EP1339404A2 - Composition and method - Google Patents
Composition and methodInfo
- 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- Withdrawn
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 18
- 238000000034 method Methods 0.000 title claims description 8
- 230000003920 cognitive function Effects 0.000 claims abstract description 14
- 230000006866 deterioration Effects 0.000 claims abstract description 14
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 6
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 18
- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims description 18
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 17
- 230000037396 body weight Effects 0.000 claims description 16
- 235000019136 lipoic acid Nutrition 0.000 claims description 10
- 229960002663 thioctic acid Drugs 0.000 claims description 10
- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-N 0.000 claims description 9
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims description 8
- 229930003268 Vitamin C Natural products 0.000 claims description 8
- 229930003427 Vitamin E Natural products 0.000 claims description 8
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 8
- 235000019154 vitamin C Nutrition 0.000 claims description 8
- 239000011718 vitamin C Substances 0.000 claims description 8
- 235000019165 vitamin E Nutrition 0.000 claims description 8
- 239000011709 vitamin E Substances 0.000 claims description 8
- 229940046009 vitamin E Drugs 0.000 claims description 8
- 235000006708 antioxidants Nutrition 0.000 claims description 5
- 229960001518 levocarnitine Drugs 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 230000000694 effects Effects 0.000 description 8
- 230000003340 mental effect Effects 0.000 description 7
- 241000282412 Homo Species 0.000 description 4
- 235000013305 food Nutrition 0.000 description 4
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 4
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 4
- 208000000044 Amnesia Diseases 0.000 description 3
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 description 3
- 208000026139 Memory disease Diseases 0.000 description 3
- 208000027382 Mental deterioration Diseases 0.000 description 3
- 206010027374 Mental impairment Diseases 0.000 description 3
- 235000017471 coenzyme Q10 Nutrition 0.000 description 3
- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 description 3
- 208000010877 cognitive disease Diseases 0.000 description 3
- 230000006735 deficit Effects 0.000 description 3
- 230000007613 environmental effect Effects 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 230000006984 memory degeneration Effects 0.000 description 3
- 208000023060 memory loss Diseases 0.000 description 3
- 239000013589 supplement Substances 0.000 description 3
- 230000000007 visual effect Effects 0.000 description 3
- GJJVAFUKOBZPCB-ZGRPYONQSA-N (r)-3,4-dihydro-2-methyl-2-(4,8,12-trimethyl-3,7,11-tridecatrienyl)-2h-1-benzopyran-6-ol Chemical class OC1=CC=C2OC(CC/C=C(C)/CC/C=C(C)/CCC=C(C)C)(C)CCC2=C1 GJJVAFUKOBZPCB-ZGRPYONQSA-N 0.000 description 2
- 108010024636 Glutathione Proteins 0.000 description 2
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 description 2
- MEFKEPWMEQBLKI-AIRLBKTGSA-N S-adenosyl-L-methioninate Chemical compound O[C@@H]1[C@H](O)[C@@H](C[S+](CC[C@H](N)C([O-])=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 MEFKEPWMEQBLKI-AIRLBKTGSA-N 0.000 description 2
- BUGBHKTXTAQXES-UHFFFAOYSA-N Selenium Chemical compound [Se] BUGBHKTXTAQXES-UHFFFAOYSA-N 0.000 description 2
- 229960004308 acetylcysteine Drugs 0.000 description 2
- 229960001570 ademetionine Drugs 0.000 description 2
- OENHQHLEOONYIE-UKMVMLAPSA-N all-trans beta-carotene Natural products CC=1CCCC(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C OENHQHLEOONYIE-UKMVMLAPSA-N 0.000 description 2
- 235000013734 beta-carotene Nutrition 0.000 description 2
- 239000011648 beta-carotene Substances 0.000 description 2
- TUPZEYHYWIEDIH-WAIFQNFQSA-N beta-carotene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C)C=CC=C(/C)C=CC2=CCCCC2(C)C TUPZEYHYWIEDIH-WAIFQNFQSA-N 0.000 description 2
- 229960002747 betacarotene Drugs 0.000 description 2
- 229960004203 carnitine Drugs 0.000 description 2
- 229940110767 coenzyme Q10 Drugs 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 229960003180 glutathione Drugs 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 235000012680 lutein Nutrition 0.000 description 2
- 229960005375 lutein Drugs 0.000 description 2
