Preparation of fagopyritols and uses therefor

Details Preparation of fagopyritols and uses therefor Preparation of fagopyritols and uses therefor

2000-05-25

2002-12-10

Gitomer, Ralph (Department: 1623)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

C514S025000, C514S053000, C514S061000, C514S866000, C536S004100, C536S123100, C536S123130, C536S128000

Reexamination Certificate

active

06492341

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to fagopyritols and to methods for using fagopyritols.
BACKGROUND OF THE INVENTION
Diabetes mellitus is a major global health problem which is recognized by the World Health Organization to be reaching epidemic proportions. It is now the fourth leading cause of death in most developed countries and a disease that is increasing rapidly in countries undergoing industrialization. Estimates of worldwide diabetes prevalence have increased from 30 million in 1985 to more than 100 million in 1994. Diabetes mellitus is a disease caused by defective carbohydrate metabolism and characterized by abnormally large amounts of glucose in the blood and urine. Diabetes mellitus can eventually damage the eyes, kidneys, heart, and limbs, and can endanger pregnancy.
Diabetes mellitus is usually classified into two types. Type I, or insulin-dependent diabetes mellitus (“IDDM”), formerly called juvenile-onset diabetes because it occurs primarily in children and young adults, has been implicated as one of the autoimmune diseases. Rapid in onset and progress, it accounts for about 10 to 15 percent of all cases. Type II, or non-insulin-dependent diabetes mellitus (“NIDDM”), formerly called adult-onset diabetes, is usually found in persons over 40 years old and progresses slowly. Often it is not accompanied by clinical illness in its initial stages and is detected instead by elevated blood or urine glucose levels.
Diabetes is considered a group of disorders with multiple causes, rather than a single disorder. The human pancreas secretes a hormone called insulin that facilitates the entry of glucose into tissues of the body and its utilization, thus providing energy for bodily activities. In a person with diabetes, however, the entry of glucose is impaired, a result either of a deficiency in the amount of insulin produced or of altered target cells. Consequently, sugar builds up in the blood and is excreted in the urine. In the Type I diabetic, the problem is almost always a severe or total reduction in insulin production. In the Type II diabetic, the pancreas often makes a considerable quantity of insulin, but the hormone is unable to promote the utilization of glucose by tissues.
With adequate treatment most diabetics maintain blood-sugar levels within a normal or nearly normal range. This permits them to live normal lives and prevents some long-term consequences of the disease. For the Type I diabetic with little or no insulin production, therapy involves insulin injections. For Type II diabetics, most of whom are at least moderately overweight, therapy is based on diet control, weight reduction, and exercise. Weight reduction appears partially to reverse the condition of insulin resistance in the tissues. If a Type II patient's blood-sugar level is still high, the physician may add insulin injections to the treatment regimen. In many cases, the need for insulin injections is not due to a deficiency in insulin but, instead, due to the patient's reduced ability to utilize insulin efficiently because of a deficiency of galactosamine D-chiro-inositol, an insulin mediator.
Besides the discomfort associated with its administration by injection, the problem of controlling the dose of insulin also exists. The hypoglycemia produced by an insulin overdose may lead to tremors, cold sweat, piloerection, hypothermia, and headache, accompanied by confusion, hallucinations, bizarre behavior, and, ultimately, convulsions and coma.
Therefore, it would be advantageous to control a diabetic's blood-sugar level without resort to insulin injections. The present invention is directed to providing such control.
SUMMARY OF THE INVENTION
The present invention relates to an isolated Fagopyritol A1, an isolated Fagopyritol A3, and an isolated Fagopyritol B3.
The present invention is also directed to a composition comprising two or more of Fagopyritol A1, Fagopyritol A3, Fagopyritol A3, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D-chiro-inositol. The composition comprises at least one isolated Fagopyritol A1, isolated Fagopyritol A3, or isolated Fagopyritol B3.
The present invention also relates to a substantially pure fagopyritol selected from the group consisting of Fagopyritol A1, Fagopyritol A3, and Fagopyritol B3.
In another aspect, the present invention relates to a method for preparing a material selected from the group consisting of Fagopyritol A1, Fagopyritol A3, Fagopyritol B3, and a mixture thereof. Buckwheat is contacted with a solvent under conditions effective to produce a crude extract. The crude extract contains non-fagopyritol materials and one or more fagopyritols selected from the group consisting of Fagopyritol A1, Fagopyritol A3, and Fagopyritol B3. The non-fagopyritol materials are then separated from the one or more fagopyritols.
The isolated fagopyritols of the present invention can be used in a pharmaceutical composition which also includes a pharmaceutical carrier. This pharmaceutical composition or, alternatively, the substantially pure fagopyritols of the present invention or the isolated fagopyritols of the present invention can be administered to a patient to treat diabetes.


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