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新生儿及成人中克林霉素、头孢唑林和头孢拉定的血浆蛋白结合情况(作者译)

[The plasma-protein-binding of Clindamycin Cephazolin and Cephradin in neonates and adults (author's transl)].

作者信息

Kiosz D, Simon C, Malerczyk V

出版信息

Klin Padiatr. 1975 Jan;187(1):71-80.

PMID:1168280
Abstract

In pooled serum of 12 healthy adults and 12 neonates (blood taken from the umbilical cord) the free and protein-bound parts of Cephazolin, Cephradin and Clindamycin were tested by equilibrium dialysis in relation to the concentration of the antibiotic. In the serum of adults at a concentration of 36 mcg/ml the free part of Cephazolin amounted to 16%, at a concentration of 35 mcg/ml the free Cephradin was 87%, at a concentration of 97 mcg/ml the free Clindamycin was 16%. The binding constant k of Cephazolin was 12.0 (rise-constant 0.58), of Cephradin 0.26 and of Clindamycin 15.8 (rise-constant 0.58). When concentration of antibiotics rose, the free part of Clindamycin and Cephazolin increased more than with Cephradin. At a concentration of 30--42 mcg/ml the differences between the sera of adults and neonates were 26.4% with Cephazolin, 3.7% with Cephradin and 3.1% with Clindamycin (concentration 92--97 mcg/ml). In neonates the free part of Cephazolin was 43%, of Clindamycin 19% and of Cephradin 90%. The lower ablumin content in serum of neonates (3.7 g%) does not altogether explain the reduced protein-binding. In neonates a different affinity for binding has to be assumed.

摘要

在12名健康成年人和12名新生儿(取自脐带血)的混合血清中,通过平衡透析法检测了头孢唑林、头孢拉定和克林霉素的游离部分和蛋白结合部分与抗生素浓度的关系。在成年人血清中,头孢唑林浓度为36微克/毫升时,游离部分占16%;头孢拉定浓度为35微克/毫升时,游离部分为87%;克林霉素浓度为97微克/毫升时,游离部分为16%。头孢唑林的结合常数k为12.0(上升常数0.58),头孢拉定为0.26,克林霉素为15.8(上升常数0.58)。当抗生素浓度升高时,克林霉素和头孢唑林的游离部分比头孢拉定增加得更多。在浓度为30 - 42微克/毫升时,成年人与新生儿血清中头孢唑林的差异为26.4%,头孢拉定为3.7%,克林霉素为3.1%(浓度92 - 97微克/毫升)。在新生儿中,头孢唑林的游离部分为43%,克林霉素为19%,头孢拉定为90%。新生儿血清中白蛋白含量较低(3.7克%)并不能完全解释蛋白结合的降低。在新生儿中,必须假定存在不同的结合亲和力。

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