EP1339404A2 - Composition and method - Google Patents

Composition and method

Info

Publication number
EP1339404A2
EP1339404A2 EP01992146A EP01992146A EP1339404A2 EP 1339404 A2 EP1339404 A2 EP 1339404A2 EP 01992146 A EP01992146 A EP 01992146A EP 01992146 A EP01992146 A EP 01992146A EP 1339404 A2 EP1339404 A2 EP 1339404A2
Authority
EP
European Patent Office
Prior art keywords
day
deterioration
cognitive function
composition
accordance
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.)
Withdrawn
Application number
EP01992146A
Other languages
German (de)
French (fr)
Inventor
Steven Curtis Zicker
Karen J. Wedekind
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.)
Colgate Palmolive Co
Original Assignee
Colgate Palmolive Co
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
Priority claimed from US09/922,633 external-priority patent/US20020052402A1/en
Application filed by Colgate Palmolive Co filed Critical Colgate Palmolive Co
Publication of EP1339404A2 publication Critical patent/EP1339404A2/en
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23KFODDER
    • A23K20/00Accessory food factors for animal feeding-stuffs
    • A23K20/10Organic substances
    • A23K20/142Amino acids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23KFODDER
    • A23K20/00Accessory food factors for animal feeding-stuffs
    • A23K20/10Organic substances
    • A23K20/158Fatty acids; Fats; Products containing oils or fats
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23KFODDER
    • A23K50/00Feeding-stuffs specially adapted for particular animals
    • A23K50/40Feeding-stuffs specially adapted for particular animals for carnivorous animals, e.g. cats or dogs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Definitions

