Preclinical pharmacokinetic evaluation and metabolites identification of methyl salicylate-2-O-beta-D-lactoside in rats using LC-MS/MS and Q-TOF-MS methods

摘要

Methyl salicylate-2-O-beta-D-lactoside (MSL) is a natural salicylate derivative from the traditional Chinese medicine of Gaultheria yunnanensis (Franch.) Rehder (G. yunnanensis). As a non-steroidal anti-inflammatory drug (NSAID), MSL exerts a significant anti-arthritis effect but hardly has any gastrointestinal toxicity. In this paper, the pharmacokinetics, distribution, excretion and identification of MSL and its metabolites are described following rat oral and intravenous administration. The biological samples were quantified by UPLC-MS/MS and the metabolites in urine and feces were identified by using Q-TOF-MS. These results will support future investigations leading to clinical development of this drug. (C) 2015 Elsevier B.V. All rights reserved.