IES68517B2 - Anti-oxidant formulations - Google Patents
Anti-oxidant formulationsInfo
- Publication number
- IES68517B2 IES68517B2 IES950246A IES68517B2 IE S68517 B2 IES68517 B2 IE S68517B2 IE S950246 A IES950246 A IE S950246A IE S68517 B2 IES68517 B2 IE S68517B2
- Authority
- IE
- Ireland
- Prior art keywords
- vitamin
- day
- carotene
- beta
- per
- Prior art date
Links
- 230000003078 antioxidant effect Effects 0.000 title claims abstract description 20
- 239000003963 antioxidant agent Substances 0.000 title claims abstract description 19
- 235000006708 antioxidants Nutrition 0.000 title claims abstract description 19
- 239000000203 mixture Substances 0.000 title claims abstract description 15
- 238000009472 formulation Methods 0.000 title claims abstract description 14
- 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 abstract description 23
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 22
- 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 claims abstract description 13
- 235000013734 beta-carotene Nutrition 0.000 claims abstract description 13
- 239000011648 beta-carotene Substances 0.000 claims abstract description 13
- 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 claims abstract description 13
- 229960002747 betacarotene Drugs 0.000 claims abstract description 13
- 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 claims abstract description 13
- 229930003427 Vitamin E Natural products 0.000 claims abstract description 10
- 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 abstract description 10
- 229940046009 vitamin E Drugs 0.000 claims abstract description 10
- 235000019165 vitamin E Nutrition 0.000 claims abstract description 10
- 239000011709 vitamin E Substances 0.000 claims abstract description 10
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229930003268 Vitamin C Natural products 0.000 claims abstract description 9
- 235000019154 vitamin C Nutrition 0.000 claims abstract description 9
- 239000011718 vitamin C Substances 0.000 claims abstract description 9
- 102000007330 LDL Lipoproteins Human genes 0.000 claims abstract description 8
- 108010007622 LDL Lipoproteins Proteins 0.000 claims abstract description 8
- 208000024172 Cardiovascular disease Diseases 0.000 claims abstract description 6
- 239000002552 dosage form Substances 0.000 claims abstract description 6
- 239000004480 active ingredient Substances 0.000 claims abstract description 5
- 239000002775 capsule Substances 0.000 claims abstract description 5
- 239000007788 liquid Substances 0.000 claims abstract description 5
- 230000003647 oxidation Effects 0.000 claims abstract description 5
- 238000007254 oxidation reaction Methods 0.000 claims abstract description 5
- 239000008280 blood Substances 0.000 claims abstract description 4
- 210000004369 blood Anatomy 0.000 claims abstract description 4
- 235000021466 carotenoid Nutrition 0.000 claims abstract description 4
- 150000001747 carotenoids Chemical class 0.000 claims abstract description 4
- IELOKBJPULMYRW-NJQVLOCASA-N D-alpha-Tocopheryl Acid Succinate Chemical compound OC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C IELOKBJPULMYRW-NJQVLOCASA-N 0.000 claims description 3
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims description 3
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims description 3
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims description 3
- 229940099418 d- alpha-tocopherol succinate Drugs 0.000 claims description 3
- 235000010323 ascorbic acid Nutrition 0.000 claims description 2
- 239000011668 ascorbic acid Substances 0.000 claims description 2
- 229960005070 ascorbic acid Drugs 0.000 claims description 2
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 claims 1
- 235000001815 DL-alpha-tocopherol Nutrition 0.000 claims 1
- 239000011627 DL-alpha-tocopherol Substances 0.000 claims 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 claims 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims 1
- 229960000984 tocofersolan Drugs 0.000 claims 1
- 235000019155 vitamin A Nutrition 0.000 claims 1
- 239000011719 vitamin A Substances 0.000 claims 1
- 229940045997 vitamin a Drugs 0.000 claims 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 claims 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 12
- 235000012000 cholesterol Nutrition 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000000843 powder Substances 0.000 description 5
- 239000000725 suspension Substances 0.000 description 5
- 229940088594 vitamin Drugs 0.000 description 4
- 229930003231 vitamin Natural products 0.000 description 4
- 235000013343 vitamin Nutrition 0.000 description 4
- 239000011782 vitamin Substances 0.000 description 4
- 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 3
- 102000015779 HDL Lipoproteins Human genes 0.000 description 3
- 108010010234 HDL Lipoproteins Proteins 0.000 description 3
