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The aim of this study is to investigate the pharmacokinetics, bioavailability and urinary excretion of scopolin and its metabolite scopoletin in rat. A LC-MS/MS method for simultaneous determination of scopolin and scopoletin in rat biomatrices was developed and validated over the rage of 5.0-2000 ng/mL. Chromatographic separation was carried out on a Hypersil GOLD C18 column with acetonitrile and 0.1% formic acid in water as mobile phase with gradient elution. Detection was performed in the positive ionization and selected reaction monitoring mode. The intra- and inter- batch precision and accuracy, extraction recovery and matrix effect, stability of scopolin and scopoletin were well within the acceptable limits of variation. There was no gender-related difference in pharmacokinetic profiles of scopolin. There were significant differences in AUC, T and Cl/F of scopoletin between the male and female rats (p < 0.05). The bioavailability of scopolin was exceptionally low. The maximal excretion rates were 7.61 μg/h and 7.15 μg/h for scopolin and 31.68 μg/h and 25.58 μg/h for scopoletin in male and female rats, respectively. The LC-MS/MS method was successfully applied to the pharmacokinetic, bioavailability and urinary excretion studies of scopolin and its metabolite scopoletin following single administration of scopolin to rats.
This article was published in the following journal.
Name: Biomedical chromatography : BMC
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