Emulsion of Carotenoids and Ocular Antioxidants

Abstract

A daily liquid supplement for ocular and body health containing at least one of lutein, zeaxanthin, meso-zeaxanthin and astaxanthin for a human subject for nutritionally supplementing macular pigments is disclosed. The micronized nutrients in a lipid based emulsion are more efficiently absorbed into the bloodstream than conventional supplement formulations resulting in higher serum levels and increased macular pigment.

Claims

1. A lipophilic formulation for nutritionally supplementing a human subject, the formulation comprising: a) hydrophobic carotenoids lutein, zeaxanthin, and meso-zeaxanthin; b) at least one hydrophilic ocular antioxidant selected from the group consisting of bilberry fruit extract and alpha-lipoic acid; c) an aqueous solvent; d) a wetting agent for enhancing dispersal of said hydrophobic carotenoid within said aqueous solvent, said wetting agent being a water-dispersible food grade lysophospholipid; e) an emulsifier for emulsifying said hydrophobic carotenoid within said aqueous solvent, said emulsifier being a food grade hydrophilic non-ionic surfactant; f) a stabilizer for stabilizing the emulsion for at least several months, said stabilizer being a food grade natural product gum; g) an absence of more than a trace quantity of hydrophobic solvent; h) an absence of more than a trace quantity of protein; and i) an oil phase comprising at least 50% of a triglyceride having a fatty acid chain length of 12 carbon atoms or greater; said hydrophobic carotenoid and said hydrophilic ocular antioxidant being combined with said aqueous solvent, together with said wetting agent, said emulsifier, said stabilizer and said oil phase by dispersal and emulsification for forming an emulsion for nutritionally supplementing macular pigments.

2. The formulation of claim 1 wherein the triglyceride is a long chain triglyceride selected from at least one of the group consisting of fish oil, cod liver oil, blubber, lard, tallow, schmaltz, butter fat, canola oil, castor oil, cocoa butter, coconut oil, coffee see oil, corn oil, cotton seed oil, evening primrose oil, grapeseed oil, flax seed oil, menhaden oil, mustard seed oil, olive oil, palm oil, palm kernel oil, peanut oil, poppy seed oil, rapeseed oil, rice bran oil, safflower oil, sesame oil, soybean oil, hazelnut oil and wheat germ oil.

3. The formulation of claim 2 wherein said wetting agent is a partially hydrolyzed de-oiled lecithin.

4. The formulation of claim 3 wherein the partially hydrolyzed de-oiled lecithin is derived from soy.

5. The formulation of claim 2 wherein said emulsifier is a polyethylene glycol sorbitan fatty acid mono-ester.

6. The formulation of claim 5 wherein said emulsifier is polysorbate 80.

7. The formulation of claim 2 wherein said stabilizer is selected from the group of natural gums consisting of pectin, xanthan, alginate, and guar gum.

8. The formulation of claim 7 wherein said stabilizer is xanthan gum.

9. The formulation of claim 2 wherein said aqueous solvent including water, a buffering agent, and a co-solvent for lowering interfacial tension of the aqueous phase and enhancing the activity of said wetting agent with respect to dispersal of said hydrophobic carotenoid within said aqueous solvent, the co-solvent being selected from the group consisting of an alcohol and a polyol.

10. The formulation of claim 9 wherein the co-solvent is glycerin.

11. The formulation of claim 9 wherein the buffering agent is a salt of citric acid.

12. The formulation of claim 10 wherein the water is purified by reverse osmosis.

13. The formulation of claim 2 further comprising a natural flavor and a sweetening agent.

14. The formulation of claim 2 further comprising a water soluble nutritional supplement selected from the group consisting of acetyl-L carnitine, biotin, coenzyme Q10, folic acid, L-taurine, N-acetyl cysteine, quercetin, vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B12, and vitamin C, said soluble nutritional supplement being admixed into the emulsion.

15. The formulation of claim 2 further comprising a hydrophobic nutritional supplement selected from the group consisting of lycopene, vitamin D3, and vitamin E, said hydrophobic nutritional supplement being admixed into the emulsion.

16. The formulation of claim 2 further comprising a mineral selected from salts of the group consisting of calcium, chromium, copper, magnesium manganese, molybdenum, potassium, selenium, and zinc; said mineral being admixed into the emulsion.

17. The formulation of claim 2 wherein the emulsion being characterized by having hydrophobic particles with an average diameter of 0.1-100 micrometers.