  • This deterioration of cognitive function in older humans can now be prevented, inhibited or treated with specific components. These components can be administered in the diet or taken separately orally.
  • composition comprising an antioxidant or mixture thereof quantities sufficient to a. prevent or b. inhibit, or r c. reverse deterioration of cognitive function
  • a further aspect is a method of preventing, inhibiting or reversing deterioration of cognitive function through the administration of this composition.
  • an antioxidant is a material that quenches a free radical.
  • examples of such materials are beta-carotene, selenium, coenzyme Q10 (ubiquinone), lutein, tocotrienols, soy isoflavones, S-adenosylmethionine, glutathione, taurine, N-acetylcysteine, Vitamin E, Vitamin C, alpha-lipoic acid, 1- carnitine and the like.
  • Vitamin E can be administered as a tocopherol or a mixture of tocopherols and various derivatives thereof such as esters like Vitamin E acetate, succinate, palmitate, and the like.
  • the alpha form is preferable but beta, gamma and delta forms can be included.
  • the d form is preferable but racemic mixtures are acceptable.
  • the forms and derivatives will function in a Vitamin E like activity after ingestion.
  • Vitamin C can be administered as ascorbic acid and its various derivatives thereof such as calcium phosphate salts, cholesteryl salt, 2-monophosphate, and the like which will function in a vitamin C like activity after ingesting by the human. They can be in any form such as liquid, semisolid, solid and heat stable form.
  • Alpha-lipoic acid can be administered as alpha lipoic acid or as a lipoate derivative as in US Patent 5,621, 117, racemic mixtures, salts, esters or amides thereof.
  • L-carnitine and various derivatives of carnitine such as the salts such as the hydrochloride, fumarate and succinate s, as well as acetylated carnitine, and the like can be used.
  • the quantities administered to the human are calculated as the active material, per se, that is measured as specific material.
  • the minimum amounts employed should not bring about toxicity.
  • Vitamin E minimum is about 50 or 100 or 150 mg/day. Generally, no more than about 2,000 or desirably about 1,000 or about 750 mg/day can be employed.
  • Vitamin C minimum quantities are generally about 150, about 200 or about 250 mg/day. Maximums generally do not exceed about 1,000 mg/day but can be lower, for example, about 900 or about 750 mg/day.
  • Alpha lipoic acid can be administered up to about 10 or 20 mg/kg body weight/ day. Minimums are about .5 or 1 mg/kg body weight/ day.
  • L-carnitine is administered in the same manner as alpha lipoic acid. Alpha lipoic acid and l-carnitine can be administered at much higher levels but there is no substantially different efficacy observed.
  • Beta-carotene at least about 0.02 mg/kg body weight/ day 1-15 ppm can be employed.
  • Lutein at least about 5 ppm mg/kg body weight/ day can be employed.
  • Tocotrienols at least about 0.5 mg/kg body weight/ day can be employed.
  • Coenzyme Q10 at least about 0.5 mg/kg body weight/ day can be employed.
  • S-adenosylmethionine at least about 1.0 mg/kg body weight/ day can be employed.
  • Taurine at least about 10 mg/kg body weight/ day can be employed.
  • Soy isoflavones at least about 0.5 mg/kg body weight/ day can be used.
  • N-acetylcysteine at least about 1.0 mg/kg/ body weight/ day can be used.
  • Glutathione at least about 1.0 g/kg body weight/ day can be used.
  • Ginkgo Biloba at least 1.0 mg/kg body weight/ day can be used.
  • the quantities can be administered in a typical "one a day" dosage similar to a vitamin. It can be administered in tablet, capsule, caplet for example, or in a liquid carrier form all for ingestion by the human. Additionally, the daily dosage can be broken down into two, three, or four dosage unit forms for convenience or other reasons. Additionally, it can be administered in a food such as snack bars, cereals, and the like.
  • Example 1
  • a supplement or food providing 750 mg vitamin E, 250 mg/ vitamin C, 200 mg lipoic acid and 400 mg of l-carnitine is eaten by an adult human on a daily basis for 5 years starting at age 45.
  • age of 50 no signs of mental deterioration such as disorientation, memory loss, learning impairment, or ability to cope independently with their environmental living situation, classified by objective (or nonobjective) tests such as Folstein's Mini-mental State Exam (MME), Logical Memory and Visual Reproduction tests from the Wechsler Memory Scale (WMS), Katz' scale of activities of daily living, Lawton's scale of instrumental activities of daily living, Pfeiffer's mental status questionnaire, or other pertinent tests as diagnosed by themselves, a care-giver, or health care provider, are observed.
  • MME Folstein's Mini-mental State Exam
  • WMS Wechsler Memory Scale
  • Katz' scale of activities of daily living Lawton's scale of instrumental activities of daily living
  • Pfeiffer's mental status questionnaire or other pertinent tests as
  • MME Folstein's Mini-mental State Exam
  • WMS Wechsler Memory Scale
  • Katz' scale of activities of daily living Lawton's scale of instrumental activities of daily living

Abstract

A composition comprising an antioxidant or mixture thereof in quantities sufficient to prevent, or inhibit, or reverse deterioration of cognitive function.

