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US20050226906A1 - Nutrient system for individualized responsive dosing regimens - Google Patents

Nutrient system for individualized responsive dosing regimens Download PDF

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Publication number
US20050226906A1
US20050226906A1 US10/868,149 US86814904A US2005226906A1 US 20050226906 A1 US20050226906 A1 US 20050226906A1 US 86814904 A US86814904 A US 86814904A US 2005226906 A1 US2005226906 A1 US 2005226906A1
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US
United States
Prior art keywords
vitamin
series
base
rda
composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
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US10/868,149
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English (en)
Inventor
Ricky Moneymaker
Larry Klesman
Jon Theus
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Micro Nutrient LLC
Original Assignee
Micro Nutrient LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Micro Nutrient LLC filed Critical Micro Nutrient LLC
Priority to US10/868,149 priority Critical patent/US20050226906A1/en
Assigned to MICRO NUTRIENT LLC reassignment MICRO NUTRIENT LLC ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: KLESMAN, LARRY S., THEUS, JON SCOTT, MONEYMAKER, RICKY D.
Priority to US11/080,790 priority patent/US7785619B2/en
Priority to PCT/US2005/008599 priority patent/WO2005102295A1/fr
Priority to EP05730880A priority patent/EP1740159A1/fr
Priority to CN200580016730XA priority patent/CN1972676B/zh
Priority to AU2005235137A priority patent/AU2005235137A1/en
Priority to CA002561553A priority patent/CA2561553A1/fr
Publication of US20050226906A1 publication Critical patent/US20050226906A1/en
Priority to US11/483,208 priority patent/US7727546B2/en
Priority to US12/033,461 priority patent/US7850987B2/en
Priority to US12/606,613 priority patent/US20100047223A1/en
Priority to US12/606,733 priority patent/US20100047364A1/en
Abandoned legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/34Copper; Compounds thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/15Vitamins
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/16Inorganic salts, minerals or trace elements
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/17Amino acids, peptides or proteins
    • A23L33/175Amino acids
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/30Dietetic or nutritional methods, e.g. for losing weight
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    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/07Retinol compounds, e.g. vitamin A
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415Pyridoxine, i.e. Vitamin B6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A61K31/51Thiamines, e.g. vitamin B1
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/5939,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7135Compounds containing heavy metals
    • A61K31/714Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/26Iron; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/30Zinc; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame

Definitions

  • the present technology relates generally to individualized responsive dosing dietary supplement systems, compositions, methods of treatment, and processes of producing the same, which allow a consumer to target identifiable, individualistic biological conditions or responses. More specifically, the present technology relates to a dietary supplement system for targeting individualized biological conditions or responses which utilizes ultra-low dosage amounts of vitamins, minerals, amino acids, co-enzymes, stimulants, and/or similar ingredients in a highly bio-active delivery system, such that an individual may take multiple doses of the same or different dietary supplement mixture based on varying biological need or desired response within each 24 hour period.
  • the Food and Nutrition Board of the National Research Council replaced and expanded the Recommended Dietary Allowances (RDAs) with Dietary Reference Intakes (DRIs) to provide recommended vitamin, mineral, or other nutrient intakes for use in a variety of settings for humans.
  • the DRIs are actually a set of four reference values: Estimated Average Requirements (EAR), Recommended Dietary Allowances (RDA), Adequate Intakes (AI), and Tolerable Upper Intake Levels (UL). These values serve as recommended dosage levels for vitamins, minerals, or other nutrients.
  • EAR Estimated Average Requirements
  • RDA Recommended Dietary Allowances
  • AI Adequate Intakes
  • UL Tolerable Upper Intake Levels
  • L-arginine is typically provided in dietary supplements in dosages of about 100 milligrams, and L-glutamine in dosages of about 500 milligrams, pursuant to the FDA.
  • Dietary supplements are generally nutrient mixtures commonly taken in single mega-dose dosage forms which contain vitamin, mineral and other nutrient doses equal to or over the Recommended Dietary Allowances (RDA) values.
  • RDA Recommended Dietary Allowances
  • a consumer usually has little choice in choosing the variety of ingredients, dosage levels, or dosing regimens of a conventional dietary supplement, such as a standard vitamin tablet.
  • Conventional dietary supplements may be effective for a general purpose, but usually provide an excess of vitamins, minerals, stimulants, or other compounds which a consumer does not desire, or those supplements may not adequately target an individual's specific dietary need or desired biological response.
