METHOD AND COMPOSITIONS FOR PREVENTION AND/OR TREATMENT OF DIABETES AND GLUCOSE MODULATION

Abstract: Compositions and methods for preventing and/or treating diabetes and glucose modulation are provided. The composition comprises conjugated linoleic acid and at least one of ginseng and chromium. Methods of using the composition are also provided.

Description: S P E C I F I C A T I O N TITLE METHOD AND COMPOSITIONS FOR PREVENTION AND/OR TREATMENT OF DIABETES AND GLUCOSE MODULATION BACKGROUND OF THE INVENTION The present invention generally relates to the treatment of disease states. More specifically, the present invention relates to the prevention and/or treatment of diabetes and/or the modulation of blood glucose levels. Diabetes mellitus (diabetes) is a syndrome characterized by hyperglycemia resulting from impaired insulin secretion and/or effectiveness. The syndrome is associated with the risk of diabetic ketoacidosis or nonketotic hyperglycemic- hyperosmolar coma as well as a group of late complications including retinopathy, nephropathy, artherosclerotic coronary and peripheral arterial disease, and peripheral and autonomic neuropathies. Diabetes has diverse genetic, environmental and pathogenic origins. See Merck Manual, 16th Ed., pp 1106- 1107. Diabetes is classified based on certain clinical criteria, e.g., the presence or absence of a propensity to diabetic ketoacidosis, as well as on ancillary criteria used to segregate specific pathogenic forms of diabetes. Specifically, diabetics are classified into insulin dependent diabetes (Type I) and non-insulin dependent diabetes (Type 11). Merck Manual, id. As a syndrome, diabetes is a chronic disease that has no cure. It affects approximately 16 million people in the United States alone and ranks as the sixth leading cause of death by disease. The estimated 16 million people who have diabetes in the United States includes over 5 million that have not yet been diagnosed with the disease. Not only is diabetes one of the leading causes of death in the United States, it is also a major cause of blindness and kidney disease. The estimated cost of treating diabetes approaches $100 billion dollars. Type II diabetes accounts for approximately 90 to 95% of diabetes. It is characterized by two primary defects: insulin resistance; and/or impaired pancreatic β-cell function, either delayed or inadequate insulin synthesis or release. Managing Type π diabetes by diet, exercise, and monitoring blood glucose levels with appropriate medications can potentially restore normal life expectancy. In treating and/or controlling at least Type II diabetes, typically the first avenue chosen is dietary restriction. However, diet has been found to be rarely effective in gaining complete control of hyperglycemia. Thus, many Type II diabetics take drugs to control their diabetes. The current drugs on the market are expensive and have undesirable effects. Nearly 40%) of Type II diabetics take sulphonylurea drugs, e.g., glipizide, which stimulates the release of insulin, but also causes individuals to gain weight as they control glycemia. Metformin a class of Biguanide drugs, causes nausea, gastrointestinal discomfort, diarrhea, leaves a metallic taste in the mouth leading to anorexia, and cannot be used by individuals with kidney disease. Another drug, Resulin had been used by 500,000 people, but recently pulled from the market by the F.D.A. because of the liver toxicity and approximately 60 attributable deaths. Thiazolindinediones is another class of anti- diabetic drugs. Therefore, there is a need for new methods and/or compositions for treating diabetes and/or controlling hyperglycemia and blood glucose levels. SUMMARY OF THE INVENTION The present invention relates to methods and/or compositions for controlling blood glucose levels, hyperglycemia, and/or diabetes. The methods and compositions of the present invention can be utilized alone or as a dietary supplement. To this end, the present invention provides a method for controlling blood glucose levels, comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. In an embodiment, approximately 0.1 to about 15 grams per day of conjugated linoleic acid is administered. In an embodiment, approximately 0.1 mg to about 1.0 mg per day of chromium is administered. In an embodiment, approximately 1.0 mg to about 9000 mg per day of ginseng is administered. In an embodiment, the conjugated linoleic acid is either a pure isomer of octadecadienoic acid, or a mixture of octadecadienoic acid isomers selected from the group consisting of: cis-8, cis-10; cis-8, trans-10; trans-8, cis-10; trans-8, trans- 