18. A method of formulating a nutritional supplement for the macular pigments of a human subject, the method comprising: a) preparing a first Preblend mixture; b) preparing a second Preblend mixture; c) slowly adding the first Preblend to the second Preblend until the pH specification is achieved, preferably 3.9-4.3 for stability of the preservative system and taste; and d) mixing with high sheer for a minimum of 6 hrs, wherein an emulsion is formed.

19. The method of claim 18, wherein the first Preblend mixture consists of a mixture prepared according to the following steps: 1) combining Water 87 wt % and Glycerin 12.6 wt % slowly; 2) adding Xanthan Gum 0.5 wt % to the product of step 1) under high speed mixing to make a slurry; 3) adding polysorbate 80 3.7 wt % to the slurry of step 2); 4) adding Vitamin E (mixed tocopherols, including gamma-tocopherol), Vitamin D, Lumega Carotenoid Blend, Lycopene, Quercetin, Astaxanthin and Lecithin one at a time to the product of step 3), mixing with high sheer for 20 minutes or until homogeneous; 5) adding remaining fat solubles one at a time; and 6) adding water solubles one at a time.

20. The method of claim 18, wherein the second Preblend mixture consists of a mixture prepared by combining Water and Citric Acid 0.5 wt % and further mixing slowly until there are no visible solids.

21. A kit comprising: (a) a box; the box further comprising a plurality of first containers, each container containing a once daily dose of a medicament for supplementing macular carotenoids, the medicament being an aqueous/hydrophobic emulsion including carotenoids, bilberry fruit extract, and alpha-lipoic add, each of said containers being sealed for preventing oxidation of the medicament therein; and (b) at least one second container containing a plurality of once daily doses of omega fatty acids, said first and second containers being packed as a kit within said box for supplying a plurality of once daily doses of the medicament in combination with but separate from the omega fatty acids.

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0062] FIG. 1 illustrates the increase in patient MPOD following administration of the formulation of the present invention.

[0063] FIG. 2 illustrates the efficiency of absorbency of the formulation of the present invention versus solid form supplements.

[0064] FIG. 3 illustrates the closed kit of the present invention.

[0065] FIG. 4 illustrates the open kit and contents of said kit of the present invention.

DETAILED DESCRIPTION OF THE DRAWINGS

[0066] FIG. 1 is a graph showing the average increase in MPOD of 872 patients taking the formulation of the present invention as measured using the MAPCATsf at weeks 14, 30, 42 and 60 of administration.

[0067] FIG. 2 is a graph showing the percentage of micronutrient absorption of the liquid formulation of the present invention in patient serum collected on days 3, 6 and 9 of administration compared to the percentage absorption of solid form supplements, i.e. tablets and capsules.

[0068] FIG. 3 illustrates the kit 1 containing the packaged emulsion of the present invention.

[0069] FIG. 4 illustrates the kit 1 of FIG. 3, having 28 sealed bottles 2 filled with the emulsion to be administered once daily, one bottle (container) 3 containing at least 28 omega fatty acid capsules, two spacers 4, and an instruction/Information insert (shown already inside box). The kit contains a 28 day supply of the emulsion and the omega fatty acid capsules, i.e., a 4 week supply.

DETAILED DESCRIPTION OF THE INVENTION

[0070] The following examples are intended to illustrate the invention by way of example only, and are not intended to limit the scope of the invention.

Example 1

Determination of Daily Dosage

[0071] The appropriate dosage of the emulsion for daily administration to a patient is determined by first obtaining a baseline measurement of the patient's Macular Pigment Optical Density (MPOD) using the MAPCATsf. The baseline measurement obtained will determine the correct dosage of the emulsion to administer to a specific patient resulting in enhanced assayable macular pigment levels.

Example 2

Emulsion Preparation

[0072] In carrying out the present invention, the total daily serving size in weight is 67239.804 mg/serving comprised of approximately 48685.000 mg Water (Reverse Osmosis), 315.000 mg Water (Reverse Osmosis) and 200.000 mg Xanthan Gum (Clear Gel).

[0073] The packaged emulsion of the present invention is formulated according to the following protocol:

Preblend A:

[0074] 1. Combine Water 87 wt % and Glycerin 12.6 wt % slowly. Next add Xanthan Gum 0.5 wt % under high speed mixing to make a slurry. Add polysorbate 80 3.7 wt %. [0075] 2. Add Vitamin E (mixed tocopherols, including gamma-tocopherol), Vitamin D, Lumega Carotenoid Blend, Lycopene, Quercetin, Astaxanthin and Lecithin one at a time to Preblend A. Mix with high sheer for 20 minutes or until homogeneous. [0076] 3. Add remaining fat solubles one at a time [0077] 4. Add water solubles one at a time

Preblend B:

[0078] 1. Combine Water, Citric Acid 0.5 wt % and mix slowly until there are no visible solids.

