Metformin hydrochloride
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Metformin hydrochloride
structure -
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CAS No:
1115-70-4
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Formula:
C4H11N5.ClH
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Chemical Name:
Metformin hydrochloride
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Synonyms:
Imidodicarbonimidic diamide,N,N-dimethyl-,hydrochloride (1:1);Biguanide,1,1-dimethyl-,monohydrochloride;Imidodicarbonimidic diamide,N,N-dimethyl-,monohydrochloride;Biguanide,1,1-dimethyl-,hydrochloride;Metformin hydrochloride;N,N-Dimethylbiguanide hydrochloride;1,1-Dimethylbiguanide hydrochloride;Meguan;N1,N1-Dimethylbiguanide hydrochloride;Diabefagos;Glucophage;Glyformin;LA 6023;Dabex;Denkaform;Dextin;Diabetmin;Diabex;Apophage;Benofomin;Diformin Retard;Dimefor;Fornidd;Geamet;Glucaminol;Glucofago;Glucomet;Glucomine;Glucoform;Glucomin;Gluconil;Glucophage 850;Glucophage Forte;Glucophage-Mite;Glucophage Retard;Gludepatic;Glufor;Gluformin;Glumeformin;Glumin;Glupermin;Glyciphage;Glycon;Metforal;Metomin;Miformin;Orabet;Siamformet;Walaphage;Diaformin;Diformin;Glyceriphage;Diabetosan;Dialon;Glucophage XR;N,N-Dimethylbiguanidinium chloride;Apo-Metformin;Brot;Glumetza;Glifage;Glucophage SR;Melbin;N,N-Dimethylbiguanidine monohydrochloride;Glucoformin;Riomet;Glumin XR;Metgluco;Neodipa;Diabetmim;FORTAMET;Obimat-SR;15537-72-1;56258-19-6;144377-16-2
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Categories:
Active Pharmaceutical Ingredients > Hormones and the Endocrine System
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CAS No:
Description
Metformin (hydrochloride) is an FDA approved first-line drug for the treatment of type 2 diabetes. Metformin decreases hepatic glucose production, mostly through a mild and transient inhibition of the mitochondrial respiratory-chain complex 1.
Characteristics
88.99000
1.05850
crystalline solid
232 °C
224.1ºC at 760 mmHg
89.3ºC
In water, 1.06X10+6 mg/L (miscible) at 25 deg C (est)
Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature 2 - 8 deg C. Storage class (TRGS 510): Non Combustible Solids. /Metformin hydrochloride/
0.0929mmHg at 25°C
Safety Information
NONH for all modes of transport
3
R22; R36/38
S26-S36
DU1800000
Xn
Stable under recommended storage conditions. /Metformin hydrochloride/
P305 + P351 + P338
H302-H315-H319
Metformin hydrochloride Use and Manufacturing
500mg of metformin free base was dissolved in 3Om^ of acetone, and then 280^ of concentrated hydrochloric acid was added, and stirred for 2 hours at room temperature. The resulting crystal was filtered and washed with acetone, and then Was charged into a 300 L autoclave100kg of dicyandiamide and 120kg of dimethylamine hydrochloride were added, and 300kg of cyclohexanol was added. The stirring speed was 45r / min, the vacuum degree of the reaction kettle was adjusted to 0.08MPa, heated to 140 and reacted for 3h. And the crude product is recrystallized with ethanol, filtered and dried to obtain metformin hydrochloride.1, 000 Kg of diphenyl ether was charged into the reaction tank, and 250 kg of dimethylamine hydrochloride and 240 kg of dicyandiamide were uniformly added thereto while stirring.After the feeding is completed, the temperature of the reaction tank is raised to 195-200°C, and the temperature is maintained for 1 hour. Insulation is completed, slowly cooled to about 50 °C and filtered, washed twice with isoamyl alcohol 250Kg at 100 °C, and dried at 130-135 °C.The crude product was recrystallized with 95percent ethanol, the amount of ethanol was about 3 times that of the crude product, and the mixture was stirred and heated to reflux so that the crude product was completely dissolved, naturally cooled to room temperature, and allowed to stand for 5 hours.White needle-like crystals were precipitated, filtered, and dried at 100°C for 12 hours to obtain 418.7 kg of metformin hydrochloride, a purity of 99.79percent, and a dicyandiamide content of less than 0.005percent (a Pharmacopoeia limit of ≤ 0.04).1 Kg of 2-cyanoguanidine and 1.15 Kg of Dimethyl amine hydrochloride were added to 2 Kg of n-butanol in a 5 L glass flask. The flask was equipped withcooling water condenser and the flask was allowed to reflux for 22 h. The resulting reaction mass was cooled to ambient temperature, preferably 10-110°C and filtered. Dried the obtained solid at 50°75°C, to get Pure Metformin hydrochloride (1.9 Kg)
1. An oral hypoglycemic agent
2. Anti-diabetic and anti-cancer activity
Computed Properties
Molecular Weight:165.62
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:2
Exact Mass:165.0781231
Monoisotopic Mass:165.0781231
Topological Polar Surface Area:91.5
Heavy Atom Count:10
Complexity:132
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes
Price Analysis
Drug Function and Efficacy
This product is a hypoglycemic drug. This product can reduce fasting and postprandial hyperglycemia in patients with type 2 diabetes, and HbAlc can be reduced by 1% to 2%. The mechanism of this product in lowering blood sugar may be: 1. Increase the sensitivity of peripheral tissues to insulin and increase insulin-mediated glucose utilization; 2. Increase the utilization of glucose by non-insulin-dependent tissues, such as the brain, blood cells, renal medulla, intestines, skin, etc.; 3. Inhibit hepatic gluconeogenesis and reduce hepatic glucose output; 4. Inhibit intestinal wall cells from taking up glucose; 5. Inhibit the biosynthesis and storage of cholesterol and reduce blood triglyceride and total cholesterol levels. Unlike the effect of insulin, this product has no effect on promoting fat synthesis and no obvious hypoglycemic effect on normal people, but has a good therapeutic effect on type 2 diabetes.
Registered Holders
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MERCK SANTE SAS
Active
United States
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Uquifa Mexico, S.A. de C.V.
Active
Japan
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Farmhispania S.A.
Active
Japan
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