  • conventional dosage forms of dietary supplements only allow a consumer to take one or two doses per 24 hour period. As a result, conventional dietary supplements fail to recognize that the physiological state and resultant nutrient requirements of any single individual can depend upon and fluctuate based upon a number of different biophysical variables during the course of each day or dosing regimen.
  • U.S. Pat. No. 4,882,167, to Jang discloses dry direct compressed products for controlled release of actives including vitamins or minerals.
  • the compositions and methods of the Jang patent do not provide for ultra-low dosage amounts of vitamins or minerals, dosing flexibility, or systems, compositions, or methods for individualized responsive dosing based on a desired biological response.
  • the process for producing an individualized responsive dosing nutrient system preferably first comprises a starting water source which preferably contains beneficial, but ultra low dosage levels of at least one nitrate, at least one nitrite, and at least one mineral.
  • a base mixture is then added containing at least two vitamins and/or minerals, which is selected from a group of two or more base compositions configured to generate one or more pre-determined biological responses.
  • the base mixture is preferably selected based on a desired biological response for the finished dietary supplement composition.
  • a pre-mix composition which is preferably of a constant compositional make-up during different runs of the process, is then added or, alternatively, is added as part of the base mixture.
  • the mixture comprising the water, base mixture, and pre-mix may then be further diluted based on a pre-determined dilution factor, to vary the ultimate dosage levels in the finished nutrient composition.
  • the amount of base mixture may be varied during processing based on a pre-determined multiplier.
  • the mixture containing water, base mixture, and pre-mix, and optionally further water is configured into or onto a delivery system (such as, but not limited to an oral film) which substantially avoids first-pass metabolism, to form a finished single nutrient composition.
  • a delivery system such as, but not limited to an oral film
  • the dosage level of any vitamin, mineral, amino acid, or co-enzyme contained in the finished nutrient compositions of the presently described technology be less than 25% of the RDA or UL for such vitamin, mineral, amino acid, co-enzyme, or other nutrient. More preferably, the dosage levels are less than 10%, 1%, or 0.1% of RDA or UL for each nutrient.
  • the foregoing process steps may be repeated one or more times, more preferably five or more times, and most preferably, ten or more times, and either a different base mixture is selected, or a different dilution or base multiplication factor is selected, to produce a system/series of nutrient compositions capable of being utilized for individualized biological responsive dosing.
  • a method for individualized responsive dosing to generate a biological response comprising the steps of providing a selection of two or more nutrient formulations in delivery systems which substantially avoid first pass metabolism and which provide two or more vitamins, minerals, amino acids, co-enzyme, or other nutrient in amounts preferably less than 10% or 1% of RDA or UL, more preferably less than 0.01% of RDA or UL, and most preferably less than 0.0001% of RDA or UL and a water source comprising at least one mineral, nitrate, nitrite, and/or other nutrients in amounts preferably less than 0.001% of RDA or UL.
  • the dosage levels are at least 1 ⁇ 10 ⁇ circumflex over ( ) ⁇ -7% of RDA or UL.
  • the two or more nutrient compositions are preferably separately configured to generate one or more pre-determined biological responses, including, but not limited to: stress-relief, cellular metabolism, energy conservation, energy utilization, energy enhancement, enhanced memory, enhanced cognitive function, calmness, awareness, stimulation of the hypothalamic-pituitary-thyroid axis, fatigue relief, enhanced immune response, antioxidation, liver detoxification, and alcohol metabolism.
  • the dose of a vitamin, mineral, or other nutritional supplement ingredient when adapted for delivery via a system that substantially avoids first pass metabolism, may be significantly reduced while still producing a desired beneficial effect/biological response.
  • the ingredients of a dietary supplement may be provided at substantially lower levels (i.e. ultra-low levels) than those recommended by the government as a raw material standard (RDA, UL, UDA, etc.).
  • ultra-low dosage levels and bioactive delivery systems allow dietary supplement compounds to be repeatedly and flexibly administered to an animal or human for the enhancement and augmentation of those biological functions known to be influenced by any of the individual components.
  • an intermediate mixture comprising the water, base mixture, and pre-mix may be further diluted based on a preferably pre-determined dilution factor, to vary the ultimate dosages of the nutrients in the final formulation.
  • a pre-determined dilution factor a preferably pre-determined dilution factor
  • the amount of base mixture may be varied during processing based on a multiplier. Both the multiplier or dilution factor are experimentally determined.
