拉替拉韦与血浆蛋白结合的特性分析。
Characterization of binding of raltegravir to plasma proteins.
机构信息
Assistance Publique, Hôpitaux de Paris, Hôpital Bicêtre, Hôpitaux Universitaires Paris-Sud, Service de Pharmacie Clinique, Paris, France.
出版信息
Antimicrob Agents Chemother. 2013 Oct;57(10):5147-50. doi: 10.1128/AAC.00625-13. Epub 2013 Jul 15.
Abstract
The objective of this study was to characterize raltegravir (RAL) binding to albumin and alpha-1-acid glycoprotein (AAG). Unbound and bound RAL were separated by ultrafiltration. The association constant (Ka) was estimated by a graphical method. In HIV-infected patients, the average plasma protein binding is 76%. RAL did not bind to AAG but bound to nonsaturable, low-affinity albumin sites with an n (number of sites) · Ka product of 9.8 × 10(2) liters/mol. A pH increase of 0.2 U led to a 2% increase in the bound fraction.
摘要
本研究旨在描述拉替拉韦（RAL）与白蛋白和α-1-酸性糖蛋白（AAG）的结合情况。通过超滤分离游离和结合的 RAL。通过图形法估算结合常数（Ka）。在感染 HIV 的患者中，平均血浆蛋白结合率为 76%。RAL 不与 AAG 结合，但与非饱和、低亲和力的白蛋白结合部位结合，n（结合部位数）·Ka 产物为 9.8×10（2）升/摩尔。pH 值增加 0.2 U 导致结合分数增加 2%。
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