Description

COMPOSITION AND METHOD
Background Of The Invention
As humans age their mental faculties appear to lessen. This applies to humans in general and is not related to specific conditions such as Alzheimer's and other known-specific disease conditions affecting mental capacity. Memory is not as good as it once was. Learning certain tasks can take a longer time. These types of mental changes are some times associated with or referred to as "old age". Fairly recently this general area is known as cognitive function deterioration and in more generic terms as diminished mental capacity.
This deterioration of cognitive function in older humans can now be prevented, inhibited or treated with specific components. These components can be administered in the diet or taken separately orally.
Summary Of The Invention
In accordance with the invention there is a composition comprising an antioxidant or mixture thereof quantities sufficient to a. prevent or b. inhibit, or r c. reverse deterioration of cognitive function,
A further aspect is a method of preventing, inhibiting or reversing deterioration of cognitive function through the administration of this composition.
Detailed Description Of The Invention Humans can start having deterioration in cognitive function as early as about 50 but generally it can become noticeable at 60, or 70 years of age.
As used in this application, the component(s) that accomplish this are an antioxidant or mixture thereof. An antioxidant is a material that quenches a free radical. Examples of such materials are beta-carotene, selenium, coenzyme Q10 (ubiquinone), lutein, tocotrienols, soy isoflavones, S-adenosylmethionine, glutathione, taurine, N-acetylcysteine, Vitamin E, Vitamin C, alpha-lipoic acid, 1- carnitine and the like. Vitamin E can be administered as a tocopherol or a mixture of tocopherols and various derivatives thereof such as esters like Vitamin E acetate, succinate, palmitate, and the like. The alpha form is preferable but beta, gamma and delta forms can be included. The d form is preferable but racemic mixtures are acceptable. The forms and derivatives will function in a Vitamin E like activity after ingestion. . Vitamin C can be administered as ascorbic acid and its various derivatives thereof such as calcium phosphate salts, cholesteryl salt, 2-monophosphate, and the like which will function in a vitamin C like activity after ingesting by the human. They can be in any form such as liquid, semisolid, solid and heat stable form. Alpha-lipoic acid can be administered as alpha lipoic acid or as a lipoate derivative as in US Patent 5,621, 117, racemic mixtures, salts, esters or amides thereof. L-carnitine and various derivatives of carnitine such as the salts such as the hydrochloride, fumarate and succinate s, as well as acetylated carnitine, and the like can be used.
The quantities administered to the human are calculated as the active material, per se, that is measured as specific material. The minimum amounts employed should not bring about toxicity. Vitamin E minimum is about 50 or 100 or 150 mg/day. Generally, no more than about 2,000 or desirably about 1,000 or about 750 mg/day can be employed. Vitamin C minimum quantities are generally about 150, about 200 or about 250 mg/day. Maximums generally do not exceed about 1,000 mg/day but can be lower, for example, about 900 or about 750 mg/day. Alpha lipoic acid can be administered up to about 10 or 20 mg/kg body weight/ day. Minimums are about .5 or 1 mg/kg body weight/ day. L-carnitine is administered in the same manner as alpha lipoic acid. Alpha lipoic acid and l-carnitine can be administered at much higher levels but there is no substantially different efficacy observed.
Additional antioxidants and their quantities are given in mg/kg body weight/ day numbers.
Beta-carotene at least about 0.02 mg/kg body weight/ day 1-15 ppm can be employed.
Selenium at about 0.02 mg/kg body weight/ day up to 5 ppm can be employed.
Lutein at least about 5 ppm mg/kg body weight/ day can be employed. Tocotrienols at least about 0.5 mg/kg body weight/ day can be employed.
Coenzyme Q10 at least about 0.5 mg/kg body weight/ day can be employed.
S-adenosylmethionine at least about 1.0 mg/kg body weight/ day can be employed.
Taurine at least about 10 mg/kg body weight/ day can be employed. Soy isoflavones at least about 0.5 mg/kg body weight/ day can be used.
N-acetylcysteine at least about 1.0 mg/kg/ body weight/ day can be used.
Glutathione at least about 1.0 g/kg body weight/ day can be used. Ginkgo Biloba at least 1.0 mg/kg body weight/ day can be used.
The quantities can be administered in a typical "one a day" dosage similar to a vitamin. It can be administered in tablet, capsule, caplet for example, or in a liquid carrier form all for ingestion by the human. Additionally, the daily dosage can be broken down into two, three, or four dosage unit forms for convenience or other reasons. Additionally, it can be administered in a food such as snack bars, cereals, and the like. Example 1
A supplement or food providing 750 mg vitamin E, 250 mg/ vitamin C, 200 mg lipoic acid and 400 mg of l-carnitine is eaten by an adult human on a daily basis for 5 years starting at age 45. By the age of 50 no signs of mental deterioration such as disorientation, memory loss, learning impairment, or ability to cope independently with their environmental living situation, classified by objective (or nonobjective) tests such as Folstein's Mini-mental State Exam (MME), Logical Memory and Visual Reproduction tests from the Wechsler Memory Scale (WMS), Katz' scale of activities of daily living, Lawton's scale of instrumental activities of daily living, Pfeiffer's mental status questionnaire, or other pertinent tests as diagnosed by themselves, a care-giver, or health care provider, are observed.
Example 2
An adult human having signs of mental deterioration, such as disorientation, memory loss, learning impairment, or ability to cope independently with their environmental living situation, as classified by objective (or nonobjective) tests such as Folstein's Mini-mental State Exam (MME), Logical Memory and Visual Reproduction tests from the Wechsler Memory Scale (WMS), Katz' scale of activities of daily living, Lawton's scale of instrumental activities of daily living, Pfeiffer's mental status questionnaire, or other pertinent tests as diagnosed by themselves, a care-giver, or a health care provider, is provided a daily food or supplement providing 750 mg vitamin E, 250 mg/ vitamin C, 200 mg lipoic acid and 400 mg of l-carnitine on a daily basis for 1 year. After one year of dosing the above signs are significantly reduced. Example 3
An adult human having signs of mental deterioration such as disorientation, memory loss, learning impairment, or ability to cope independently with their environmental living situation, as classified by objective (or nonobjective) tests such as Folstein's Mini-mental State Exam (MME), Logical Memory and Visual Reproduction tests from the Wechsler Memory Scale (WMS), Katz' scale of activities of daily living, Lawton's scale of instrumental activities of daily living, Pfeiffer's mental status questionnaire, or other pertinent tests as diagnosed by themselves, a care-giver, or a health care provider, is provided a daily food or supplement providing 750 mg vitamin E, 250 mg/ vitamin C, 200 mg lipoic acid and 400 mg of l-carnitine on a daily basis for 2 years. After 2 years of dosing the aforementioned signs have essentially disappeared.

