Co-Zincretin 50/500/Co-Zincretin 50/1000/Co-Zincretin XR 100/1000 Description

Co-Zincretin 50/500/Co-Zincretin XR 100/1000: Sitagliptin Phosphate + Metformin HCl combines two antihyperglycemic agents with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes: sitagliptin phosphate, a dipeptidyl peptidase 4 (OPP-4) inhibitor; and metformin hydrochloride, a member of the biguanide class.
Sitagliptin Phosphate: Sitagliptin Phosphate is an orally-active, potent and highly selective inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme for the treatment of type 2 diabetes. The DPP-4 enzyme is a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, sitagliptin increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduce hepatic glucose production. The mechanism is unlike the mechanism seen with sulfonylureas; sulfonylureas cause insulin release even when glucose levels are low, which can lead to sulfonylurea-induced hypoglycemia in patients with type 2 diabetes and in normal subjects. Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations. Sitagliptin differs in chemical structure and pharmacologic action from GLP-1 analogues, insulin, sulfonylureas or meglitinides, biguanides, peroxisome proliferator-activated receptor gamma (PPARγ) agonists, alpha-glucosidase inhibitors, and amylin analogues.
Metformin hydrochloride: Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Its pharmacologic mechanisms of action are different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patients with type 2 diabetes or normal subjects (except in special circumstances, see Metformin hydrochloride under Precautions) and does not cause hyperinsulinemia. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease.
Sitagliptin Phosphate + Metformin HCl contains sitagliptin phosphate and metformin hydrochloride. Sitagliptin Phosphate is a white or almost white powder. Soluble in water and N, N-Dimethylfonnamide, slightly soluble in methanol and insoluble in 2-propanol. Sitagliptin Phosphate is chemically designated as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluoromethyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a] pyrazine phosphate (1:1) monohydrate. Its empirical formula is C₁₆H₁₅F₆N₅₀H₃PO₄H₂O and its molecular weight is 523.32.
Metformin Hydrochloride is a white or almost white crystalline powder. Freely soluble in water, slightly soluble in Alcohol, practically insoluble in Acetone and Methylene dichloride. Metformin Hydrochloride is chemically designated as N, N- dimethylbiguanide Hydrochloride. N'-dimethlyguanylguanidine Hydrochloride LA-6023 (Metformin or Metformin Hydrochloride); Metformina, hidrocloruro de; Metforrnini Hydrochloridum. 1, 1-Dimethylbiguanide hydrochloride. Its empirical formula is C₄H₁₁N_5,HCl, and its molecular weight is 165.65.
Co-Zincretin 50/500: Each Film-Coated tablet contains: Sitagliptin Phosphate Monohydrate, USP Eq. to Sitagliptin 50 mg, Metformin Hydrochloride, BP 500 mg.
Sitagliptin Phosphate + Metformin Hydrochloride is a extended release film coated tablets, White colored, elongated shaped, biconvex film coated tablets having one side central breakline & other side plain. It contains the following inactive ingredients: Microcrystalline Cellulose, Maize starch, PVP K-30, Methyl Paraben Sodium, Propyl Paraben Sodium, Purified Water, Sodium Starch Glycolate, Purified Talc, Magnesium Stearate, Colloidal anhydrous silica, Film Coat, Titanium Dioxide, Isopropyl Alcohol & Dichloromethane.
Co-Zincretin 50/1000: Each Film-Coated Tablet contains: Sitagliptin (as phosphate monohydrate) 50 mg, Metformin Hydrochloride 1 g.
White coloured, capsule shaped, biconvex, film-coated tablet, plain on both sides.
Co-Zincretin XR 100/1000: Each Extended Release Film-Coated tablet contains Sitagliptin Phosphate Monohydrate, USP Eq. to Sitagliptin 100 mg, Metformin Hydrochloride, BP 1 g.
Sitagliptin Phosphate + Metformin HCl is a extended release film coated tablets, Red colored, elongated shaped, biconvex extended release, film coated tablets having one side central break line & other side plain. It contains the following inactive ingredients: Microcrystalline Cellulose, Maize starch, PVP K-30, Methyl Paraben Sodium, Propyl Paraben Sodium, Purified Water, Sodium Starch Glycolate, Purified Talc, Magnesium Stearate, Colloidal anhydrous silica, Film Coat, Red oxide Iron, Isopropyl Alcohol & Dichloromethane.