Lee S, Casteel D A, Fleckenstein L
The University of Iowa, College of Pharmacy, Iowa City 52242, USA.
J Chromatogr B Biomed Sci Appl. 1997 Dec 19;704(1-2):181-5. doi: 10.1016/s0378-4347(97)00424-6.
Diethylcarbamazine (DEC, 1-diethylcarbamyl-4-methylpiperazine) is an antiparasitic piperazine derivative used in the treatment of lymphatic filariasis. DEC-N-oxide is a major metabolite in humans which has antifilarial activity. Gas chromatographic analysis of DEC in plasma can be complicated by the presence of the metabolite, since the thermally unstable DEC-N-oxide is converted to a material which coelutes with DEC under the conditions of the analysis. We now report a method to separate DEC-N-oxide from DEC in plasma using solid-phase extraction with subsequent gas chromatographic analysis using a nitrogen specific detector. 1-Diethylcarbamyl-4-ethylpiperazine (E-DEC) was the internal standard. The standard curve of DEC is linear in the range of 10 to 200 ng/ml. The limit of detection is 4 ng/ml. Reproducibility at 10, 100 and 200 ng/ml concentration points of the standard curve gives coefficients of variation of 6.1%, 7.8% and 1.6%, respectively. Recovery following solid-phase extraction is 99.3% for DEC and 94.8% for the internal standard. This sensitive and specific analytical method is suitable for pharmacokinetic studies of DEC.
乙胺嗪（DEC，1-二乙氨基甲酰基-4-甲基哌嗪）是一种抗寄生虫哌嗪衍生物，用于治疗淋巴丝虫病。DEC-N-氧化物是人体中的主要代谢产物，具有抗丝虫活性。血浆中DEC的气相色谱分析可能会因该代谢产物的存在而变得复杂，因为热不稳定的DEC-N-氧化物会转化为一种在分析条件下与DEC共洗脱的物质。我们现在报告一种使用固相萃取从血浆中分离DEC-N-氧化物与DEC的方法，随后使用氮特异性检测器进行气相色谱分析。1-二乙氨基甲酰基-4-乙基哌嗪（E-DEC）为内标。DEC的标准曲线在10至200 ng/ml范围内呈线性。检测限为4 ng/ml。标准曲线在10、100和200 ng/ml浓度点的重现性分别给出变异系数为6.1%、7.8%和1.6%。固相萃取后的回收率，DEC为99.3%，内标为94.8%。这种灵敏且特异的分析方法适用于DEC的药代动力学研究。