- 239000001656 lutein Substances 0.000 description 2
- KBPHJBAIARWVSC-RGZFRNHPSA-N lutein Chemical compound C([C@H](O)CC=1C)C(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\[C@H]1C(C)=C[C@H](O)CC1(C)C KBPHJBAIARWVSC-RGZFRNHPSA-N 0.000 description 2
- ORAKUVXRZWMARG-WZLJTJAWSA-N lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C ORAKUVXRZWMARG-WZLJTJAWSA-N 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 229910052711 selenium Inorganic materials 0.000 description 2
- 239000011669 selenium Substances 0.000 description 2
- 235000011649 selenium Nutrition 0.000 description 2
- 235000003687 soy isoflavones Nutrition 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 2
- 229960003080 taurine Drugs 0.000 description 2
- 229930003799 tocopherol Natural products 0.000 description 2
- 239000011732 tocopherol Substances 0.000 description 2
- 229930003802 tocotrienol Natural products 0.000 description 2
- 239000011731 tocotrienol Substances 0.000 description 2
- 229940068778 tocotrienols Drugs 0.000 description 2
- 235000019148 tocotrienols Nutrition 0.000 description 2
- KBPHJBAIARWVSC-XQIHNALSSA-N trans-lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C KBPHJBAIARWVSC-XQIHNALSSA-N 0.000 description 2
- FJHBOVDFOQMZRV-XQIHNALSSA-N xanthophyll Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C=C(C)C(O)CC2(C)C FJHBOVDFOQMZRV-XQIHNALSSA-N 0.000 description 2
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 2
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- 235000008100 Ginkgo biloba Nutrition 0.000 description 1
- 244000194101 Ginkgo biloba Species 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 239000007894 caplet Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol group Chemical group [C@@H]1(CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C)[C@H](C)CCCC(C)C HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 1
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- NPCOQXAVBJJZBQ-UHFFFAOYSA-N reduced coenzyme Q9 Natural products COC1=C(O)C(C)=C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)C(O)=C1OC NPCOQXAVBJJZBQ-UHFFFAOYSA-N 0.000 description 1
- 229940091258 selenium supplement Drugs 0.000 description 1
- -1 semisolid Substances 0.000 description 1
- 235000009561 snack bars Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 125000002640 tocopherol group Chemical class 0.000 description 1
- 235000019149 tocopherols Nutrition 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical class [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 229940035936 ubiquinone Drugs 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K20/00—Accessory food factors for animal feeding-stuffs
- A23K20/10—Organic substances
- A23K20/142—Amino acids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K20/00—Accessory food factors for animal feeding-stuffs
- A23K20/10—Organic substances
- A23K20/158—Fatty acids; Fats; Products containing oils or fats
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K50/00—Feeding-stuffs specially adapted for particular animals
- A23K50/40—Feeding-stuffs specially adapted for particular animals for carnivorous animals, e.g. cats or dogs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic 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
- A61K31/352—Heterocyclic 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
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K31/355—Tocopherols, e.g. vitamin E
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Polymers & Plastics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Food Science & Technology (AREA)
- Animal Husbandry (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Psychiatry (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Birds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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
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.
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US922633 | 1986-10-24 | ||
| 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 | |
| US253446P | 2000-11-28 | ||
| US253447P | 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) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2239404C1 (en) * | 2003-09-17 | 2004-11-10 | Бессонов Дмитрий Михайлович | Method for preventing human body aging |
| JP2005185188A (en) * | 2003-12-25 | 2005-07-14 | Nichirei Corp | Processed acerola and composition containing L-carnitine |
