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2-氯-2'-脱氧腺苷(克拉屈滨)在健康受试者和白血病患者体内的蛋白结合情况。

Protein binding of 2-chloro 2'-deoxyadenosine (cladribine) in healthy subjects and in patients with leukaemia.

作者信息

Albertioni F, Herngren L, Juliusson G, Liliemark J

机构信息

Department of Clinical Pharmacology, Karolinska Hospital, Stockholm, Sweden.

出版信息

Eur J Clin Pharmacol. 1994;46(6):563-4. doi: 10.1007/BF00196117.

DOI:10.1007/BF00196117
PMID:7995327
Abstract

The plasma protein binding of 2-chloro-2'-deoxyadenosine (CdA) at 37 degrees C was studied by ultrafiltration in 5 healthy volunteers, in 11 patients with haematological malignancies and in purified protein preparations. In the patients, the binding of CdA to plasma proteins was 25.0% and in healthy subjects it was 21.1%. In a solution of human serum albumin (40 g.l-1), 24.3% CdA was bound, but less than 5% was bound in a solution of alpha 1-acid-glycoprotein (0.7 g.l-1). No dependence of binding on the concentration of CdA was found within a range 25-1000 nmol.l-1. In conclusion, due to its limited binding to plasma proteins, any change in the binding of CdA is unlikely to have a major influence on its pharmacological effect.

摘要

通过超滤法,在5名健康志愿者、11名血液系统恶性肿瘤患者以及纯化蛋白制剂中研究了2-氯-2'-脱氧腺苷(CdA)在37℃时与血浆蛋白的结合情况。在患者中,CdA与血浆蛋白的结合率为25.0%,在健康受试者中为21.1%。在人血清白蛋白溶液(40 g·l⁻¹)中,24.3%的CdA被结合,但在α1-酸性糖蛋白溶液(0.7 g·l⁻¹)中,结合率不到5%。在25 - 1000 nmol·l⁻¹范围内,未发现结合情况与CdA浓度有关。总之,由于CdA与血浆蛋白的结合有限,其结合情况的任何变化都不太可能对其药理作用产生重大影响。

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本文引用的文献

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On the bioavailability of 2-chloro-2'-deoxyadenosine (CdA). The influence of food and omeprazole.关于2-氯-2'-脱氧腺苷(CdA)的生物利用度。食物和奥美拉唑的影响。
Eur J Clin Pharmacol. 1993;44(6):579-82. doi: 10.1007/BF02440863.
2
Cladribine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in haematological malignancies.克拉屈滨。对其血液系统恶性肿瘤的药效学、药代动力学特性及治疗潜力的综述。
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