This validated method for tolvaptan and its two main metabolites for use in a human pharmacokinetic study has not previously been reported.
An RP-HPLC–MS/MS method for tolvaptan and its two main metabolites in vivo was developed and fully validated.
This method was successfully used to quantify tolvaptan and its two main metabolites in plasma samples from a phase I clinical trial of tolvaptan.
The specificity and sensitivity, the chromatography conditions, and the sample pre-treatment procedure are reported.
Compared to previously published methods, this RP-HPLC–MS/MS method is easier to perform, more rapid and has higher sensitivity.