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Absorption of Topical Tacrolimus (FK506) in vitro through Human Skin: Comparison with Cyclosporin A

 

作者: Antti I. Lauerma,   Christian Surber,   Howard I. Maibach,  

 

期刊: Skin Pharmacology and Physiology  (Karger Available online 1997)
卷期: Volume 10, issue 5-6  

页码: 230-234

 

ISSN:1660-5527

 

年代: 1997

 

DOI:10.1159/000211510

 

出版商: S. Karger AG

 

关键词: Cyclosporin A;Tacrolimus;Skin absorption

 

数据来源: Karger

 

摘要:

Cyclosporin A (CsA) is efficacious in many dermatoses as an oral but not as a topical form, while tacrolimus (FK506) has been shown to be effective in both forms. As inadequate skin absorption has been proposed as the reason for inefficacy of topical CsA, factors contributing to percutaneous absorption of FK506 and CsA were studied. Partitioning of FK506 and CsA between octanol and water, stratum corneum and water, and stratum corneum and isopropyl myristate was determined. Absorption of FK506 and CsA through dermatomed human cadaver skin was determined with in vitro flow-through cells. In partitioning experiments, CsA was more lipo-philic than FK506. Both drugs were seen in comparable amounts in skin layers, but FK506 permeated the skin to a greater extent than CsA.

 

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