01
Sitagliptin Base 486460-32-6 For Sitagliptin
Product Specification
Appearance: |
White to light yellow crystalline powder |
Identification: |
Infrared absorption、HPLC RT |
Loss on drying： |
≤1.0% |
Chiral impurity： |
≤0.5% |
Related impurity： |
Any individual impurity≤0.3%、Total impurities ≤0.5% |
HPLC assay： |
98.0%~102.0% |
description1
PRODUCT DESCRIPTION
Sitagliptin Base is an intermediate of Sitagliptin, an orally accessible selective DPP4 inhibitor found by optimizing a class of DPP4 inhibitors derived from β-aminoacids. It decreases DPP4 activity after once daily treatment, maintains intact GIP and GLP1 levels in the bloodstream after meals in both acute and long-term tests, and lowers blood sugar levels without appreciably raising hypoglycemia.Because it increases levels of GLP-1 (peptide-1) and GIP (glucose-dependent insulinotropic peptide), two active incretin hormones, sitagliptin phosphate (STG) is used to treat type 2 diabetes by improving glycemic control. When these incretins are activated in β-pancreatic cells, intracellular calcium and cyclic adenosine monophosphate (cAMP) levels rise, which in turn triggers glucose-dependent insulin secretion (2). Dipeptidyl peptidase IV inhibitors are a novel class of hypoglycemic medications that includes this one. The FDA gave STG approval in 2006.
The European Union approved sitagliptin in March 2007 and the U.S. Food and Drug Administration (FDA) approved it in October 2006. Sitagliptin is currently approved for use in 42 countries. It is advised to take 100 mg of the medication once daily, with or without food. When diet and exercise are not enough to control blood glucose levels in patients with type 2 diabetes, it can be used as either monotherapy or as an adjuvant therapy to any of the two other types of oral diabetic medicines, metformin or thiazolidinediones.In April 2007, the FDA approved a combination medication that included sitaglibtin and metformin for the treatment of type 2 diabetes. In a year of clinical trials, sitagliptin improved glycaemic control by reducing fasting and postprandial glucose concentrations.
The levels of glycosylated hemoglobin dropped in a way that was clinically significant as a result. When administered as a monotherapy, sitagliptin 100 mg once day lowers mean HbA1c by 0.6–0.79% (mean difference from placebo). When metformin or pioglitazone are taken together, the average reduction in HbA1c is 0.7% and 0.9%, respectively. Sitagliptin is thought to be weight and lipid neutral.