An HPLC-MS/MS method for quantitation of trelagliptin and application in a comparative pharmacokinetic study.

A sensitive HPLC-MS/MS approach was established to quantify trelagliptin and explore the pharmacokinetic characteristics in rats for up to 7 days. Meanwhile, the pharmacokinetic differences of trelagliptin were investigated for the first time. The ion pairs of 358.2→341.2 for trelagliptin and 340.3→116.1 for alogliptin (internal standard) were detected in positive mode. Trelagliptin displayed a good linearity in the range of 4-4000 ng/ml (r = 0.9997) with a mean recovery rate of 86.9-94.1%. Compared with normal groups, the T1/2, apparent volume of distribution, area under the curve and bioavailability in model rats were significantly increased while the apparent plasma clearance decreased. The approach is proved to be straightforward and appropriate for quantitation of trelagliptin and application in pharmacokinetics studies.