- 229940042585 tocopherol acetate Drugs 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 102000004895 Lipoproteins Human genes 0.000 description 2
- 108090001030 Lipoproteins Proteins 0.000 description 2
- 235000019486 Sunflower oil Nutrition 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 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 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 150000003254 radicals Chemical class 0.000 description 2
- 239000002600 sunflower oil Substances 0.000 description 2
- 235000001809 DL-alpha-tocopherylacetate Nutrition 0.000 description 1
- 239000011626 DL-alpha-tocopherylacetate Substances 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- UPYKUZBSLRQECL-UKMVMLAPSA-N Lycopene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1C(=C)CCCC1(C)C)C=CC=C(/C)C=CC2C(=C)CCCC2(C)C UPYKUZBSLRQECL-UKMVMLAPSA-N 0.000 description 1
- JEVVKJMRZMXFBT-XWDZUXABSA-N Lycophyll Natural products OC/C(=C/CC/C(=C\C=C\C(=C/C=C/C(=C\C=C\C=C(/C=C/C=C(\C=C\C=C(/CC/C=C(/CO)\C)\C)/C)\C)/C)\C)/C)/C JEVVKJMRZMXFBT-XWDZUXABSA-N 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000007123 defense Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000008297 liquid dosage form Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 235000012661 lycopene Nutrition 0.000 description 1
- OAIJSZIZWZSQBC-GYZMGTAESA-N lycopene Chemical compound CC(C)=CCC\C(C)=C\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C=C(/C)CCC=C(C)C OAIJSZIZWZSQBC-GYZMGTAESA-N 0.000 description 1
- 239000001751 lycopene Substances 0.000 description 1
- 229960004999 lycopene Drugs 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 235000020777 polyunsaturated fatty acids Nutrition 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000002000 scavenging effect Effects 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- ZCIHMQAPACOQHT-ZGMPDRQDSA-N trans-isorenieratene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/c1c(C)ccc(C)c1C)C=CC=C(/C)C=Cc2c(C)ccc(C)c2C ZCIHMQAPACOQHT-ZGMPDRQDSA-N 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Anti-oxidant formulations are disclosed which comprise vitamin E, vitamin C and carotenoids (beta-carotene) in respective amounts effective to assist in delaying oxidation of low density lipoproteins in the blood stream of a human mammal thereby preventing the onset of cardiovascular diseases. Depending on the particular dosage form i.e. liquid or tablet form, the respective concentrations of the active ingredients in the anti-oxidant formulations of the invention are such that the following dosage ranges would be provided per daily dosage i.e. per teaspoon (5 gms) in the case of a liquid form or per capsule in the case of the encapsulated form: Range per dosage form: Vitamin E - 1 to 3,000 mg/day, Vitamin C - 1 to 10,000 mg/day, Beta-carotene 1 to 500 mg/day.
Description
ANTI-OXIDANT FORMULATIONS
The present invention relates to anti-oxidant formulations for assisting in the prevention of cardiovascular diseases, i.e. diseases related to problems affecting the heart and the blood circulation.
It is known that probably the most important predictor of cardiovascular diseases is a high level of cholesterol in the blood. The human bloodstream contains two major forms of lipoproteins namely, high-density lipoproteins and low-density lipoproteins. The high-density lipoproteins counteract the action of the low-density lipoproteins by removing deposits of cholesterol from arteries and by transporting these cholesterol deposits to the liver for subsequent excretion, thus preventing accumulation of cholesterol. High levels of low-density lipoproteins predict the onset of cardiovascular diseases whereas high levels of high-density lipoproteins indicate protection against such diseases. Low-density lipoproteins contain lipids, particularly polyunsaturated fatty acids and cholesterol. Both these fatty acids and cholesterol are prone to oxidation as a result of free radical attack. Having been oxidised, the low-density lipoproteins possess altered properties which can result in damage to the arterial walls.
Anti-oxidant compounds counteract the oxidizing effects on the lipids by scavenging oxygen free radicals. Among these compounds are antioxidant vitamins: vitamin E, vitamin C, and beta-carotene. The level of these essential antioxidant vitamins is, in contrast to other antioxidative defenses, mainly determined by their dietary supply.
sees 17
Published results from in vitro experiments with plasma samples from different human donors indicated thatlow-density lipoprotein resistance against oxidation depends on the total amount of antioxidant vitamins present, namely vitamin E, vitamin C and the carotenoids (beta-carotene and lycopene).
The present invention seeks to provide anti-oxidant formulations containing effective amounts of each vitamin to produce a synergistic effect on the human body.
