Römsing Susanne, Lindegardh Niklas, Bergqvist Yngve
Dalarna University College, Borlänge, Sweden.
Bioanalysis. 2011 Aug;3(16):1847-53. doi: 10.4155/bio.11.173.
The growing problem of parasites developing resistance to the traditional antimalarial drugs makes the development of new effective and safe drugs crucial. Tafenoquine is a new promising antimalarial drug for prophylaxis and treatment.
A bioanalytical method for the determination of tafenoquine in 100 µl of capillary blood applied onto sampling paper and in 100 µl of plasma has been developed and validated. The Whatman 31 ET Chr paper was treated with 0.6 mol/l tartaric acid to improve the extraction recovery and solid-phase extraction was used for cleanup procedure of the blood samples. Plasma samples were precipitated with methanol. Tafenoquine and internal standard were separated on a Zorbax SB-CN column by reversed-phase LC and detected with fluorescence detection at 262 and 470 nm. The within- and between-day variations were below 10 and 14%, respectively, over the range 50-200 nmol/l for capillary blood on sampling paper and below 6 and 10% for plasma samples. The LLOQ of the method was 50 nmol/l.
The developed method has adequate sensitivity and is highly suitable for clinical studies in dried blood spots and plasma.
寄生虫对传统抗疟药物产生耐药性这一日益严重的问题使得开发新的有效且安全的药物至关重要。他非诺喹是一种用于预防和治疗的有前景的新型抗疟药物。
已开发并验证了一种用于测定涂在采样纸上的100 μl毛细血管血和100 μl血浆中他非诺喹的生物分析方法。用0.6 mol/l酒石酸处理Whatman 31 ET Chr纸以提高提取回收率，并使用固相萃取对血样进行净化处理。血浆样品用甲醇沉淀。他非诺喹和内标在Zorbax SB-CN柱上通过反相液相色谱分离，并在262和470 nm处用荧光检测进行检测。对于采样纸上的毛细血管血，在50 - 200 nmol/l范围内，日内和日间变化分别低于10%和14%，对于血浆样品则分别低于6%和10%。该方法的定量下限为50 nmol/l。
所开发的方法具有足够的灵敏度，非常适合于干血斑和血浆的临床研究。