  • the multiplier ranges from 20 to 40.
  • the final dosage amounts of any components in the final formulation i.e. the final oral strip, liquid drops, capsules, troches, lozenges, etc.
  • the final dosage amounts of any components in the final formulation can be calculated.
  • a manufacturer may efficiently create a number of different series, such as illustrative Series S, Series T, Series U, Series V, Series K, Series L, Series M, Series N, Series X, and Series W, by utilizing different base mixtures.
  • Examples 4 through 13 describe preferred base compositions for creation of the foregoing series.
  • Each series may generate a desired and distinct biological effect or responses, or may overlap slightly in degree of the same response.
  • a manufacturer may utilize differing dilution or multiplication factors to efficiently create a gradient of biological responses (i.e. sleep (low energy) to awake and active high energy).
  • Examples 3 and 15 gives a examples of a gradient of dilution factors and corresponding biological effects/responses observed within a given series. (Series S).
  • compositions of the present technology can include any of the water-soluble and/or fat-soluble vitamins, a coenzyme such as Q 10 , essential and/or non-essential amino acids, and minerals including without limitation calcium, phosphorus, magnesium, sodium, potassium, chloride, chromium, copper, fluoride, iodine, iron, manganese, molybdenum, selenium and zinc.
  • the presently described technology can also include other ingredients, for example, nitrate, nitrite, folic acid, and stimulants such as caffeine. It is also contemplated that the compositions of the present technology may further include pharmaceutical compositions.
  • the water can vary from source to source, but preferably contains at least one nitrate, at least one mineral, and at least one nitrite.
  • the presently described technology utilizes water from an Appalachia water source, preferably a water source from the Eastern slope of the Shenandoah Valley. Different water sources would require empirical analysis of its constituents to ensure that the dosage amounts are consistent with spirit of the presently described technology. For example, the base composition multiplier could be changed in order to obtain an adjusted base with a preferred compositional make-up in light of a different water source.
  • base mixtures of the present technology are embodied in Tables 4 through 13 and have been designated as series S, T, U, V, K, L, M, N, X and W.
  • Those examples illustrate the preferred makeup in grams of the individual ingredients/components of exemplar base compositions, including the amount of vitamin premix used and the amount of any additional components admixed with the vitamin premix.
  • Table 4 illustrates that the base composition for the S series comprises 0.02500 grams of vitamin premix admixed with additional components, including for example 0.06000 grams of magnesium chloride.
  • the adjustment of each component of the base composition by application of a dilution or multiplication factor to arrive at the adjusted base composition.
  • the multiplier is based upon the dissolution of the selected components in a final volume of 1 gallon of profiled water.
  • Any base composition multiplier may be experimentally determined in regards to a desired biological effect/response, and is, for illustrative purposes, established relative to that water characterized in Example 2.
  • a multiplication factor is preferably empirically determined so as to compensate for variables.
  • the variables that are taken into consideration can include without limitation: any additional ingredients/components coming from selected water sources used for dissolution; any processing required to arrive a final dosage form; and/or any adjustments required to achieve a desired biological response/effect.
  • the multiplier is empirically derived and can range from a factor of about 20 to about 40.
  • additional components/ingredients added to the vitamin premix to form a base composition may include without limitation magnesium chloride, sodium chloride, potassium chloride, calcium chloride, ascorbic acid, caffeine, niacin, potassium benzoate, chromium picolinate, chromium polynicolinate, coenzyme Q10, L-glutamine, and potassium sorbate, sodium ascorbate, potassium carbonate, calcium ascorbate, calcium carbonate, L-arginine, sodium nitrite, and combinations and derivatives thereof.
  • composition of the present invention is formulated to promote absorption of ingredients/components of the final formulation through the buccal, sublingual, pharyngeal and/or esophageal mucous membranes.
  • pre-gastric absorption will occur primarily across the mucous membranes in the mouth or oral cavity, pharynx and esophagus.
  • the oral mucosa has a thin epithelium and a rich vascularity that favors absorption. Blood capillaries are extremely close to the surface in these areas and readily absorb the ingredients into the blood stream. The flow is from this area of the mouth to the Carotid Artery and it is envisaged that distribution to the brain and the rest of the body will be rapid, thereby resulting in greatly enhanced efficacy and/or rates of response.
