IES950246A2

IES950246A2 - Anti-oxidant formulations

Info

Publication number: IES950246A2
Authority: IE
Inventors: Diarmaid Joseph Long
Original assignee: Diarmaid Joseph Long
Priority date: 1995-04-05
Filing date: 1995-04-05
Publication date: 1996-06-26
Also published as: IES68517B2

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

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. ~ OPEN TCPD·· SECTION 2b Ahi. , 23 JNL. No... j.W. - .OF V 950246 Published results from in vitro experiments with plasma samples from different human donors indicated that low-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 gms) 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 Vitamin C to 10,000 mg/day Beta-carotene to 500 mg/day The anti-oxidant formulations of the present invention 950246 - 3 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 incrredients per batch: Amounts of ingredients Pure vitamin E acetate per dose (dL-alpha-tocopherol acetate) 125 mg Ascorbyl palmitate 235 mg Beta-carotene 30% oily suspension 50 mg Sunflower oil 4590 mg 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. 950246 Example 2 Capsule dosage form Active ingredients per batch: Amounts of ingredients per dose Ascorbic acid Beta-carotene 10% water dispersible 300 mg powder Vitamin E succinate (d-alpha-tocopherol succinate) (water dispersible powder) 150 mg 150 mg 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.

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. 950246 - 5 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,

Claims

CLAIMS :

1. 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.

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; 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.