The present invention accordingly provides anti-oxidant formulations comprising vitamin E, vitamin C and carotenoids (beta-carotene) in respective amounts effective to assist in delaying oxidation of low density lipoproteins in the blood stream of a human mammal thereby preventing the onset of cardiovascular diseases.
Depending on the particular dosage form i.e. liquid or tablet form, the respective concentrations of the active ingredients in the anti-oxidant formulations of the invention are such that the following dosage ranges would be provided per daily dosage i.e. per teaspoon (5 gins) in the case of a liquid form or per capsule in the case of the encapsulated form:
Range per dosage form
Vitamin E to 3,000 mg/day
Beta-carotene to 500 mg/day
The anti-oxidant formulations of the present invention
Vitamin C to 10,000 mg/day i
will now be described more particularly with reference to the following Examples, which show, by way of example only, two embodiments of the anti-oxidant formulations of the invention:
Example 1
Liquid dosage form (oily solution/suspension)
Active ingredients per batch:
Amounts of ingredients per dose
125 mg 235 mg 50 mg 4590 ma
Pure vitamin E acetate (dL-alpha-tocopherol acetate)
Ascorbyl palmitate Beta-carotene 30% oily suspension Sunflower oil
The amount per batch of each ingredient is directly related to the amount per dose multiplied by the number of doses to be prepared from each batch.
Method
The requisite amount of Ascorbyl palmitate is heated to 60°C in the sunflower oil and allowed to infuse. The resulting solution/suspension is cooled to 40°C under nitrogen and the beta-carotene suspension and vitamin E acetate are added. The ingredients are then homogenised. The resultant oily solution/suspension is then poured in storage/dispensing bottles.
Example 2
Capsule dosage form
Active ingredients per batch:
Amounts of ingredients per dose
300 mg
150 mg
150 mg is directly
Ascorbic acid
Beta-carotene 10% water dispersible powder
Vitamin E succinate (d-alpha-tocopherol succinate) (water dispersible powder)
The amount per batch of each ingredient related to the amount per dose multiplied by the number of doses to be prepared from each batch.
The beta-carotene water dispersible powder and vitamin E water dispersible powder are spray dried forms of the oily material which are absorbed onto an inert carrier and are milled to form a cold water dispersible powder.
The requisite amounts of the ingredients are blended, milled and subsequently dispensed into water soluble capsules.
It will of course be understood that the invention is not limited to the specific details described herein, which are given by way of example only, and that various modifications and alterations are possible within the scope of the invention.
MACLACHLAN & DONALDSON, Applicant's Agents,
Merrion Square, DUBLIN 2.
Claims (4)
1. Anti-oxidant formulations comprising vitamin E, 4 vitamin C and carotenoids (beta-carotene) in respective amounts effective to assist in delaying oxidation of low density lipoproteins in the blood stream of a human mammal thereby preventing the onset of cardiovascular diseases.
2. Anti-oxidant formulations according to claim 1, wherein the respective concentration of the active ingredients in the anti-oxidant formulations of the invention are such that the following dosage ranges would be provided per daily dosage i.e. per teaspoon (5 gms) in the case of a liquid form or per capsule in the case of the encapsulated form: Vitamin E Vitamin C Beta-carotene Range per dosage form 1 to 3,000 mg/day 1 to 10,000 mg/day 1 to 500 mg/day
3. Antioxidant formulations according to claim 1 or claim / 2 wherein vitamin E is included in the form of / · dL-alpha-tocopherol or d-alpha-tocopherol succinate; ;/ I vitamin A in the form of beta-carotene and vitamin C in the form of ascorbyl palmitate or ascorbic acid. ’
4. Anti-oxidant formulations substantially as herein described in the Examples.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IES950246 IES950246A2 (en) | 1995-04-05 | 1995-04-05 | Anti-oxidant formulations |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IES950246 IES950246A2 (en) | 1995-04-05 | 1995-04-05 | Anti-oxidant formulations |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IES68517B2 true IES68517B2 (en) | 1996-06-26 |
| IES950246A2 IES950246A2 (en) | 1996-06-26 |
Family
ID=11040709
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IES950246 IES950246A2 (en) | 1995-04-05 | 1995-04-05 | Anti-oxidant formulations |
Country Status (1)
| Country | Link |
|---|---|
| IE (1) | IES950246A2 (en) |
-
1995
- 1995-04-05 IE IES950246 patent/IES950246A2/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| IES950246A2 (en) | 1996-06-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK9A | Patent expired |