  • ingredients absorbed by pre-gastric absorption will pass straight into the systemic circulatory system and thereby avoid the gastrointestinal track and first pass metabolism in the liver. Accordingly, bioavailability of an active ingredient delivered in this way may also be increased. Additionally, the bioavailability of a number of vitamins, minerals, amino acids, co-enzymes, and/or other nutrients in concert can also be increased. It is desired that the dose of an ingredient may be minimized, while still producing the desired beneficial effects, with close to zero order kinetics (immediate efficacy) thereby decreasing the required dose. These concentrations may vary and will be selected primarily on the desired biological response and dosage form selected.
  • the preferred method of dosing provides a selection of three or more nutrient formulations in delivery systems which substantially avoid first pass metabolism, and each member of the selected nutrient formulations comprises: (a) at least five or more vitamins, minerals, amino acids, co-enzyme, or other nutrients in amounts no greater than about 25% of the Recommended Daily Allowance (RDA) or Upper Limit (UL); (b) water containing at least one mineral, nitrate, and nitrite, each in an amount less than about 25% of the RDA or UL for that component; and (c) optionally, a stimulant. Furthermore, each of the three or more nutrient formulations is separately configured to generate a specific, pre-determined biological response/effect.
  • the different formulations of the present technology may be configured to generate the following pre-determined biological responses: cellular metabolism including nucleic acid and amino acid metabolism; energy metabolism, including energy conversion and utilization; mental acuity, including memory and cognitive function; nerve signaling including neuromuscular transmission and propagation; hormone signaling including stimulation of the hypothalamic-pituitary-thyroid axis; management of peripheral and central fatigue, including the enhancement of antioxidant defense systems; the mitigation of episodic and/or chronic stress; and detoxification by the liver including increased alcohol metabolism.
  • each formulated series has a different biological effect/response which can be graded within the series.
  • a series such as exemplary Series S may be anecdotally shown to produce varying levels of energy or relaxation per composition/formulation within the series.
  • the gradient of Example 15 may be observed.
  • a series such as the exemplary S series may enhance biochemical signal processing within cellular tissues to cause a gradient of energy levels observed which are dependent upon the concentration (i.e., solids content) of the composition within the series utilized (i.e., S-1 biological effects v. S-10 biological effects). It is further believed that such energy enhancement effects are due to enhanced cellular radical scavenging, oxygenation, or utilization of GABA as well as tissue responses such as vasodilation or enhanced glomerular filtration.
  • the administration of these formulations to the body in a delivery system which preferably avoids first pass metabolism increases bioavailability of the formulations to the body, which in turn enhances component ingredient capacity or concentrations at a cellular level to the tissues, which in turn again with increased capacity improves cellular absorptive capacity of the component/ingredient leading to a biochemical signal being generated to those tissues and a biological/biochemical response produced.
  • an individual may select one of the series to begin with and attempt to achieve a particular desired biological response.
  • the patient may select the S-series to achieve enhanced levels of energy or drowsiness depending upon which composition within the S-series is selected. If the patient selects an illustrative S-1 composition, then the patient could preferably take 1 strip or 1 drop of the composition at a time to try and achieve the “energy” effect desired. If the effect is not achieved, then the patient may continue with a strip by strip or drop by drop approach to try and achieve the particular biological effect desired with that particular composition of the series.
  • This particular dosage methodology is an individualized responsive dosing or titration approach. For a liquid formulation, an individual may preferably begin with 5 drops and continue to titrate drop by drop to attempt to achieve the desired biological response/effect. For comparison purposes, 120 drops equal 1 Teaspoon.
  • composition of the series still does not provide the biological response/effect the individual desires, then the individual can select a high solids content formulation within the series such as, for example, S-2 to S-10 to try and achieve the desired effect (or change of effect, i.e., from sleep to energy) on a strip by strip or drop by drop basis again.
  • a high solids content formulation within the series such as, for example, S-2 to S-10 to try and achieve the desired effect (or change of effect, i.e., from sleep to energy) on a strip by strip or drop by drop basis again.
  • a different series/formulation may generate completely different biological responses/effects (i.e. calmness versus enhanced memory), or may overlap in its response/effect.
  • S and K the only differences are that S starts at a lower energy level than K where K starts at a higher energy level immediately at the K-1 sub-series. In contrast, S-1 is more suitably directed to sleep promotion.
  • T-1 formulation will have a different biological effect than an S-1 formulation, although certain T Series formulations may have similar biological effects to certain S Series formulations (i.e., effect/response overlap). Yet, the same individualized responsive dosing approach is utilized.
