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KMID : 0369820160460050495
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Jorunal of Korean Pharmaceutical Sciences
2016 Volume.46 No. 5 p.495 ~ p.504
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High performance liquid chromatographic determination of YJC-10592, a new chemokine receptor 2 (CCR-2) antagonist, in biological samples
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Du Eun-Sin
Moon Hong-Sik
Lim Soo-Jeong
Chang Sun-Young
Kim So-Hee
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Abstract
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YJC-10592, a new chemokine receptor 2 (CCR-2) antagonist, was newly synthesized for the treatment of asthma and atopic dermatitis. To evaluate the pharmacokinetic characteristics of YJC-10592, a high-performance liquid chromatographic (HPLC) method was developed for the determination of YJC-10592 in rat plasma, urine, and tissue homogenates, using YJC-10450 as an internal standard. The mobile phase was a gradient of acetate buffer (50 mM, pH 3.0) in acetonitrile at a flow rate of 1.0 mL/min. Chromatograms were monitored by an ultraviolet detector at 230 nm. The retention times for YJC-10592 and the internal standard were 8.0 and 6.3 min, respectively, and the lower limits of quantification (LLOQ) for YJC-10592 in rat plasma and urine were 0.05 and 0.2 μg/mL, respectively. The intra- and inter-assay precisions (coefficients of variation, CVs) were generally low (below 11.4 %) for rat plasma and urine samples. The accuracies (relative errors) ranged from 94.2 to 108 %. No interferences from endogenous substances were found. YJC-10592 was stable in rat whole blood but unstable in the liver homogenate. An initial pharmacokinetic study was performed in Sprague?Dawley rats and demonstrated that YJC-10592 has a half-life of 86.8 min and wide tissue distribution. In summary, this HPLC method can be applied to future preclinical and clinical evaluation of YJC-10592.
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KEYWORD
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YJC-10592, Chemokine receptor 2, CCR-2, HPLC, Pharmacokinetics
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