The Science of Ketosis

 

Patent Application Serial No. 61/803,203
“Compositions and methods for producing elevated and sustained ketosis”

SUMMARY OF THE INVENTION

A ketogenic diet is effective at raising blood ketone levels and has potential broad applications, but achieving the advantages of those applications requires strict compliance with the diet. The present invention provides a strategy to elevate and sustain blood ketone body levels through the administration of novel combinations of ketogenic supplements and causes a rapid and sustained elevation of blood ketones with a single oral administration. The invention exploits the metabolic and physiological advantages of sustained ketosis (e.g. keto-adaptation) which utilizes ketones as an alternative fuel to improve metabolic health, physical performance and enhance disease prevention.

As such, a composition of ketone precursors is disclosed which comprises at least one medium chain fatty acid, or an ester thereof such as a medium chain triglyceride, and a β-hydroxybutyrate ketone source or precursor. There are numerous sources of ketones and ketogenic precursors.

Nonlimiting examples of the beta-hydroxybutyrate compound include beta-hydroxybutyrate salts such as sodium beta-hydroxybutyrate and arginine beta-hydroxybutyrate, potassium beta-hydroxybutyrate, calcium beta-hydroxybutyrate, magnesium beta-hydroxybutyrate, lithium beta-hydroxybutyrate, lysine beta-hydroxybutyrate, histidine beta-hydroxybutyrate, ornithine beta-hydroxybutyrate, creatine beta-hydroxybutyrate, agmatine beta-hydroxybutyrate, citrulline beta-hydroxybutyrate, beta-hydroxy butyrate sodium salt, beta-hydroxy butyrate potassium salt, beta-hydroxy butyrate calcium salt, beta-hydroxy butyrate magnesium salt, or a combination of salts.

Nonlimiting examples of combinations of beta-hydroxybutyrate salts include sodium beta-hydroxybutyrate and arginine beta-hydroxybutyrate, or beta-hydroxy butyrate sodium salt and beta-hydroxy butyrate potassium salt. Other β-hydroxybutyrate ketone sources include, without limiting the scope, 1,3-butanediol, ethyl acetoacetate, and ethyl beta-hydroxybutyrate. The compounds, are optionally administered between 2 grams and 50 grams, between 5 grams and 30 grams, or between 10 grams and 20 grams. For example, the ketone compounds are optionally administered at 2 grams, 4 grams, 5 grams, 6 grams, 7 grams, 8 grams, 9 grams, 10 grams, 11 grams, 12 grams, 13 grams, 14 grams, 15 grams, 17 grams, 19 grams, 20 grams, 22 grams, 24 grams, 26 grams, 28 grams, 30 grams, 32 grams, 34 grams, 36 grams, 38 grams, 40 grams, 42 grams, 44 grams, 46 grams, 48 grams, or 50 grams.

In some variations of the invention, the beta-hydroxy butyrate compound is histidine beta-hydroxybutyrate, ornithine beta-hydroxybutyrate, creatine beta-hydroxybutyrate, agmatine beta-hydroxybutyrate, or citrulline beta-hydroxybutyrate. The compound is optionally a racemic DL-beta hydroxybutyrate or the single isomer R-beta hydroxybutyrate.
It is also contemplated that additional ketone precursors or supplements might be used in combination with beta hydroxybutyrate and medium chain triglycerides. These additional ketone precursors or supplements might include acetoacetate, ketone esters, and other compounds that cause a rise in blood ketone levels.

As noted, many individuals, especially females, experience lethargy and light-headedness, referred to by some as the “low carb flu,” caused by glucose withdraw in the brain and to a depletion of minerals, especially sodium and potassium in the plasma when entering ketosis through a ketogenic diet. These symptoms can be attenuated or reversed with sufficient supplementation of sodium, potassium, calcium and magnesium.

Supplemental administration of minerals prevents potassium depletion via the renal-adrenal aldosterone pathway. As such, the invention optionally uses mineral salts of beta-hydroxybutyrate (βHB). Mineral salts of βHB are described above and include, without limiting the scope of the invention, potassium βHB, sodium βHB, calcium βHB, magnesium βHB, lithium βHB and any other feasible non-toxic mineral salts of βHB. Organic salts of βHB include, without limiting the scope of the invention, salts of organic bases such as arginine βHB, lysine βHB, histidine βHB, ornithine βHB, creatine βHB, agmatine βHB, and citrulline βHB. The salts may contain the racemic DL-beta hydroxybutyrate or the single isomer R-beta hydroxybutyrate.

Non-limiting examples and sources of the medium chain fatty acid, or an ester thereof such as a medium chain triglyceride, include coconut oil, coconut milk powder, fractionated coconut oil, palm oil, palm kernel oil, caprilic acid, isolated medium chain fatty acids, such as isolated hexanoic acid, isolated octanoic acid, isolated decanoic acid, medium chain triglycerides either purified or in natural form such as coconut oil, and ester derivatives of the medium chain fatty acids ethoxylated triglyceride, enone triglyceride derivatives, aldehyde triglyceride derivatives, monoglyceride derivatives, diglyceride derivatives, and triglyceride derivatives, and salts of the medium chain triglycerides. Ester derivatives optionally include alkyl ester derivatives, such as methyl, ethyl, propyl, butyl, hexyl, etc. Oils may be spray dried onto solid supports such as maltodextrin to facilitate delivery in powder form. The at least one medium chain triglyceride is optionally administered at between 5 grams and 50 grams, between 10 grams and 40 grams, or between 15 grams and 30 grams. As a nonlimiting example, the medium chain triglyceride is administered at 5 grams, 6 grams, 7 grams, 8 grams, 9 grams, 10 grams, 11 grams, 12 grams, 13 grams, 14 grams, 15 grams, 17 grams, 19 grams, 20 grams, 22 grams, 24 grams, 26 grams, 28 grams, 30 grams, 32 grams, 34 grams, 36 grams, 38 grams 40 grams.
The composition optionally includes at least one non-toxic mineral salt. Nonlimiting examples include the minerals Na, Mg, V, K, Cr, Mn, Co, Cu, Zn, As, Mo and Se associated with an ion of chlorine, sulfate, iodine, bromine, or other known ion in the art. Examples include sodium chloride, zinc sulfide, potassium iodine.

