Raw Material Powder 1,1-Dimethylbiguanide hydrochloride (Metformin HCL) CAS: 1115-70-4

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16_副本

Pharmaceutical Raw Materials Anti-Diabetic

1,1-Dimethylbiguanide hydrochloride (Metformin HCl )
Synonyms: 1,1-dimethyl-biguanidhydrochloride;diabefagos;diformin;dimethylbiguanidehydrochloride;Dimethyldiguanidinehydrochloride;gliformin;haurymellin;meguan
Metformin HCL CAS: 1115-70-4
Metformin HCL MF: C4H12ClN5
Metformin HCL MW: 165.62
Metformin HCL EINECS: 214-230-6
Metformin HCL Product Categories:Pharmaceuticals;Miscellaneous Compounds;Aerobic Glycolysis (the Warburg Effect);Cancer Metabolism;Inhibitors and Activators of the AMPK pathway;Inhibitors of Aerobic Glycolysis (the Warburg Effect);Guanidines
Chemical Properties: Crystalline Solid
Metformin HCL Assay:99%
Metformin HCL Standard:USP37/EP7.0
Metformin HCL Usage: An oral hypoglycemic agent,Anti-diabetic and anti-cancer activity.
Metformin HCL Biological Activity: Antidiabetic agent; lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis via activation of the LKB1/AMPK pathway. Displays antiproliferative effects in cancer cell lines.
Metformin HCL Packing:25kg/paper barrel

Absorption coefficient of this product, accurately weighed, dissolved in water and diluted quantitatively per 1ml solution containing 5μ G. According to the spectrophotometric determination of absorbance at 233nm wavelength, the absorption coefficient of 778~818

.Metformin hydrochloride is a biguanide oral hypoglycemic agents, also known as metformin hydrochloride, Glucophage, United Dikang, hypoglycemic effect is weaker than phenformin, the main role is to reduce the A cell glucagon secretion, promote the conversion of glucose to glycogen, has not stimulate insulin secretion from pancreatic β -cell characteristics.

Hypoglycemic mechanism is as follows:

1. Increase the sensitivity of peripheral tissues to insulin, increased insulin -mediated glucose utilization.
2 glucose utilization increase in non -insulin-dependent tissues such as brain, blood cells, kidney medulla, intestine, skin and so on.
3 hepatic gluconeogenesis inhibition effect, reducing hepatic glucose output.
4 inhibited intestinal cell uptake of glucose.
5 Inhibition of cholesterol biosynthesis and storage, reduce blood triglyceride and total cholesterol levels.

Clinically metformin hydrochloride for the treatment of simple diet control are not satisfied with type II diabetes patients, especially with obesity and hyperinsulinemia who use the drug not only hypoglycemic effect, may also have to reduce the weight and hyperinsulinemia effect. For some sulfonylureas may be effective in patients with poor efficacy, such as the sulfonylureas, intestinal glucosidase inhibitors or thiazolidinediones, TZDs hypoglycemic drugs, were better than the results alone. Can also be used in patients with insulin therapy to reduce the amount of insulin.

Adverse effects and precautions:
Biguanide oral hypoglycemic agents can increase glucose utilization of surrounding tissues and inhibit the intestinal absorption of glucose, and inhibit glycogen gluconeogenesis and hepatic glucose output,it is mainly applied to obesity, dyslipidemia, type II diabetes patients. It almost has no hypoglycemic effect for normal persons , 2 to 3 hours after taking for diabetes patients ,glucose decreases significantly.
Commonly used oral hypoglycemic agents include phenformin and metformin hydrochloride.
The incidence of adverse effects of metformin hydrochloride is higher than tolbutamide , common gastrointestinal reactions are anorexia, nausea, vomiting, abdominal pain, diarrhea, occasional metallic taste in the mouth, bad breath, nausea, loss of appetite and diarrhea and other gastrointestinal reactions, sometimes hypoglycemia is visible .
Since the biguanide drugs enhance sugar anaerobic glycolysis, and inhibit glycogen generation, small number of patients may suffer with ketosis or lactic acidosis, which should be particularly vigilant, but metformin effect is weak , adverse reactions are only 1/50 of other biguanides, and it has rapid clearance, there are no accumulation in the liver, it rarely induces lactic acidosis, sometimes there is mild increase in blood lactate. patients with heart, liver, kidney diseases are prone to these adverse reactions, diabetes patients with these types of complications are hanged. It can reduce the absorption of vitamin B12, but it seldom causes anemia. The following cases are contraindications:
1. Pregnant and lactating women, children under 10 years of age, 80 years of age or older.
2. Diabetic ketoacidosis, diabetic hyperglycemic hyperosmolar syndrome, diabetes lactic acidosis.
3. Severe liver and kidney dysfunction, blood urea nitrogen and creatinine higher than normal, hypovolemic shock, heart failure, AMI, in vivo hypoxic condition such as heart failure, pulmonary insufficiency, or any systemic hypoxia circumstances and other serious heart and lung diseases.
4. Severe infection or trauma, major surgery, clinical hypotension , hypoxia and so on.
5. Complications with severe diabetic nephropathy and retinopathy. When there are symptoms,the drug should be immediately discontinued; cimetidine can reduce the renal excretion of metformin hydrochloride, agar types can reduce the absorption of metformin, patients must check liver and kidney function and cardiac ketones regularly.
6. Alcoholics, vitamin B12 and folate deficiency which are not corrected.

 

Application
The product belongs to hypoglycemic agents. It can be used in patients with type diabetes to reduce fasting and postprandial hyperglycemia, HbAlc can be decreased by 1% to 2%, hypoglycemic mechanism of this product may be: I increase the sensitivity of peripheral tissues to insulin, increases insulin-mediated glucose utilization . II increase glucose utilization of non-insulin dependent tissues, such as brain, blood cells, kidney medulla, intestine, skin and the like. III inhibit hepatic gluconeogenesis effect, reduce hepatic glucose output. IV inhibit glucose uptake by intestinal cells.
Indications: For mild diabetes.
Metformin hydrochloride is an anti-diabetic agent, reducing blood glucose levels, and improving insulin sensitivity. Its metabolites (including the inhibition of hepatic gluconeogenesis) is activated through LKB1-AMPK (AMP-activated protein kinase) path.
Hypoglycemic agents, it is used for non-insulin-dependent diabetes. Rat oral LD50 of 1000 mg/kg.

Overview of 1,1-Dimethylbiguanide hydrochloride:

Properties:White crystalls or crystal powder.Melting point is 232 ºC (218-232 ºC).Soluble in water, dissolved in methanol, slightly soluble in ethanol, insoluble in ether and chloroform.Odourless, taste bitter.

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