究的目的是研究洋甘菊的主要活性成分倍半萜醇的皮肤吸收情况。为了进行这些研究,通过将[14C] - 乙酸盐生物化学掺入分子中制备了14C标记的左旋薄荷醇(( - ) - 6 - 甲基 - 2 - (4 - 甲基 - 3 - 环己烯 - 1 - 基) - 5 - 庚烯 - 2 - 醇;( - ) - α - 红没药醇)。将放射性标记物质局部应用于裸鼠5小时后,在皮肤中发现了一半的放射性。另一部分在组织和器官中进行了测量。该放射性的90%被分析为完整的左旋薄荷醇。为了证明该物质在皮肤中的分布,将一部分皮肤组织用冷冻切片机切成水平切片。从这些切片制作了放射自显影片。密度测量显示左旋薄荷醇可快速渗透到皮肤中。局部应用5小时后,该物质从最外层区域转移到最内层区域。从这些结果可以预期,具有抗炎和解痉作用的左旋薄荷醇在皮肤中具有快速的皮肤吸收和长期的治疗效果。

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