新型抗癌药物KW 2149（丝裂霉素C的类似物，7-N-[2-[2-(γ-L-谷氨酰胺基)乙基)二硫代)乙基]丝裂霉素C）的测定
Determination of the new anticancer agent KW 2149, 7-N-[2-[2-(gamma-L-glutamylamino)ethyl)dithio)ethyl]mitomycin C, an analogue of mitomycin C.
作者信息
Pattyn G, van Oosterom A T, de Bruijn E A, Tjaden U R
机构信息
Laboratory of Cancer Research and Clinical Oncology, University of Antwerp, Wilrijk, Belgium.
出版信息
J Chromatogr. 1991 Mar 8;564(1):352-4. doi: 10.1016/0378-4347(91)80102-i.
The new mitomycin 7-N-[2-[2-(gamma-L-glutamylamino)ethyl)dithio)ethyl] mitomycin C (KW 2149) (I) proved to be active against a wide variety of experimental tumours. In order to perform pharmacokinetic studies with the new drug in Phase I sessions, a fast and reliable method has been developed based on the data of previous assays for mitomycin C. XAD-2 was preferred for isolation of I from blood plasma. The recovery of I was 50% whereas that of mitomycin C was 85%. Optimal separation was obtained on octadecyl silica columns with methanol-water (45:55, v/v) as mobile phase, while ultraviolet absorbance detection was performed at 375 nm. The assay enabled determination of I in a plasma concentration range of 20-1000 ng/ml using porfiromycin as internal standard.
新型丝裂霉素7 - N - [2 - [2 -（γ - L - 谷氨酰胺基）乙基）二硫代）乙基]丝裂霉素C（KW 2149）（I）被证明对多种实验性肿瘤具有活性。为了在I期试验中对这种新药进行药代动力学研究，基于先前对丝裂霉素C的测定数据开发了一种快速可靠的方法。从血浆中分离I时首选XAD - 2。I的回收率为50%，而丝裂霉素C的回收率为85%。以甲醇 - 水（45:55，v/v）为流动相，在十八烷基硅胶柱上可获得最佳分离效果，同时在375 nm处进行紫外吸光度检测。该测定法能够以卟吩霉素为内标，测定血浆浓度范围为20 - 1000 ng/ml的I。
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