Use of zinc tranexamate in the treatment of diabetes

Details Use of zinc tranexamate in the treatment of diabetes Use of zinc tranexamate in the treatment of diabetes

2001-03-07

2002-03-19

Weddington, Kevin E. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heavy metal containing doai

C514S866000

Reexamination Certificate

active

06358999

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to use of a zinc tranexamate compound in the treatment of diabetes. More particularly, it relates to use of a zinc tranexamate compound in the treatment of diabetes as an &agr;-glucosidase inhibitor and also as a drug for treating insulin-resistant type II diabetes.
BACKGROUND OF THE INVENTION
In the past, it had been recommended to treat patients with type II diabetes by the diet and/or exercise therapy to control their blood sugar levels before starting drug therapy. Because the insulin-secreatory function of the patient gradually decreases as the disease proceeds, it is current practice to positively control the blood sugar level of the patients from the early stage of diabetes.
Known therapeutic agents for diabetes include insulin preparations and oral hypoglycemic agents such as sulfonyl ureas (SU). In addition, &agr;-glucosidase inhibitors are of current interest in the treatment of diabetes &agr;-Glucosidase is an enzyme which acts on poly- and oligosaccharides to hydrolyze into their constituent monosaccharides. Administration of an &agr;-glucosidase inhibitor may delay the absorption of glucose through digestive tract by inhibiting the enzyme in vivo.
Known oral hypoglycemic drugs including SU may result in acute hypoglycemic conditions when an excessive dose is administered and exhibit a variety of their own adverse effects. Known &agr;-glucosidase inhibitors may produce high incidence of gastrointestinal side effects and present, therefore, a number of problems upon long term administration. All of the above drugs are not effective in the treatment of insulin-resistant type II diabetes.
Antidiabetics in general are administered for a long term and thus require low incidence of adverse effects. A need exists for a new &agr;-glucosidase-inhibiting antidiabetic drug which is safe and retards elevation of blood sugar level of diabetic patients after taking a meal without affecting their normal blood sugar levels by adequately delaying the absorption of glucose from digestive tracts. It is also desirable to provide a drug which is effective to treat insulin-resistant type II diabetes.
SUMMARY OF THE INVENTION
In one aspect, the present invention provides a method for the treatment of diabetes comprising orally administering a therapeutically effective amount of a zinc tranexamate compound to a patient with diabetes.
In another aspect, the present invention is directed to use of a zinc tranexamate compound in the manufacture of a medicament for treating diabetes in human subjects.
DETAILED DESCRIPTION OF THE INVENTION
Tranexamic acid, chemically trans-1-(aminomethyl)cyclohexanecarboxylic acid, is an antiplasminic hemostatic agent. Two moles of this acid form a stable salt with one atom of zinc, called “zinc tranexamate”. The zinc salt, in turn, forms a water-soluble complex with a physiologically nontoxic organic acid such as acetic, glycolic, lactic, succinic, malic, tartaric, maleic or fumaric acid. As used herein, the term “zinc tranexamate compounds” includes zinc tranexamate either anhydrous or hydrated form and its complex with an organic acid.
Zinc tranexamate compounds were first synthesized and found to have antiinflammatory and antiulcerative activities by Fujimura et al. See, JP-B-0702524 and U.S. Pat. No. 5,506,264. It was not known, however, that either tranexamic acid or zinc tranexamate compounds are effective in the treatment of diabetes.
Suprisingly, we have discovered through a series of animal tests that zinc tranexamate compounds have a delaying effect on the absorption of glucose from digestive tracts by inhibiting &agr;-glucosidase in vivo that leads to remarkable suppression of blood sugar levels in animals with experimental diabetes after loading the animals with a substrate sugar. We have also discovered that insulin resistance in rats with insulin-resistant type II diabetes was ameliorated by the oral administration of a zinc tranexamate compound. Details of the animal tests are given in the following examples in which zinc tranexamate monohydrate (Y-4) was used in the form of a suspension in 0.5% aqueous CMC solution unless otherwise indicated.


REFERENCES:
patent: 5506264 (1996-04-01), Fujimura et al.

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