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Modification of the apparent lipophilicity of steroidal drugs with gamma-cyclodextrin.

作者信息

Cserháti T, Forgács E

机构信息

Hungarian Academy of Sciences, Budapest, Hungary.

出版信息

Eur J Pharm Biopharm. 1998 Sep;46(2):153-9. doi: 10.1016/s0939-6411(97)00171-9.

DOI:10.1016/s0939-6411(97)00171-9
PMID:9795037
Abstract

The interaction between 17 steroidal drugs and gamma-cyclo-dextrin (gamma-CD) was determined by charge-transfer chromatography and the relative strength of interaction was calculated. The relationship between the strength of interaction and the physico-chemical parameters of steroidal drugs was elucidated with principal component analysis. Gamma-CD interacted with each steroidal drug decreasing the apparent hydrophobicity of the guest molecules. Calculations indicated that the interaction between the drugs and gamma-CD is of mixed character: steric, hydrophobic and electronic forces are involved in the complex formation. The marked influence of gamma-CD on the apparent hydrophobicity of drugs suggests that this interaction may modify the biological properties (absorption, uptake, half-life etc.) of drug-gamma-CD complexes resulting in modified efficacy.

摘要

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