API, White or almost white powder.
Molecular formula: C16H15F6N5O·H3PO4·H2O
This product is used in combination with diet control and exercise to improve blood sugar control in patients with type 2 diabetes. When blood glucose control is not good with metformin hydrochloride alone, it can be used in combination with metformin hydrochloride to improve blood glucose control in patients with type 2 diabetes on a diet and exercise basis.
Sigliptin dipeptidyl peptidase 4 (DPP-4) inhibitor can improve blood glucose control by increasing the level of active incretin in type 2 diabetes patients. Intestinal insulinotropic hormones, including glucagon like peptide-1 (GLP-1) and glucose dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day and increase in levels after meals. Intestinal islet stimulating hormone is a part of the endogenous system involved in the physiological regulation of glucose homeostasis. When blood glucose levels are normal or elevated, GLP-1 and GIP can increase pancreatic beta cell synthesis and release insulin through intracellular signaling pathways involving cyclic adenosine monophosphate. In the animal model of type 2 diabetes, GLP-1 or DPP-4 inhibitor treatment can improve the responsiveness of pancreatic β cells to glucose and promote the biosynthesis and release of insulin. As insulin levels increase, the tissue's uptake of glucose increases. In addition, GLP-1 can also inhibit the secretion of glucagon by pancreatic alpha cells. The decrease in glucagon concentration and the increase in insulin levels can reduce liver glucose production, thereby lowering blood glucose levels. The effects of GLP-1 and GIP are glucose dependent. When blood glucose concentrations are low, GLP-1 does not promote insulin release or inhibit glucagon secretion. When glucose levels are higher than normal concentrations, GLP-1 and GIP enhance their ability to promote insulin release. In addition, GLP-1 does not impair the body's normal glucagon release response to hypoglycemia. The activity of GLP-1 and GIP is limited by DPP-4 enzyme, which can rapidly hydrolyze intestinal insulinotropic hormone to produce inactive products. Sitagliptin can prevent DPP-4 from hydrolyzing intestinal insulinotropic hormone, thereby increasing the plasma concentration of active forms of GLP-1 and GIP. By increasing the level of active intestinal insulinotropic hormone, sitagliptin can increase insulin release and reduce glucagon levels in a glucose dependent manner. For type 2 diabetes patients with hyperglycemia, the above changes in insulin and glucagon levels can reduce glycosylated hemoglobin A1c (HbA1c) and lower fasting and postprandial blood glucose levels. The glucose dependent mechanism of action of Sigliptin is different from that of sulfonylurea drugs. Even at low glucose levels, sulfonylurea drugs can increase insulin secretion, thus causing hypoglycemia in type 2 diabetes patients and normal subjects. Sitagliptin is an effective and highly selective DPP-4 enzyme inhibitor that does not inhibit DPP-8 or DPP-9, which are closely related to DPP-4, at therapeutic concentrations.
Individuals allergic to any ingredient in this product are prohibited from using it.
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