Abstract

EVALUATION OF EFFICACY OF TENELIGLIPTIN BY QUANTIFICATION WITH ACTIVE GLUCAGON LIKE PEPTIDE-1 (GLP-1) FROM INDIAN HUMAN PLASMA USING NOVEL BIOANALYTICAL METHOD IN LC- ESI-MS/MS

Pallab Mandal, Soumya Chakraborty, Md. Adil Shaharyar, Rudranil Bhowmik, Arnab Sarkar, Avishek Mandal, Sanmoy Karmakar* and Tapan Kumar Pal*

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Abstract

Teneligliptin is an inhibitor of DPP-4 enzyme by which treated hyperglycemic patient. The main target of this proteonomic study was to evaluation of the efficacy of teneligliptin on inhibition of DPP-4 enzyme. In previous literature several studies depended on quantifying the concentration of DPP-4 enzyme by ELISA method. But in this study inhibition of DPP-4 enzyme by teneligliptin was evaluated by quantification of the active concentration of Glucagon like peptide- 1(GLP-1) by a novel validated LC-MS/MS QTRAP (API-4000) method. Active GLP-1 is an endogenous compound, so before administration of reference preparation, endogenous compound active GLP-1 concentration in human plasma was 31±11 fg/ml and in the case of test preparation 42±11 fg/ml. After treating reference preparation the maximum plasma concentration of active GLP-1 was 330 ± 28.0 fg/ml (Cmax) at 1.05 ±0.18 hr (tmax) and after administration of test product in the fasting state teneligliptin tablet IP 10mg the maximum plasma concentration of active GLP-1 was 141.00 ± 11.00 fg/ml (Cmax) at 1.01 ± 0.00 hr (tmax) then decrease its concentration and again increase it to 71.00 ± 5.10 fg/ml at (Cmax)14.01 ± 0.00 hr (tmax) after administration of a second dose of teneligliptin tablet IP 10mg after 12hrs of first dosing time of administration. This method is highly selective, sensitive, specific, low ion suppressive, highly recovered, validated according to US-FDA and EMA guidelines, and successfully used for quantifying pharmacokinetic parameters of active concentration of peptide and teneligliptin from Indian healthy human plasma.

Keywords: Active-GLP-1 assay, Teneligliptin, Efficacy study, Bioequivalence study, LC-MS/MS QTRAP.