从色谱行为推导异恶唑基青霉素活性代谢物的物理化学性质
Physico-chemical properties of the active metabolites of the isoxazolylpenicillins as deduced from their chromatographic behaviour.
作者信息
Thijssen H H
出版信息
Arzneimittelforschung. 1978;28(7):1065-7.
Reversed-phase chromatography of the active metabolites of the isoxazolylpenicillins revealed that the metabolites of oxacillin, cloxacillin, and dicloxacillin have the same fractional increase in hydrophilicity. The metabolite of flucloxacillin showed a much lesser decrease in lipid solubility. Regarding the relationship between the free-energy related hydrophobicity parameter pi and structure, it is concluded that the biotransformation of the isoxazolylpenicillins results in the same structural alteration of oxacillin, cloxacillin, and dicloxacillin. Flucloxacillin is handled differently by the drug metabolizing systems.
异恶唑基青霉素活性代谢产物的反相色谱分析表明，苯唑西林、氯唑西林和双氯西林的代谢产物在亲水性方面具有相同的分数增加。氟氯西林的代谢产物在脂溶性方面的降低要小得多。关于与自由能相关的疏水性参数π与结构之间的关系，可以得出结论，异恶唑基青霉素的生物转化导致苯唑西林、氯唑西林和双氯西林发生相同的结构改变。药物代谢系统对氟氯西林的处理方式不同。
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