10; cis-9, cis-11; cis-9, trans-11; trans-9, cis-11; trans-9, trans-11; cis-10, cis-12; cis-9, trans-12; trans-9, cis-12; trans-10, trans-12; cis-11, cis-13; cis-11, trans-13; trans-11, cis-13; trans-11, trans-13 octadecadienoic acid; metabolites thereof, including but not limited to 18:3 cis-6, cis-9, trans-11; 18:3 cis-6, trans-10, cis-12; 18:3 cis-8, trans-12, cis-14; 20:3 cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, trans-12, cis-14; as well as precursors or derivatives thereof. In an embodiment, the composition includes a flavor. In an embodiment, the composition includes an artificial sweetener. In an embodiment, the composition is in pill form. In an embodiment, the composition includes both chromium and ginseng. In another embodiment of the present invention, a method of treating diabetes is provided. The method comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. In an embodiment, approximately 0.1 to about 15 grams per day of conjugated linoleic acid is administered. hi an embodiment, approximately 0.1 mg to about 1.0 mg per day of chromium is administered. In an embodiment, approximately 1.0 mg to about 9000 mg per day of ginseng is administered. In an embodiment, the composition includes both chromium and ginseng. The present invention also provides a composition comprising conjugated linoleic acid, chromium, and ginseng. In a still further embodiment of the present invention, a method of treating hyperglycemia is provided. The method comprises the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. In an embodiment, approximately 0.1 to about 15 grams per day of conjugated linoleic acid is administered. In an embodiment, approximately 0.1 mg to about 1.0 mg per day of chromium is administered. In an embodiment, approximately 1.0 mg to about 9000 mg per day of ginseng is administered. In an embodiment, the composition includes both chromium and ginseng. In yet a further embodiment, the present invention provides a method of reducing the risk of diabetes or hyperglycemia in a susceptible patient. The method comprises the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. In a still further embodiment of the present invention, a method of reducing the risk of diabetes is provided. The method comprises the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng to a patient at risk of developing diabetes. Accordingly, an advantage of the present invention is to provide an improved method for preventing or treating diabetes. A further advantage of the present invention is to provide a composition for preventing or treating diabetes. Still further, an advantage of the present invention is to provide an improved method and composition for maintaining healthy blood sugar levels. Another advantage of the present invention is to provide a product for modulating glucose levels. An additional advantage of the present invention is to provide a dietary supplement for maintaining healthy glucose levels. Moreover, an advantage of the present invention is to provide a composition and method for normalizing hyperglycemia. Still, another advantage of the present invention is to provide a dietary supplement for increasing insulin sensitivity. A further of the present invention is to provide a method and composition for lowering hyperinsulinemia. Additional features and advantages of the present invention are described in and will be apparent from the detailed description of the presently preferred embodiments. DETAILED DESCRIPTION OF THE PRESENTLY PREFERRED EMBODIMENTS The present invention provides improved methods and compositions for the treatment of diabetes, hyperglycemia, and the modulation of glucose levels. Pursuant to the present invention, treatments and compositions are provided for modulating blood glucose levels, lowering hyperglycemia, as well as hyperinsulinemia, and preventing or treating diabetes. The compositions of the present invention can be a pharmaceutical product or component thereof, over-the- counter product, and/or dietary supplement, functional or medical food or component thereof. Pursuant to the present invention, a composition is provided containing mixtures of conjugated linoleic acid, and at least one of chromium and ginseng. It has been found that this combination provides synergistic assistance in reducing or normalizing plasma glucose levels and increasing insulin sensitivity. As noted above, the product can be provided in a pharmaceutical product e.g., pill or emulsion, dietary supplement, or an over-the-counter product, as well as a functional or medical food, or component thereof. The product is believed to have specific application to hyperglycemic individuals, pre-diabetic and Type II diabetics, reducing the individual's plasma