Metformindrug info

Sitagliptin and metformin hydrochloride extended-release tablets for oral use contain two antihyperglycemic medications: sitagliptin and metformin extended-release. Sitagliptin Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Sitagliptin phosphatedrug substance is used to manufacture sitagliptin and metformin hydrochloride extended-release tablets. Sitagliptin phosphate is described chemically as 7-[( R )-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3- a ]pyrazine monophosphate with an molecular formula of C 16 H 15 F 6 N 5 O

H 3 PO 4 and a molecular weight of 505.31. The structural formula is: Sitagliptin phosphate is a white to off-white, crystalline powder and slightly hygroscopic in nature. It is soluble in water, very slightly soluble in anhydrous ethanol and practically insoluble in n-heptane. Metformin Metformin hydrochloride, USP (Imidodicarbonimidic diamide, N, N -dimethyl-, monohydrochloride) is a white crystalline powder with a molecular formula of C 4 H 11 N 5

HCl and a molecular weight of 165.6. Metformin hydrochloride, USP is freely soluble in water, slightly soluble in alcohol and is practically insoluble in acetone, and in methylene chloride. The pK a of metformin hydrochloride, USP is 12.1. The pH of 10 % solution of metformin hydrochloride, USP in purified water is 6.89 ( ̴ 7.0), at the temperature 25°C. The structural formula is as shown: Sitagliptin and Metformin Hydrochloride Extended-Release Tablets Sitagliptin and metformin hydrochloride extended-release tablets are available as bi-convex oval, film-coated tablets containing: 62.03 mg sitagliptin phosphate (equivalent to 50 mg sitagliptin) and 500 mg metformin hydrochloride (sitagliptin and metformin hydrochloride extended-release tablets 50/500). 62.03 mg sitagliptin phosphate (equivalent to 50 mg sitagliptin) and 1000 mg metformin hydrochloride (sitagliptin and metformin hydrochloride extended-release tablets 50/1000). 124.06 mg sitagliptin phosphate (equivalent to 100 mg sitagliptin) and 1000 mg metformin hydrochloride (sitagliptin and metformin hydrochloride extended-release tablets 100/1000). All doses of sitagliptin and metformin hydrochloride extended-release tablets contain the following inactive ingredients: colloidal silicon dioxide, hypromellose, kaolin powder, polyethylene glycol, povidone, propyl gallate, sodium stearyl fumarate. In addition, 50 mg/500 mg tablet contains microcrystalline cellulose. In addition, the film coating for all doses contains the following inactive ingredients: FD&C blue #2/Indigo carmine aluminum lake, carnauba wax, hydroxypropyl cellulose, hypromellose, titanium dioxide. The sitagliptin and metformin hydrochloride extended-release 50 mg/500 mg and 50 mg/1000 mg tablets film coating also contain the inactive ingredient iron oxide yellow. structure1 structure2