  • the overall dosing methodology above is referred to as individualized responsive dosing since the individual is dosing his or herself in a stepwise fashion to attempt to achieve the desired biochemical signal and resultant biological effect, response, or condition.
  • Conventional vitamin regimens do not allow patients to variably and individually dose themselves based upon their biological responses and biochemical signals because conventional vitamin/mineral compositions are a one mega-dose/one dosing regimen fits all type approach which would be counter to the presently described technology's individualized responsive dosing approach.
  • Dilution rate to 1 gallon mixture Sub-series for processing into final product S-1 0.5 oz to 1 gallon S-2 1 oz to 1 gallon S-3 2 oz to 1 gallon S-4 3 oz to 1 gallon S-5 4 oz to 1 gallon S-6 5 oz to 1 gallon S-7 6 oz to 1 gallon S-8 7 oz to 1 gallon S-9 8 oz to 1 gallon S-10 9 oz to 1 gallon S-11 10 oz to 1 gallon S-16 15 oz to 1 gallon S-21 20 oz to 1 gallon S-26 25 oz to 1 gallon Dilution Method for all S Series products - Mix initial proscribed amount of Base Mixture with the same quantity of profiled water. Agitate for 1 minute per dilution. Repeat until 1 gallon of finished mixture is produced. For example, 8 such steps are required for S-1. Preferably, wait about 8 hours between dilution steps.
  • Ascorbic acid 0.50000 g 23 11.5 g (ester C)
  • Ascorbic acid 0.50000 g 23 11.5 g (ester C)
  • Ascorbic acid 0.50000 g 23 11.5 g (ester C)
  • S-1 Generates a biochemical signal for sleep (almost unconscious)
  • S-2 Generates a biochemical signal for relaxation
  • S-3 Generates a biochemical signal for calmness
  • S-4 Generates a biochemical signal for decreased anxiety
  • S-5 Generates a biochemical signal for increased mental alertness
  • S6-S7 Generates a biochemical signal for increased mental acuity and focus
  • S-8 Generates a biochemical signal for increased energy
  • S-9 Generates a biochemical signal for further increased energy without the sensation of a lactic acid burn
  • S-10 Generates a biochemical signal for enhanced energy sensation.

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US10/868,149 US20050226906A1 (en) 2004-04-08 2004-06-15 Nutrient system for individualized responsive dosing regimens
CA002561553A CA2561553A1 (fr) 2004-04-08 2005-03-15 Composition(s) et systeme(s) de pharmanutrition destines a des regimes posologiques individualises adaptes aux besoins
CN200580016730XA CN1972676B (zh) 2004-04-08 2005-03-15 用于个体化应答式给药方案的营养药的组合物和系统
PCT/US2005/008599 WO2005102295A1 (fr) 2004-04-08 2005-03-15 Composition(s) et système(s) de pharmanutrition destinés à des régimes posologiques individualisés adaptés aux besoins
EP05730880A EP1740159A1 (fr) 2004-04-08 2005-03-15 Composition(s) et système(s) de pharmanutrition destin s à des r gimes posologiques individualis s adapt s aux besoins
US11/080,790 US7785619B2 (en) 2004-04-08 2005-03-15 Pharmanutrient composition(s) and system(s) for individualized, responsive dosing regimens
AU2005235137A AU2005235137A1 (en) 2004-04-08 2005-03-15 Pharmanutrient composition(s) and system(s) for individualized, responsive dosing regimens
US11/483,208 US7727546B2 (en) 2004-04-08 2006-07-07 Nutrient system for individualized responsive dosing regimens
US12/033,461 US7850987B2 (en) 2004-04-08 2008-02-19 Nutrient composition(s) and system(s) for individualized, responsive dosing regimens
US12/606,613 US20100047223A1 (en) 2004-04-08 2009-10-27 Pharmanutrient Composition(s) and System(s) for Individualized, Responsive Dosing Regimens
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CN1972676A (zh) 2007-05-30
EP1740159A1 (fr) 2007-01-10
US20100047364A1 (en) 2010-02-25
WO2005097085A1 (fr) 2005-10-20
CN1972676B (zh) 2013-04-03
WO2005102295A1 (fr) 2005-11-03
US20060269619A1 (en) 2006-11-30
CA2561553A1 (fr) 2005-11-03
US7727546B2 (en) 2010-06-01

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