glucose levels and providing a better insulin response. Pursuant to the present invention, the composition and method can be used to treat diabetes. In this regard, the composition can control hyperglycemia and increase insulin sensitivity. The composition may also decrease glycosylated hemoglobin. All of these are metabolic factors that eventually lead to blindness, kidney disease, and reduce life expectancy in the diabetic population. The ingredients that are used in the compositions of present invention are preferably all naturally occurring substances or derived therefrom; the active ingredients are all naturally occurring substances or derived therefrom. As compared to prior treatments and compositions, the present invention provides a less expensive alternative with no foreseeable side effects. Pursuant to the present invention, the method and composition comprises administering conjugated linoleic acid, and at least one of ginseng e.g., American Ginseng extract (panax quinquefolium), and chromium. If desired, the composition can include non-active ingredients and/or agents such as flavors, artificial sweeteners, excipients, etc. This product is intended to provide a physiologically based means to aid in maintaining normal plasma glucose levels and provide a normal insulin response. Conjugated linoleic acid is believed to be absorbed efficiently into the body in a manner similar to that of other fatty acids, e.g., linoleic acid. The safety of conjugated linoleic acid has been demonstrated in detailed toxicological assessments. It is believed that conjugated linoleic acid is safe for human consumption. The inventors believe that conjugated linoleic acid has favorable effects on glucose homeostasis. Conjugated linoleic acid administration alone is believed to be associated with normalization of glucose metabolism. Further, conjugated linoleic acid is believed to restore insulin sensitivity. It is believed these effects may be related to conjugated linoleic acid's influence on steroid hormone receptors. Conjugated linoleic acid acts similar to a class of antidiabetic drugs, thiazolidinediones, which are potent insulin sensitizers thought to activate peroxisome proliferator-activated receptors. The striking anti-diabetic properties of conjugated linoleic acid appear to be linked to conjugated linoleic acid - activation of PPARγ. The conjugated linoleic acid of the present invention can comprise a variety of compositions such as those set forth in U.S. Patent No. 5,986,116, the disclosure of which is incorporated herein by reference. As noted above, in addition to conjugated linoleic acid, the composition of the present invention includes ginseng and chromium. Ginseng has been used as a therapeutic agent for a couple thousand years. In this regard, it is included in national pharmacopoeias of Austria, China, France, Germany, Japan, Switzerland, and Russia. In various cultures, its therapeutic indications include a wide range of health applications. No significant adverse affects or health risks have been noted with ginseng except with massive overdoses which may induce sleeplessness, hypertomia, and edema. Ginseng appears to significantly reduce post-prandial glycemia in diabetic subjects taking ginseng before meals. The mechanism by which ginseng lowers blood glucose is unknown. However, a couple possible hypotheses have been presented. First, based on two different observations, it has been suggested that ginseng may possibly slow digestion and decrease carbohydrate absorption. A second hypothesis is that ginseng increases Glucose Transporter 2 which can increase glucose uptake in cells. This effect may be mediated by nitric oxide. Additionally, ginseng may directly modulate insulin secretion possibly via nitric oxide. Chromium has long been recognized as a necessity for proper human nutrition. The estimated safe and adequate dietary intake of chromium has been estimated at 50-200 ug per day for adults. The dietary ingestion of chromium in most industrialized nations generally falls short of recommended levels. Chromium regulates carbohydrate and lipid metabolism. Normal dietary intake of chromium in humans is often less than the adequate daily dietary intake. Chromium deficiency may be promoted by increasing its loss through physiological stressors such as physical trauma, acute exercise, lactation, and consuming a diet high in simple sugars. Insufficient chromium intake is associated with signs and symptoms similar to diabetes. It is believed that chromium's mode of action potentiates insulin either by an effect on insulin dependent factors, or by maintaining these functions with less insulin, or a combination of