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1-(2-氯乙基)-3-[1-(5'-对硝基苯甲酰基-2',3'-异亚丙基)-α,β-D-呋喃核糖基]-1-亚硝基脲(RFCNU)的稳定性及初步药代动力学研究,RFCNU是一种非免疫抑制性亚硝基脲

Stability and preliminary pharmacokinetic studies of 1-(2-chloroethyl)-3-[1-(5'-paranitrobenzoyl-2',3'-isopropylidene)-alpha, beta-D-ribofuranosyl]-1-nitrosourea (RFCNU), a nonimmunosuppressive nitrosourea.

作者信息

Lemoine R, Gouyette A

出版信息

Cancer Treat Rep. 1979 Aug;63(8):1335-41.

PMID:38907
Abstract

Using high-performance liquid chromatography, the stability of RFCNU was monitored as a function of pH in aqueous buffers at 37 degrees C and as a function of temperature in plasma. The kinetics of degradation of RFCNU are apparently first-order. The log kappa-pH profile demonstrated the hydroxyl ion-catalyzed solvolysis and a maximum stability around pH 3.0. This analytic assay was reliable for quantitating intact RFCNU in biologic fluids. After administration of 400 mg of RFCNU orally to a female patient, no intact drug was excreted in the urine and plasma levels were very low.

摘要

使用高效液相色谱法,在37℃的水性缓冲液中监测RFCNU的稳定性与pH的关系,以及在血浆中监测其稳定性与温度的关系。RFCNU的降解动力学显然是一级的。log kappa-pH曲线表明存在氢氧根离子催化的溶剂解作用,且在pH 3.0左右具有最大稳定性。该分析方法对于定量生物流体中的完整RFCNU是可靠的。在一名女性患者口服400 mg RFCNU后,尿液中未排出完整药物,血浆水平非常低。

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