| PT1711070E (en) * | 2004-01-28 | 2016-02-15 | Nestec Sa | Nutritional composiition for improving skin condition and preventing skin diseases |
| US20090176864A1 (en) * | 2004-11-24 | 2009-07-09 | Hill's Pet Nutrition, Inc. | Methods For Improving Hepatic and Immune Function In An Animal |
| EP1817058B1 (en) * | 2004-11-24 | 2015-09-02 | Hill's Pet Nutrition, Inc. | Composition for use in improving liver clearance of xenobiotic substances in an animal |
| JP5138380B2 (en) * | 2004-11-24 | 2013-02-06 | ヒルズ・ペット・ニュートリシャン・インコーポレーテッド | Methods for increasing immune responses in animals |
| CN101287460B (en) * | 2005-08-17 | 2012-04-25 | 希尔氏宠物营养品公司 | Composition for preventing and treating kidney disease |
| CN1895671B (en) * | 2005-12-08 | 2012-11-28 | 淮北辉克药业有限公司 | Compound preparation for treating viral liver disease |
| CN101045048B (en) * | 2006-03-27 | 2011-05-18 | 中国科学院上海生命科学研究院 | Application of chondriosome nutrient composition |
| WO2008099469A1 (en) * | 2007-02-14 | 2008-08-21 | Tohoku University | Composition and method for suppressing lipid peroxidation in erythrocytes |
| EP2453759B1 (en) * | 2009-07-14 | 2015-10-21 | Hill's Pet Nutrition, Inc. | Pet food compositions including a sustained-release lipoic acid and methods of manufacture and use thereof |
| EP2508179A1 (en) | 2011-04-05 | 2012-10-10 | Lonza Ltd. | Use of L-Carnitine, salts and derivatives thereof for reducing or preventing fatigue and improving cognitive function |
| KR20140019827A (en) | 2011-04-05 | 2014-02-17 | 론자 아게 (론자 엘티디.) | Use of l-carnitine, salts and derivatives thereof for reducing or preventing fatigue and improving cognitive function |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06199690A (en) * | 1992-03-06 | 1994-07-19 | Yunie:Kk | Agent for promoting cerebral metabolism and improving cerebral function |
| DE4343592C2 (en) * | 1993-12-21 | 1998-04-16 | Asta Medica Ag | Use of R - (+) - alpha-lipoic acid and its metabolites in the form of the free acid or as salts or esters or amides for the treatment of glucose metabolic disorders in the central nervous system |
| FR2721516B1 (en) * | 1994-06-27 | 1996-09-13 | Inst Rech Biolog Sa | New uses of a complex based on brain phospholipids in therapy and in food. |
| US5977162A (en) * | 1996-09-16 | 1999-11-02 | Seidman; Michael D. | Therapeutic treatment for auditory function |
| IT1302307B1 (en) * | 1998-09-01 | 2000-09-05 | Sigma Tau Healthscience Spa | COMPOSITION WITH ANTIOXIDANT ACTIVITY AND FOR IMPROVING THE METABOLIC USE OF GLUCOSE, INCLUDING ACETYL |
| ES2204531T3 (en) * | 1999-03-16 | 2004-05-01 | Merck Patent Gmbh | COMPOSITION THAT INCLUDES ISOQUERCETINA AND ASCORBIC ACID IN A SUSTAINED RELEASE FORM. |
| WO2000057876A1 (en) * | 1999-03-26 | 2000-10-05 | Lipogenics, Inc. | Novel antioxidant formulations and methods for using them |
| DE19920316A1 (en) * | 1999-05-03 | 1999-12-09 | Heinz Kiefer | Antioxidant medicament containing vitamins and trace elements, useful e.g. for maintaining cellular function and preventing cancer |
| AU768189B2 (en) * | 1999-06-15 | 2003-12-04 | Nutri-Logics, Inc. | Nutrient formulations for disease reduction, and related treatment and component screening methods |
| JP2003513039A (en) * | 1999-11-03 | 2003-04-08 | ジュヴェノン インコーポレイテッド | How to treat benign amnesia |
| US20010043983A1 (en) * | 2000-01-25 | 2001-11-22 | Hamilton Nathan D. | Nutritional supplements for aged pets |
| HU227182B1 (en) * | 2000-03-06 | 2010-09-28 | Andras Javor | Lecitin-ascorbic acid combination |
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- 2001-10-30 CN CNA018181880A patent/CN1477958A/en active Pending
- 2001-10-30 CA CA002427470A patent/CA2427470A1/en not_active Abandoned
- 2001-10-30 WO PCT/US2001/048665 patent/WO2002043666A2/en not_active Ceased
- 2001-10-30 JP JP2002545645A patent/JP2004514686A/en active Pending
- 2001-10-30 EP EP01992146A patent/EP1339404A2/en not_active Withdrawn
- 2001-10-30 AU AU2002232616A patent/AU2002232616A1/en not_active Abandoned
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| M.H. BEERS, R. BERKOW: "The Merck Manual of Diagnosis and Therapy, Seventeenth Edition", 1999, MERCK RESEARCH LABORATORIES, WHITEHOUSE STATION, N.J. * |
| See also references of WO0243666A3 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004514686A (en) | 2004-05-20 |
| WO2002043666A2 (en) | 2002-06-06 |
| CA2427470A1 (en) | 2002-06-06 |
| WO2002043666A3 (en) | 2003-01-30 |
| CN1477958A (en) | 2004-02-25 |
| AU2002232616A1 (en) | 2002-06-11 |
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