Investigation of the mechanism of flux across human skin in vitro by quantitative structure-permeability relationships.
Eur J Pharm Sci
; 7(4): 325-30, 1999 Mar.
Article
em En
| MEDLINE
| ID: mdl-9971916
ABSTRACT
Permeability coefficients for 114 compounds across excised human skin in vitro were taken from Kirchner et al. Forty-seven descriptors were calculated encompassing the relevant physicochemical parameters of the compounds. Quantitative structure-permeability relationships (QSPRs) were developed using least-squares regression analysis. A two-parameter QSPR, describing the permeability coefficients (Kp) across excised skin, was obtained log Kp=0.772 log P -0.0103 Mr - 2.33 where log P is the logarithm of the octanol-water partition coefficient and Mr is molecular mass. This equation indicates that percutaneous absorption is mediated by the hydrophobicity and the molecular size of the penetrant. Comparison with a QSPR based on penetration across a synthetic (polydimethylsiloxane) membrane suggests that the mechanisms of drug flux across polydimethylsiloxane membranes and excised human skin are significantly different.
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Base de dados:
MEDLINE
Assunto principal:
Pele
/
Absorção Cutânea
Limite:
Humans
Idioma:
En
Ano de publicação:
1999
Tipo de documento:
Article