Metformin glycinate salt for blood glucose control

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The term “modulate” refers to the treating, prevention, suppression, enhancement or induction of a function or condition. For example, the compounds of the present invention can modulate hyperlipidemia by lowering cholesterol in a human, thereby suppressing hyperlipidemia.

The term “treating” means the management and care of a human subject for the purpose of combating the disease, condition, or disorder and includes the administration of a compound of the present invention to prevent the onset of the symptoms or complications, alleviating the symptoms or complications, or eliminating the disease, condition, or disorder.

As used herein and in the claims, “treating hyperglycemia ” refers to slowing, interrupting, arresting, or stopping the failure to maintain appropriate blood sugar levels in the body, and does not necessarily indicate total elimination of metabolic defects in production and utilization of glucose.

By the term “effective amount” what is meant is an amount which is effective for either prophylactic or therapeutic purposes to prevent or mitigate the failure to maintain appropriate blood sugar levels n the body or reduce blood glucose level in question.

Metformin glycinate is a biguanide with pharmacological properties different from that of metformin chlorydrate (generic drug). The metformin glycinate acts by inhibiting the liberation of hepatic glucose and increasing the peripheral sensitivity to endogenous insulin to promote attachment of insulin in the receptor. This is why we take into consideration an antihyperglycemic agent in as much as the manner prevents the increase in the quantity of glucose. However, the differences between metformin chlorhydrate, metformin glycinate have been demonstrated in the possession of hypoglycemic effect in preclinical research and clinical research, by the decreasing amount of plasma glucose in a direct manner. Although the mechanism of action for which the cause and effect has not yet been defined, it has been seen to be consistent in various studies. In one study, it has been observed that the glycemic curve after acute oral administration of metformin glycinate in rats has pronounced effect on hypoglycemic rats when the medicament was administered, as compared to rats where metformin chlorhydrate was administered. In another study, the toxicity evaluation of metformin glycinate was determined where it was orally administered repeatedly in rats during 28 days, a different dosage as compared with metformin chlorhydrate. With the obtained results, it was concluded that there were no differences in so far as toxicity profile between metformin glycinate and metformin chlorhydrate at high dosage. Although the observed differences in relation to the clinical pathological results demonstrate a severe hypoglycemia suggesting pharmacological effect was exaggerated (excessive) and indicated a pharmacological activity much distinct between the two drugs.

The solid pharmaceutical composition contains pharmaceutical excipients of about 10-50% of one or more combination of microcrystalline cellulose, lactose, dibasic calcium phosphate, dextrose, calcium carbonate, magnesium carbonate, maltodextrin, mannitol, compressed sugar, sorbitol, etc.; disintegrants include about 1-15% of one or more combination of sodium crosscarmellose, crospovidone, starch, pregelatinized starch, etc.

Binders include about 1-15% of one or more of combination of povidone, dextrin, maltodextrin, polymethacrylates, alginate, sodium alginate, carboxymethylcellulose, ethylcellulose, starch, pregelatinized starch, gelatin, gum tragacanth, etc. Glidants include about 0.1-15% of one or more combination of talc, colloidal silicon dioxide, magnesium trisilicate, starch etc.; lubricant is about 0.5-7% of one or more combination of magnesium stearate, zinc stearate, calcium stearate, glycerol monostearate, glycerylpalmitylstearate, polyethyleneglycol, sodium benzoate, sodiumlaurylsulfate, sodium stearyl fumarate, stearic acid, etc.; polymers include about 0.3-5% of one or more combination of methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, ethylcellulose, polymethacrylates, polyvinylalcohol, etc.

Solid pharmaceutical composition preferably contains about 20% anhydrous dibasic calcium phosphate, about 5% povidone, about 5% starch sodium glycolate, about 0.3% colloidal silicon dioxide, about 5% talc, about 1% magnesium stearate, and about 0.7% coating.

The recommended dosage is at least about 1050.6 mg once or twice a day. The dosage range is about 100 mg to about 3.5 g. The dosage of metformin glycinate is adjusted gradually in response to how well it is tolerated and how well the patients blood sugar levels respond to the drug.

The studies specified below are a preferred embodiment of the invention, but are not intended to limit either the compositions to be administered, which may be in the form of a tablet, caplet, gel, paste, powder, prolonged-release granules, capsule, prolonged-release tablet, liquid with buffer agent, effervescent tablets, suspension, syrup, aerosol and others, or the administration route, which may be oral, intravenous injectable, intramuscular injectable, nasal, intraperitoneal, sublingual, etc.