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应用5-氨基乙酰丙酸及其甲酯后大鼠口腔黏膜和皮肤中原卟啉IX的形成动力学

Kinetics of protoporphyrin IX formation in rat oral mucosa and skin after application of 5-aminolevulinic acid and its methylester.

作者信息

Kristiansson Stefan, Juzeniene Asta, Juzenas Petras, Iani Vladimir, Löfgren Lennart, Moan Johan

机构信息

Department of Otolaryngology, Orebro University Hospital, Orebro, Sweden.

出版信息

Photochem Photobiol. 2005 Mar-Apr;81(2):394-7. doi: 10.1562/2004-04-02-RA-132.

DOI:10.1562/2004-04-02-RA-132
PMID:15535733
Abstract

The kinetics of accumulation of protoporphyrin IX (PpIX) after topical application of 5-aminolevulinic acid (ALA) and its methylester (5-aminolevulinic acid methylester [ALA-Me]) was studied on rat oral mucosa. The accumulation of PpIX in mucosa and skin after intravenous injection of ALA and ALA-Me was also studied. The elimination rate of PpIX was dependent on drug and dose as well as on administration route. Application of ALA on rat oral mucosa and skin caused a systemic effect with PpIX building up in remote skin sites not exposed to the drugs. No such systemic effect was seen after application of ALA-Me either in mucosa or on skin. Intravenous injection of the drugs (0.2 g/kg) leads to more fluorescence in the skin than topical application of the drug (20%). For mucosa, the opposite is true. Maximal PpIX fluorescence appeared later after application of high concentrations of the drugs (around 8 h for 5% and 20% wt/wt) than after application of low concentrations (around 3-5 h for 1% and 2% wt/wt).

摘要

在大鼠口腔黏膜上研究了局部应用5-氨基乙酰丙酸(ALA)及其甲酯(5-氨基乙酰丙酸甲酯[ALA-Me])后原卟啉IX(PpIX)的蓄积动力学。还研究了静脉注射ALA和ALA-Me后PpIX在黏膜和皮肤中的蓄积情况。PpIX的消除率取决于药物、剂量以及给药途径。在大鼠口腔黏膜和皮肤上应用ALA会产生全身效应,PpIX在未接触药物的远端皮肤部位蓄积。在黏膜或皮肤上应用ALA-Me后未观察到这种全身效应。静脉注射药物(0.2 g/kg)比局部应用药物(20%)在皮肤中产生更多荧光。对于黏膜,情况则相反。应用高浓度药物(5%和20%重量/重量,约8小时)后比应用低浓度药物(1%和2%重量/重量,约3-5小时)后出现最大PpIX荧光的时间更晚。

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