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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。

Chemical stability of ecomustine, a new antitumor agent in aqueous and biological media as assessed by high-performance liquid chromatography.

作者信息

el Abed I, Roger P, Gosse C, Atassi G, Gouyette A

机构信息

Laboratoire de Pharmacologie Clinique (URA 158 CNRS, U140 INSERM), Institut Gustave-Roussy, Villejuif, France.

出版信息

Cancer Chemother Pharmacol. 1991;27(4):295-300. doi: 10.1007/BF00685115.

Abstract

Ecomustine, or CY233 (NSC-609224), is a new water-soluble nitrosoureido sugar derived from acosamine. A high-performance liquid chromatographic assay (HPLC) developed to quantify the unchanged drug in aqueous solutions and biological specimens enabled us to study the chemical stability as a function of pH, light, and temperature. In buffered aqueous solutions, the kinetics of degradation of CY233 is a first-order process. The log k-pH profile demonstrated hydroxide ion-catalyzed solvolysis. The drug is most stable at pH 4, more stable than some other nitrosoureas in 5% glucose (t1/2, 62-67 h) and in 0.9% isotonic saline (t1/2, 25-37 h) solutions. Based on these findings, blood samples should be collected in cold tubes (4 degrees C) containing citrate buffer (pH 4) and all manipulations should be protected from heat and light.

摘要

生态莫司汀,即CY233(NSC - 609224),是一种源自阿考胺的新型水溶性亚硝基脲糖。所开发的一种用于定量水溶液和生物样本中未变化药物的高效液相色谱测定法(HPLC),使我们能够研究其作为pH、光照和温度函数的化学稳定性。在缓冲水溶液中,CY233的降解动力学是一级过程。log k - pH曲线表明存在氢氧根离子催化的溶剂解作用。该药物在pH 4时最稳定,在5%葡萄糖溶液(半衰期,62 - 67小时)和0.9%等渗盐溶液(半衰期,25 - 37小时)中比其他一些亚硝基脲更稳定。基于这些发现,血液样本应收集在含有柠檬酸盐缓冲液(pH 4)的冷试管(4℃)中,并且所有操作都应避免受热和光照。

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