both. Pursuant to the present invention, compositions are provided comprising conjugated linoleic acid and at least one of chromium and ginseng. The compositions can take a variety of forms, for example, pill, powder or emulsion. It is believed this composition provides a synergistic effect. A method of providing treatment to diabetics, as well as reducing hyperglycemia, modulating glucose levels, maintaining healthy glucose levels, and increasing susceptibility to insulin is provided. In an embodiment of the present invention a composition is provided comprising as the active ingredients approximately: 67 to 99 % by weight conjugated linoleic acid; 0 to 1 % by weight chromium; and 0 to 33 % by weight ginseng. Preferably, the form of chromium is chromium chloride. Preferably, the form of ginseng is American Ginseng. By way of example and not limitation, examples of the present invention are as follows: Product Example No. 1 Tablets containing conjugated linoleic acid/American ginseng powder/chromium. It is envisioned that two tablets will be taken with each meal as a typical dose. Each dose of two tablets contain: conjugated linoleic acid powder 500 mg American ginseng (root powder) 700 mg chromium as chromium chloride 0.10 mg The tablets will include the following excipients and flavorings: magnesium stearate, silicone dioxide, croscarmelose sodium, stearic acid, microcrystalline cellulose, calcium phosphate, aqueous base film coat. Product Example No. 2 Tablets containing conjugated linoleic acid/American ginseng extract/chromium. It is envisioned that two tablets will be taken with each meal as a typical dose. Each dose of two tablets contain: conjugated linoleic acid powder 970 mg American ginseng (25% extract) 28 mg chromium as chromium chloride 0.10 mg The tablets will include the following excipients and flavorings: magnesium stearate, silicone dioxide, croscarmelose sodium, stearic acid, microcrystalline cellulose, calcium phosphate, aqueous base film coat. Product Example No. 3 Capsules containing conjugated linoleic acid/American ginseng extract/chromium. It is envisioned that two capsules will be taken with each meal as a typical dose. Each dose of two capsules contain: conjugated linoleic acid oil 500 mg American ginseng (25% extract) 28 mg chromium as chromium chloride 0.10 mg By way of example and not limitation, contemplative examples of the present invention are as follows: Contemplative Example No. 1 In order to control diabetes in a Type II patient, the product of the present invention would be administered daily to provide: 20 mg/kg/day conjugated linoleic acid to 100 mg/kg/day conjugated linoleic acid, 1 g/day Ginseng to 2 g/day Ginseng (as powder) (or 100 to 200 mg/day as 25% extract), and 0.2 mg/day chromium to 0.4 mg/day chromium. It is thought that these levels help control diabetes in a Type II patient. Contemplative Example No. 2 As a dietary supplement to prevent the onset of Type II diabetes, the product of the present invention would be administered daily to provide: 20 mg/kg/day conjugated linoleic acid to 100 mg/kg/day conjugated linoleic acid, 1 g Ginseng/kg/day to 2 g Ginseng/kg/day (as powder) (or 100 to 200 mg as 25%> extract), and 0.15mg chromium/day to 0.3 mg chromium/day. It is thought that these levels may prevent the onset of diabetes in certain susceptible individuals. Contemplative Example No. 3 In order to increase insulin sensitivity the product of the present invention would be administered daily to provide: 20 mg/kg/day conjugated linoleic acid to 60 mg/kg/day conjugated linoleic acid, 1 g Ginseng/day to 2 g Ginseng/ day (as powder) (or 100 to 200 mg/day as 25%o extract), and O.lmg/day chromium to 0.2 mg/day chromium. These levels may increase insulin sensitivity in those individuals requiring same. Contemplative Example No. 4 In order to maintain healthy plasma glucose levels, the product of the present invention would be administered daily to provide: 20 mg/kg/day conjugated linoleic acid to 60 mg/kg/day conjugated linoleic acid, 1 g/day Ginseng to 2 g/day Ginseng (as powder) (or 100 to 200 mg/day as 25%) extract), and O.lmg/day chromium to 0.2 mg/day chromium. It is thought that these levels would help maintain healthy plasma glucose levels in susceptible individuals. It should be understood that various changes and modifications to the presently preferred embodiments described herein will be apparent to those skilled in the art. Such changes and modifications can be made without departing from the spirit and scope of the present invention and without diminishing its intended advantages. It is therefore intended that such changes and modifications be covered by the appended claims.

