Yun-Bin Zhao, Qing-Ye Yan, Ke Zhang, Ya-Lu Zhang and Heng Zheng
Huazhong University of Science and Technology, China
Posters & Accepted Abstracts: Med Chem (Los Angeles)
An efficient and sensitive method based on liquid chromatography coupled with tandem mass spectrometry (LC�MS/MS) has been developed for the simultaneous determination of meptazinol and its three metabolites, 7-oxomeptazinol (M1), 3-hydroxyethylmeptazinol (M2) and N-desmethylmeptazinol (M3), in human plasma. After enzymolysis and protein precipitation, chromatographic separation within 6.0 minutes was obtained from Welch Ultimate XB-C18 column using gradient elution. Meptazinol-d3 was used for the internal standard and the analytes were simultaneously determined by using the following [M+H]+transitions: m/z 234.2�107.2 for meptazinol, m/z 248.2�107.1 for M1, m/z 250.1�107.1 for M2 and m/z 220.2�107.0 for M3. The calibration curves were prepared in the concentration ranges of 100-100000 ng/mL for meptazinol, 5-5000 ng/mL for M1, 5-500 ng/mL for M2 and 50-20000 ng/mL for M3. The relative errors ranged from -6.85% to 3.33%, -5.40% to 4.30%, -5.80% to 2.80% and -4.27% to 8.89% for meptazinol, M1, M2 and M3, respectively. This method has been successfully applied to the determination of meptazinol and its metabolites in plasma of eight healthy volunteers who had a single oral administration of 400 mg hydrochloride meptazinol capsule.
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