Claims

ClaimsWhat is claimed is:
1. A composition comprising an antioxidant or mixture thereof in quantities sufficient to
a. prevent, or b. inhibit, or c. reverse deterioration of cognitive function.
The composition m accordance with claim 1 wherein deterioration of cognitive function is prevented.
The composition in accordance with claim 1 wherein deterioration of cognitive function is inhibited.
The composition in accordance with claim 1 wherein deterioration of cognitive function is reversed.
5. The composition in accordance with claim 1 wherein Vitamin E is at least about 50 mg/day, Vitamin C is at least about 150 mg/day, l-carnitine is at least about 0.5 mg/kg body weight/ day, and alpha lipoic acid is at least about 0.5 mg/kg body weight/ day.
6. A method for preventing or inhibiting or reversing deterioration of cognitive function in a human which comprises administering a composition of claim 1 to said human.
7. The method in accordance with claim 6 wherein the human is in need of said administering.
8. The method in accordance with claim 6 wherein the deterioration of cognitive function is prevented.
. The method in accordance with claim 6 wherein the deterioration of cognitive function is inhibited.
10. The method in accordance with claim 6 wherein the deterioration of cognitive function is reversed.
EP01992146A 2000-10-31 2001-10-30 Composition and method Withdrawn EP1339404A2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US922633 1992-07-30
US24451100P 2000-10-31 2000-10-31
US244511P 2000-10-31
US25344600P 2000-11-28 2000-11-28
US25344700P 2000-11-28 2000-11-28
US253447P 2000-11-28
US253446P 2000-11-28
US09/922,633 US20020052402A1 (en) 2000-10-31 2001-08-06 Composition and method
PCT/US2001/048665 WO2002043666A2 (en) 2000-10-31 2001-10-30 Compositions containing an antioxidant such as alpha lipoic acid, carnitine, vitamin c or vitamin e for preventing or inhibiting loss of cognitive function

Publications (1)

Publication Number Publication Date
EP1339404A2 true EP1339404A2 (en) 2003-09-03

Family

ID=27500158

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01992146A Withdrawn EP1339404A2 (en) 2000-10-31 2001-10-30 Composition and method

Country Status (6)

Country Link
EP (1) EP1339404A2 (en)
JP (1) JP2004514686A (en)
CN (1) CN1477958A (en)
AU (1) AU2002232616A1 (en)
CA (1) CA2427470A1 (en)
WO (1) WO2002043666A2 (en)

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See also references of WO0243666A3 *

Also Published As

Publication number Publication date
AU2002232616A1 (en) 2002-06-11
CA2427470A1 (en) 2002-06-06
JP2004514686A (en) 2004-05-20
WO2002043666A2 (en) 2002-06-06
CN1477958A (en) 2004-02-25
WO2002043666A3 (en) 2003-01-30

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