Dua V K, Kar P K, Sarin R, Sharma V P
Malaria Research Centre, Ranipur, Hardwar, India.
J Chromatogr B Biomed Appl. 1996 Jan 12;675(1):93-8. doi: 10.1016/0378-4347(95)00357-6.
A reversed-phase HPLC method using acetonitrile-methanol-1 M perchloric acid-water (30:9:1:95, v/v) at a flow-rate of 1.5 ml/min on a mu-Bondapak C18 column with UV detection at 254 nm was developed for the separation of primaquine, its major metabolite carboxyprimaquine and other metabolites such as N-acetylprimaquine, 4-hydroxyprimaquine, 5-hydroxyprimaquine, 5-hydroxy-6-methoxyprimaquine, demethylprimaquine and 6-methoxyprimaquine, and also other antimalarials. The calibration graphs were linear in the range 0.025-100 micrograms/ml for primaquine and 4-1000 micrograms/ml for carboxyprimaquine. The within-day and day-to-day coefficients of variation averaged 3.65 and 6.95%, respectively, for primaquine and 3.0 and 7.52%, respectively for carboxyprimaquine in plasma. The extraction recoveries for primaquine and carboxyprimaquine were 89 and 83%, respectively. The mean carboxyprimaquine concentration was much higher in plasma and blood cells of Plasmodium vivax patients than that in plasma from healthy subjects. The carboxyprimaquine level was also higher in blood cells than plasma whereas the primaquine concentration was the same in both cases.
建立了一种反相高效液相色谱法，采用乙腈 - 甲醇 - 1M高氯酸 - 水（30:9:1:95，v/v），流速为1.5 ml/min，在μ - Bondapak C18柱上，于254 nm处进行紫外检测，用于分离伯氨喹及其主要代谢产物羧基伯氨喹以及其他代谢产物，如N - 乙酰伯氨喹、4 - 羟基伯氨喹、5 - 羟基伯氨喹、5 - 羟基 - 6 - 甲氧基伯氨喹、去甲基伯氨喹和6 - 甲氧基伯氨喹，以及其他抗疟药。伯氨喹的校准曲线在0.025 - 100微克/毫升范围内呈线性，羧基伯氨喹的校准曲线在4 - 1000微克/毫升范围内呈线性。血浆中伯氨喹日内和日间变异系数平均分别为3.65%和6.95%，羧基伯氨喹分别为3.0%和7.52%。伯氨喹和羧基伯氨喹的提取回收率分别为89%和83%。间日疟患者血浆和血细胞中的羧基伯氨喹平均浓度远高于健康受试者血浆中的浓度。血细胞中的羧基伯氨喹水平也高于血浆，而两种情况下伯氨喹的浓度相同。
