Gorsen R M, Weiss A J, Manthei R W
J Chromatogr. 1980 Dec 12;221(2):309-18. doi: 10.1016/s0378-4347(00)84316-9.
Twelve compounds representing procarbazine, seven metabolites, and an internal standard were analyzed by gas chromatography-mass spectrometry on a 3% OV-1 column. Procarbazine and four metabolites were derivatized with acetic anhydride. A sensitive, specific and quantitative assay was established by selected ion monitoring using a synthetic analogue of the drug as an internal standard. The limits of detection were approximately 1 ng/ml of plasma while the limits of quantitation were 10 ng/ml of plasma. Studies of the degradation of procarbazine . HCl in 0.05 M phosphate buffer (pH 7.4) were compared to in vivo studies. At 1 h after incubation of procarbazine . HCl in buffer, the azo and aldehyde metabolites were detected in the highest concentrations representing 27.2% and 20.3% of total drug and metabolites. In the in vivo studies, analyses of rat plasmas indicated that 1 h after an oral dose of procarbazine . HCl, the aldehyde metabolite represented 72% of the total drug and metabolites, and that relatively little of the azo metabolite was present.
采用气相色谱 - 质谱联用仪在3% OV - 1柱上分析了代表丙卡巴肼的12种化合物、7种代谢物和1种内标物。丙卡巴肼和4种代谢物用乙酸酐进行衍生化处理。以该药物的一种合成类似物作为内标物，通过选择离子监测建立了一种灵敏、特异且定量的检测方法。检测限约为血浆1 ng/ml，定量限为血浆10 ng/ml。将丙卡巴肼盐酸盐在0.05 M磷酸盐缓冲液（pH 7.4）中的降解研究与体内研究进行了比较。在缓冲液中孵育丙卡巴肼盐酸盐1小时后，偶氮和醛代谢物的检测浓度最高，分别占总药物和代谢物的27.2%和20.3%。在体内研究中，对大鼠血浆的分析表明，口服丙卡巴肼盐酸盐1小时后，醛代谢物占总药物和代谢物的72%，且偶氮代谢物含量相对较少。
