Sensitive analysis and pharmacokinetic study of epalrestat in C57BL/6J mice.

Epalrestat is clinically applied for the management of diabetic peripheral neuropathy, yet its pharmacokinetic properties are not well understood. In this study, a rapid and sensitive LC-MS/MS method was established for assaying epalrestat in bio-samples of mice. The method was validated and it showed a good linearity over the range of 2-5000ng/mL, a precision of less than 12.3%, and recovery and matrix effects of 112.5-123.6% and 87.9-89.5%, respectively. After administration of a single dose of epalrestat administered, the exposure level of AUC0-∞ was positively dose-dependent and the mean Cmax, AUC0-12h, T1/2, and MRT were 36.23±7.39μg/mL, 29,086.5μg/Lh, 1.2h and 1.8h, respectively. Epalrestat was highly exposed in stomach, intestine, liver and kidney, and only a small amount was detected in brain, urine and feces. Multi-dose of epalrestat significantly increased MRT and apparent volume of distribution (Vd) relative to those of a single-dose. Copyright © 2017 Elsevier B.V. All rights reserved.

Citation

Jingqiu Huang, Runbin Sun, Siqi Feng, Jun He, Fei Fei, Haoxue Gao, Yuqing Zhao, Yue Zhang, Huilin Gu, Jiye Aa, Guangji Wang. Sensitive analysis and pharmacokinetic study of epalrestat in C57BL/6J mice. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2017 Jun 15;1055-1056:98-103

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PMID: 28445852

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