[0079] Slowly add Preblend A to Preblend B until the pH specification is achieved, preferably 3.9-4.3 for stability of the preservative system and taste. Mix with high sheer for a minimum of 6 hrs prior to filling.

Example 3

[0080] Table 1 shows an example LUMEGA-Z emulsion formulation.

TABLE-US-00001 TABLE 1 LUMEGA-Z Formula Specification: Amount per % Daily serving Value Vitamin C 500 mg 833% Thiamin 1.5 mg 100% Riboflavin 1.7 mg 100% Niacin 20 mg 100% Vitamin B6 10 mg 500% Folate 800 mcg 200% Vitamin B12 1000 mcg 16667% Vitamin D3 2000 IU 500% Vitamin E 200 IU 665% Biotin 100 mcg 33% Pantothenic Acid 10 mg 100% Calcium 250 mg 25% Magnesium 100 mg 25% Zinc 25 mg 167% Selenium 70 mcg 100% Copper 3 mg 150% Manganese 2 mg 100% Chromium 120 mcg 100% Molybdenum 75 mcg 100% NAC (N-acetyl-cysteine) 500 mg * Proprietary Ocular Antioxidant Blend 200 mg * (billberry fruit extract 4:1, alpha- kipoic acid) Acetyl-L-Carnitine 500 mg * Taurine 500 mg * Quercetin 100 mg * CoQ10 50 mg * Lycopene 500 mcg * Lutein 15 mg * Zeaxanthin 3 mg * Meso-Zeaxanthin 10 mg * Astaxanthin 1000 mcg * * Daily value not established.

Example 4

Results of Lumega-Z Administration to Human Subject

[0081] The total number of patients that participated in the study was 872. Patients then returned after weeks 14, 30, 42 and 60 of Lumega-Z administration for retesting on the MAPCATsf.

[0082] The results dearly showed that the formula was effective on all patients, without exception, by increasing patient MPOD (FIG. 1). There were few patients who only showed an Increase of 15-18%, and it is now presumed that these individuals may have more difficulty absorbing the carotenoids or they were not taking the Lumega-Z every day as indicated. The remaining patients showed increases in MPOD ranging from 20% to 30%.

Example 5

[0083] Analysis of Efficiency of Absorption for Lumega-Z v. Solid Form Supplements

[0084] The efficiency of absorption (EOA) of lipid based micronized liquid, Lumega-Z, was compared with solid form supplements. Two products were compared to the Lumega-Z formulation: 1) a widely used multi-vitamin in tablet form (tablet); and 2) a commonly prescribed over the counter products used for patients diagnosed with macular degeneration in capsule form (capsule).

[0085] The total number of subjects for the analysis was twelve: four subjects received Lumega-Z; four subjects received the multi-vitamin tablets; and four subjects received the AMD capsule. Serum samples were collected from each subject on day 3, 6 and 9 and concentrations of key micronutrients represented in all administered forms were quantified by high performance liquid chromatography (HPLC).

[0086] The results surprisingly showed that the subjects taking Lumega-Z demonstrated an EOA of 90% compared to 32% and 39% for the tablet and capsule, respectively (FIG. 2). These data show that when taken as a dietary supplement Lumega-Z may significantly increase patient MPOD over time resulting in the prevention of macular degeneration and/or the correction of atypical macular pigment distribution. These data also show that the formulation of the present invention is superior to similar solid form supplements currently available and is more efficient at delivering the necessary micronutrients to the human body.

[0087] It will be appreciated that details of the foregoing embodiments, given for purposes of illustration, are not to be construed as limiting the scope of this invention. Although several embodiments of this invention have been described in detail above, those skilled in the art will readily appreciate that many modifications are possible in the exemplary embodiments without materially departing from the novel teachings and advantages of this invention. Accordingly, all such modifications are intended to be included within the scope of this invention, which is defined in the following claims and all equivalents thereto. Further, it is recognized that many embodiments may be conceived that do not achieve all of the advantages of some embodiments, particularly of the preferred embodiments, yet the absence of a particular advantage shall not be construed to necessarily mean that such an embodiment is outside the scope of the present invention.