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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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1
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.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
Cancer Treat Rep. 1979 Aug;63(8):1335-41.
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1
Pharmacokinetics of tauromustine in cancer patients. Phase I studies.
Cancer Chemother Pharmacol. 1989;23(3):176-80. doi: 10.1007/BF00267951.
2
Chemical stability of ecomustine, a new antitumor agent in aqueous and biological media as assessed by high-performance liquid chromatography.通过高效液相色谱法评估新型抗肿瘤药物依考莫司汀在水性和生物介质中的化学稳定性。
Cancer Chemother Pharmacol. 1991;27(4):295-300. doi: 10.1007/BF00685115.