The ketone precursors are preferably ingested along with nutritional substrates such as free amino acids, amino acid metabolites, vitamins, minerals, electrolytes and metabolic optimizers such as NADH, soluble ubiquinol, tetrahydrobiopeterin, alpha-ketoglutaric acid, carnitine, and/or alpha lipoic acid, nutritional co-factors, calcium beta-methyl-beta-hydroxybutyrate, arginine alpha-ketoglutarate, sodium R-alpha lipoic acid, thiamine, riboflavin, niacin, pyridoxine, ascorbic acid, citric acid, malic acid, sodium benzoate, potassium sorbate, acesulfame K, aspartame, xanthan gum, or a combination thereof. Nonlimiting examples of nutritional co-factors include R-alpha lipoic acid, acetyl-1-carnitine, ketoisocaproate, alpha-ketoglutarate, alpha-hydroxyisocaproate, creatine, branched chain amino acids (leucine, isoleucine, valine), beta-hydroxy-beta methylbutyrate (HMB), B vitamins, vitamin C, soluble ubiquinol, and carnitine that assist in mitochondrial function. In some variations, the supplemental mixture shall provide no more than 400 calories per day.

The compositions are useful for weight loss and treatment of high blood glucose or type II diabetes and can improve the user’s general health in a short period of time. In another embodiment, the βHB salt/medium chain triglyceride formula is used to facilitate weight loss, as a brain tonic, to enhance athletic performance, to help prevent diseases related to metabolic dysfunction, mitochondrial defect, and insulin resistance, as an adjunct to a ketogenic diet, as an anti-aging supplement, and other uses associated with improved metabolic health. A combination βHB/MCT composition is optionally administered in a range of 1:1 to 1:2 mixture to elevate blood ketones to a level that would be considered a state of nutritional ketosis.

Administration can be performed with or without dietary restriction. In some variations, the patient preferably follows a ketogenic diet that restricts intake of carbohydrates and protein during the period of administration of the βHB/MCT composition. In specific embodiments, the patient restricts the dietary intake to a ratio of about 65% fat, 25% protein, and 10% carbohydrates.

The therapeutic ketosis produced herein provides a rapid and sustained keto-adaptation as a metabolic therapy for a wide range of metabolic disorders, and provides nutritional support for therapeutic fasting, weight loss, and performance enhancement. As such, the composition is optionally administered once per day, twice per day, or three times per day to a subject desiring to promote and/or sustain a state of ketosis.

In an embodiment of the invention, the preferred route of administration of the mixture of βHB salts and MCT oil is oral. The product may be delivered as a powdered mixture, as a ready-to-drink liquid, in hard or soft gelatin caps, as hard-pressed tablets, concentrated gels, or any other dosage form known to those trained in the art. The product is preferably delivered in the form of a ready-to-drink formula consisting of a mixture of sodium and potassium βHB along with coconut milk powder. The drink may be pH adjusted with citric and/or malic acid, and artificial sweetener and flavoring can be added. The drink should be homogenized and pasteurized.

Because the supplements and methods of the present invention will raise the level of blood ketones, the subject may enjoy greater flexibility in the diet that must be followed to maintain a state of ketosis. Thus, while consistently taking the supplement of the present invention, a subject may be able to enjoy an occasional carbohydrate or sugar “cheat” and not significantly jeopardize their ketogenic state.

Come in and out of Ketosis “at-will” (even after a cheat day)

Indeed, because the present invention facilitates the quick and easy transition into ketosis, should one need to depart from a strict ketogenic diet for a day or two, getting back into ketosis can be accomplished quickly and without the difficult symptoms which heretofore impeded the process.

Through the consumption of the supplements of the present invention, a measureable increase in blood ketones can often be observed within hours of taking the supplements. This is particularly true if the subject maintains a ketogenic diet while taking the supplements. Thus, whereas it may take weeks to measure an increase of blood ketones following a ketogenic diet alone, the utilization of the present invention will allow the increase of blood ketones to be measured quickly, thereby encouraging and motivating those pursuing a state of ketosis.

Patent US-6,613,356
“Weight Loss Medication and Method”

SUMMARY OF INVENTION

The present invention comprises potassium butyrate and certain closely related chemical compounds, which reduce appetite in mammals when administered orally to the mammals.

The invention also comprises certain other chemicals mixed with the butyrate compounds which facilitate the dispersion of the medication in the mammal’s stomach, and it also involves a method both as to timing and dosage for administering the medication to humans.

OBJECTS AND ADVANTAGES

The objects and advantages of the present invention are:

1. The medication is easy to manufacture.

2. The medication is inexpensive to manufacture.

3. The medication is a substance which often naturally occurs in the intestines of mammals, and is therefore expected to have minimal toxicity or side effects.

4. The medication adds to the physician’s armamentarium against obesity.

6. The medication’s dispersion in the mammal’s stomach is facilitated by gas generating substances in the tablet or capsule.

7. The medication can be used for longer periods than many other weight loss medications.
Still further objects and advantages will become evident from the detailed description of the invention, and the drawings.

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