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庆大霉素C(1)、C(1a)和C(2)组分的色谱分离及其与血清蛋白的个体结合评估。

Chromatographic separation of the C(1), C(1a), and C(2) components of gentamicin and the assessment of their individual binding to serum proteins.

作者信息

Griffiths W C, Belliveau J F, Bensted C L, Calabresi S G, Diamond I

出版信息

J Pharm Sci. 1984 Dec;73(12):1836-7. doi: 10.1002/jps.2600731248.

DOI:10.1002/jps.2600731248
PMID:6527273
Abstract

[3H]gentamicin and [14C]gentamicin samples were purified by Sephadex column chromatography and separated by an HPLC technique into the three major, medicinally active gentamicin components. These separated components were used in equilibrium dialysis studies to determine their percent binding to serum proteins. The bindings of the components were inversely related to concentrations of ionized calcium and magnesium. When dialyzed against a buffer containing physiological concentrations of the divalent cations, the binding of the C(1) component was 2.2 +/- 1.0%, the binding of the C(1a) component was 1.2 +/- 1.9%, and the binding of the C(2) component was 5.0 +/- 2.0%. The percent bindings are not identical and, due to their low values, probably have negligible clinical significance. The radioactive composition and purity of the 3H- and 14C-labeled gentamicin samples differed and these may be important factors in the variance of reported gentamicin bindings.

摘要

[3H]庆大霉素和[14C]庆大霉素样品通过葡聚糖凝胶柱色谱法纯化,并采用高效液相色谱技术分离成三种主要的、具有药用活性的庆大霉素成分。这些分离出的成分用于平衡透析研究,以确定它们与血清蛋白的结合百分比。这些成分的结合与离子化钙和镁的浓度呈负相关。当与含有生理浓度二价阳离子的缓冲液进行透析时,C(1)成分的结合率为2.2±1.0%,C(1a)成分的结合率为1.2±1.9%,C(2)成分的结合率为5.0±2.0%。结合百分比并不相同,并且由于其值较低,可能在临床上没有显著意义。3H和14C标记的庆大霉素样品的放射性组成和纯度不同,这些可能是报道的庆大霉素结合差异的重要因素。

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Chromatographic separation of the C(1), C(1a), and C(2) components of gentamicin and the assessment of their individual binding to serum proteins.庆大霉素C(1)、C(1a)和C(2)组分的色谱分离及其与血清蛋白的个体结合评估。
J Pharm Sci. 1984 Dec;73(12):1836-7. doi: 10.1002/jps.2600731248.
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