ABSTRACT

‘Gliptins’ is the nickname given to a group of anti-diabetic medicines-DPP-4 inhibitors, such as sitagliptin, vildagliptin, sexagliptin, linagliptin, alogliptin and teneligliptin, which are used with metformin for combination therapy of type 2 diabetes mellitus. Advantages of this combined therapy are low risks of hypoglycemia and weight gain compared with other classes of anti-diabetic drugs. In the present study efforts, were made to develop and validate a bioanalytical method for simultaneous estimation of metformin and teneligliptin in human plasma by LC-MS/MS with an application to quantification of plasma samples obtained from the comparative pharmacokinetic studies on healthy human volunteers. The developed method for simultaneous determination and quantification of teneligliptin and metformin in human plasma was also validated as per the US-FDA guidelines. The validation parameters were found to be within the specified regulatory limits, hence the method acceptable. The present method had a short run time (3.5min) and easy extraction process. Therefore, developed method was found to be simple, specific, highly selective, sensitive and reproducible. This was applied for the analysis of volunteer plasma samples obtained from comparative pharmacokinetic study. On the basis of comparison of AUC0-t, the relative bioavailability of test preparation was found to be 97.64% and 91.37% for teneligliptin and metformin, with respect to that of the reference preparation.