A highly sensitive LC-MS/MS method for the determination and quantification of a recently identified -nitrosamine impurity in the sitagliptin phosphate monohydrate active pharmaceutical ingredient. | LitMetric
Chemical Process Research and Development, Zhejiang Tianyu Pharmaceutical Co., Ltd, Taizhou, 318020, China.
Published: January 2023
AI Article Synopsis
Article Abstract
A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was used for the quantification of 7-nitroso-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-]pyrazine (NTTP) in the sitagliptin phosphate monohydrate active pharmaceutical ingredient. Chromatographic separation was achieved using an Agilent-ZORBAX SB-C18 column, with 0.01 mol L ammonium formate in water as mobile phase A and acetonitrile as mobile phase B in gradient elution mode at a 0.4 mL min flow rate. Quantification of impurities was carried out using triple quadrupole mass detection with electrospray ionization in the multiple reaction monitoring mode. The method was fully validated with good linearity over the concentration range of 0.098-0.925 ppm of the sitagliptin phosphate monohydrate test concentration for NTTP. The correlation coefficient obtained in each case was >0.998. The recoveries were found to be satisfactory over the range between 80.0 and 120.0% for NTTP. The developed method was able to quantitate NTTP at a concentration level of 0.98 ng mL (0.098 ppm with respect to 10 mg mL sitagliptin phosphate monohydrate).
Mucosal Health and Immunology Laboratory (MHIL), Center for Natural and Human Science, Federal University of ABC, Santo André, São Paulo, Brazil; Institute of Biomedical Sciences, University of São Paulo, São Paulo, São Paulo, Brazil. Electronic address:
Macrophages play a crucial role in regulating the immune response both in normal conditions and during inflammation, and sitagliptin, a diabetes drug, has shown potential anti-inflammatory effects.
This study investigated how sitagliptin affects macrophage polarization, finding that it enhances the M2 macrophage phenotype while reducing pro-inflammatory markers like TNF-α.
Additionally, sitagliptin treatment impacted mitochondrial function in M2 macrophages, leading to lower energy production and reduced ability to engulf particles.
Introduction: A slower adoption rate of fixed dose combinations (FDC) in diabetes management is partly due to insufficient data. This study evaluates the safety and efficacy of an FDC of dapagliflozin + sitagliptin + metformin hydrochloride extended release (XR), compared to a dual FDC of sitagliptin + metformin hydrochloride XR among patients with type 2 diabetes mellitus (T2DM) with poor glycemic control when treated with metformin monotherapy.
Methods: A total of 274 patients with T2DM were randomized (1:1) to either arm X, receiving FDC of dapagliflozin (10 mg) + sitagliptin (100 mg) + metformin hydrochloride XR (1000 mg) (Dapa + Sita + Met) tablets, or arm Y, receiving sitagliptin phosphate (100 mg) + metformin hydrochloride XR (1000 mg) (Sita + Met) tablets, and treated for 16 weeks.
Background: The regulatory neuropeptide Y (NPY) is implicated in anxiety and post-traumatic stress disorder (PTSD)-related behaviors. NPY exerts its effects through 5 receptor subtypes, with Y1 and Y2 receptors being predominantly expressed in the rat brain. Activation of Y1 by full-length NPY1-36 induces anxiolytic effects, whereas Y2 binds truncated peptides, eliciting region-specific anxiogenic responses.
Impaired function of the retinal neurovascular unit (NVU) is an early event in diabetic retinopathy (DR). It has been previously shown that topical delivery of the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin can protect against diabetes-mediated dysfunction of the retinal NVU in the db/db mouse. The aim of the present study was to examine whether sitagliptin could prevent the DR-like lesions within the NVU of the new non-diabetic model of DR, the Trpv2 knockout rat (Trpv2).
Introduction: Type II Diabetes mellitus (T2DM) patients often do not achieve glycemic control with oral hypoglycemic agents (OHAs). There are two main approaches to address this challenge: transitioning to a triple OHA regimen, or adding Insulin to the existing dual OHA regimen.
Aim: This study aimed to compare the efficacy of adding Insulin to dual OHAs (Sitagliptin + Metformin) against adding a third OHA to Sitagliptin + Metformin in achieving glycemic control among patients with uncontrolled T2DM.