Claims: WE CLAIM: 1. A method for controlling blood glucose levels comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. 2. The method of Claim 1 wherein approximately 0.1 to about 15 grams per day of conjugated linoleic acid is administered. 3. The method of Claim 1 wherein approximately 0.1 mg to about 1.0 mg per day of chromium is administered. 4. The method of Claim 1 wherein approximately 1.0 mg to about 3000 mg per day of ginseng is administered. 5. The method of Claim 1 wherein the conjugated linoleic acid is selected from the group consisting of: either a pure isomer of octadecadienoic acid, a mixture of octadecadienoic acid isomers, cis-8, cis-10; cis-8, trans-10; trans-8, cis 10; trans-8, trans-10; cis-9, cis-11; cis-9, trans-11; trans-9, cis-11; trans-9, trans- 11; cis-10, cis 12; cis-9 trans-12; trans-9, cis-12; trans-lO-trans-12; cis-11, cis-13; cis-11, trans-13; trans-11, cis-13; trans-11, trans-13 octadecadienoic acid; 18:3 cis- 6, cis-9, trans 11; 18:3 cis-6, trans-10, cis-12; 18:3 cis-8, trans-12, cis-14; 20:3 cis- 8, cis-11, trans-13; 20:4 cis-5, cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, trans-12, cis-14, metabolites thereof; and precursors and derivatives thereof. 6. The method of Claim 1 wherein the composition includes a flavor. 7. The method of Claim 1 wherein the composition includes an artificial sweetener. 8. The method of Claim 1 wherein the composition is in pill form, or in a capsule form. 9. The method of Claim 1 wherein the composition includes both chromium and ginseng. 10. A method of treating diabetes comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. 11. The method of Claim 10 wherein approximately 0.1 to about 15 grams per day of conjugated linoleic acid are administered. 12. The method of Claim 10 wherein approximately 0.1 mg to about 1000 mg per day of chromium is administered. 13. The method of Claim 10 wherein approximately 1.0 mg to about 3000 mg per day of ginseng is administered. 14. The method of Claim 10 wherein the conjugated linoleic acid is selected from the group consisting of: either a pure isomer of octadecadienoic acid, a mixture of octadecadienoic acid isomers, cis-8, cis-10; cis-8, trans-10; trans-8, cis 10; trans-8, trans-10; cis-9, cis-11; cis-9, trans-11; trans-9, cis-11; trans-9, trans- 11; cis-10, cis 12; cis-9 trans-12; trans-9, cis-12; trans-lO-trans-12; cis-11, cis-13; cis-11, trans-13; trans-11, cis-13; trans-11, trans-13 octadecadienoic acid; 18:3 cis- 6, cis-9, trans 11; 18:3 cis-6, trans-10, cis-12; 18:3 cis-8, trans-12, cis-14; 20:3 cis- 8, cis-11, trans-13; 20:4 cis-5, cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, trans-12, cis-14, metabolites thereof; and precursors and derivatives thereof. 15. The method of Claim 10 wherein the composition includes a flavor. 16. The method of Claim 10 wherein the composition includes an artificial sweetener. 17. The method of Claim 10 wherein the composition is in pill form. 18. The method of Claim 10 wherein the composition includes both chromium and ginseng. 19. A composition comprising a therapeutically effective amount of conjugated linoleic acid, chromium, and ginseng. 20. The composition of Claim 19 wherein approximately 67%> to about 99%o by weight of the composition is conjugated linoleic acid. 21. The composition of Claim 19 wherein approximately 0.1% to about 1% of the composition is chromium. 22. The composition of Claim 19 wherein approximately 0.1% to about 3% by weight of the composition is ginseng. 23. The composition of Claim 19 wherein the conjugated linoleic acid is selected from the group consisting of: either a pure isomer of octadecadienoic acid, a mixture of octadecadienoic acid isomers, cis-8, cis-10; cis-8, trans-10; trans-8, cis 10; trans-8, trans-10; cis-9, cis-11; cis-9, trans-11; trans-9, cis-11; trans- 9, trans-11; cis-10, cis 12; cis-9 trans-12; trans-9, cis-12; trans-lO-trans-12; cis-11, cis-13; cis-11, trans-13; trans-11, cis-13; frans-11, trans-13 octadecadienoic acid; 18:3 cis-6, cis-9, trans 11; 18:3 cis-6, trans-10, cis-12; 18:3 cis-8, trans-12, cis-14; 20:3 cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, cis-11, trans-13; 20:4 cis-5, cis-8, trans-12, cis-14, metabolites thereof; and precursors and derivatives thereof. 24. The composition of Claim 19 wherein the composition includes a flavor. 25. The composition of Claim 19 wherein the composition includes an artificial sweetener. 26. The composition of Claim 19 wherein the composition is in pill form. 27. The composition of Claim 19 wherein the composition includes both chromium and ginseng. 28. A method of reducing the risk of diabetes or hyperglycemia in an obese patient comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng. 29. A method for maintaining healthy glucose comprising the step of administering a therapeutically effective amount of a composition comprising conjugated linoleic acid and at least one agent chosen from the group consisting of chromium and ginseng to a patient at risk of developing diabetes.

Inventors: MENARD MICHAEL, ROCKWAY SUSIE, MENARD, MICHAEL, ROCKWAY, SUSIE
Applicants: MENARD MICHAEL, PHARMANUTRIENTS, ROCKWAY SUSIE, MENARD, MICHAEL, ROCKWAY, SUSIE
Application year: 2000
Main classification: A61K31
IPC codes: A23L1, A61K9, A61K31, A61K33, A61K36, A61P3