# US 11,304,900 B1 · Transparent colloidal vitamin supplement blend

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- Number: US 11,304,900 B1
- Document ID: US11304900B1
- Status: Granted
- Kind: B1
- Application number: 16/902,842
- Filed: 2020-06-16
- Granted: 2022-04-19
- Earliest claimed: 2017-12-08
- Assignees: Quicksilver Scientific, Inc.
- Applicants: Quicksilver Scientific, Inc.
- Inventors: Christopher W. Shade; Steven Tieu
- Web page: https://patentgrep.com/patent/US11304900B1

## CPC

- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A23L 33/15: Vitamins
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 9/1277: Preparation processes; Proliposomes
- A61K 31/015: carbocyclic
- A61K 31/07: Retinol compounds, e.g. vitamin A (retinoic acids A61K31/203)
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/205: Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
- A61K 31/355: Tocopherols, e.g. vitamin E
- A61K 31/375: Ascorbic acid, i.e. vitamin C; Salts thereof
- A61K 31/4415: Pyridoxine, i.e. Vitamin B6 (pyridoxal phosphate A61K31/675)
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61K 31/51: Thiamines, e.g. vitamin B1
- A61K 31/525: Isoalloxazines, e.g. riboflavins, vitamin B2
- A61K 31/593: 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
- A61K 31/714: Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)

## Abstract

An aqueous, intra-oral, transparent nanoemulsion blend in the form of a stable dispersion delivers both oil- and water-soluble components of a vitamin supplement in the desired concentrations to the cells of a mammal when orally administered. The transparent nanoemulsion blend includes at least two different bilayer water-core liposome components and at least one monolayer surfactant bound particle component. The transparent nanoemulsion blend optionally may include a micelle formed from phosphatidylcholine (PC).

## Claims

### Claim 1

An aqueous, intra-oral, transparent nanoemulsion blend for delivering oil- and water-soluble components of a vitamin supplement to the cells of a mammal when orally administered, the blend comprising:
Vitamin C and a Vitamin C delivery means for delivering the Vitamin C to the bloodstream of the mammal, where the Vitamin C delivery means comprises at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, where the Vitamin C delivery means further comprises ethanol and glycerin and where a capsule interior of the Vitamin C delivery means comprises the Vitamin C dissolved in water;
Vitamin B complex and a Vitamin B complex delivery means for delivering the Vitamin B complex to the bloodstream of the mammal, where the Vitamin B complex delivery means comprises at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, where the Vitamin B complex delivery means further comprises ethanol and water and where a capsule interior of the Vitamin B complex delivery means comprises the Vitamin B complex dissolved in water-;
at least one oil-soluble vitamin;
at least one oil-soluble carotenoid; and
an oil-soluble vitamin and oil-soluble carotenoid delivery means for delivering the at least one oil-soluble vitamin and the at least one oil-soluble carotenoid to the bloodstream of the mammal,
where the oil-soluble vitamin and oil-soluble carotenoid delivery means comprises at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, and
where the blend has an average particle diameter from 10 to 60 nanometers and is a stable dispersion.

### Claim 2 (depends on 1)

The blend of claim 1, where when the blend is administered intra-orally to the mammal, the Vitamin C delivery means, the Vitamin B complex delivery means, and the oil-soluble vitamin and oil-soluble carotenoid delivery means in combination deliver at least 60% of the Vitamin C, the Vitamin B complex, the at least one oil-soluble vitamin, and the at least one oil-soluble carotenoid to the bloodstream of the mammal by transmucosal absorption through the mouth of the mammal.

### Claim 3 (depends on 1)

The blend of claim 1, where when the blend is administered intra-orally to the mammal, the Vitamin C delivery means, the Vitamin B complex delivery means, and the oil-soluble vitamin and oil-soluble carotenoid delivery means in combination deliver at least 80% of the Vitamin C, the Vitamin B complex, the at least one oil-soluble vitamin, and the at least one oil-soluble carotenoid to the bloodstream of the mammal by transmucosal absorption through the mouth of the mammal.

### Claim 4 (depends on 1)

The blend of claim 1, where the Vitamin C comprises sodium ascorbate and comprises from 100 to 140 mg per 5 mL of the blend.

### Claim 5 (depends on 1)

The blend of claim 1, where the Vitamin B complex delivery means further comprises anhydrous betaine.

### Claim 6 (depends on 5)

The blend of claim 5, where the anhydrous betaine comprises from 20 to 30 mg per 5 mL of the blend.

### Claim 7 (depends on 1)

The blend of claim 1, where the Vitamin B complex is a methyl B complex comprising Vitamins B1-B3, B5-B7, B9, and B12.

### Claim 8 (depends on 1)

The blend of claim 1, where the Vitamin B complex comprises from 40 to 100 mg per 5 mL of the blend.

### Claim 9 (depends on 1)

The blend of claim 1, where the Vitamin B complex delivery means further comprises milk thistle extract.

### Claim 10 (depends on 1)

The blend of claim 1, where the at least one oil-soluble vitamin comprises at least one tocotrienol isomer of Vitamin E and at least one tocopherol isomer of Vitamin E.

### Claim 11 (depends on 10)

The blend of claim 10, where the at least one tocotrienol isomer of Vitamin E and the at least one tocopherol isomer of Vitamin E comprise from 20 to 50 mg per 5 mL of the blend.

### Claim 12 (depends on 10)

The blend of claim 10, where the at least one tocotrienol isomer of Vitamin E and the at least one tocopherol isomer of Vitamin E are present in a ratio from 1:0.5 to 1:3.

### Claim 13 (depends on 1)

The blend of claim 1, where the at least one oil-soluble vitamin comprises Vitamin K1 and Vitamin K2.

### Claim 14 (depends on 13)

The blend of claim 13, where the Vitamin K1 comprises from 35 to 55 mcg per 5 mL of the blend and the Vitamin K2 comprises from 35 to 55 mcg per 5 mL of the blend.

### Claim 15 (depends on 1)

The blend of claim 1, where the at least one oil-soluble vitamin comprises Vitamin A and Vitamin D3.

### Claim 16 (depends on 15)

The blend of claim 15, where the Vitamin A includes from 10% to 20% by weight beta carotene.

### Claim 17 (depends on 1)

The blend of claim 1, where the at least one oil-soluble carotenoid is selected from the group consisting of lutein, zeaxanthin, lycopene, and combinations thereof.

### Claim 18 (depends on 1)

The blend of claim 1 comprising from 3.2 to 7.9 milligrams of the at least one oil-soluble carotenoid in 5 mL of the blend.

### Claim 19 (depends on 1)

The blend of claim 1, where the at least one oil-soluble carotenoid comprises from 2 mg to 6 mg of lutein per 5 mL of the blend.

### Claim 20 (depends on 1)

The blend of claim 1, where the at least one oil-soluble carotenoid comprises from 0.7 to 1.0 mg of lycopene per 5 mL of the blend.

### Claim 21 (depends on 1)

The blend of claim 1, where the at least one oil-soluble carotenoid comprises from 0.5 mg to 0.9 mg of zeaxanthin per 5 mL of the blend.

### Claim 22 (depends on 1)

The blend of claim 1, where the Vitamin C delivery means, the Vitamin B complex delivery means, and the oil-soluble vitamin and oil-soluble carotenoid delivery means are particles having average particle diameters from 10 nm to 50 nm.

### Claim 23 (depends on 1)

The blend of claim 1, further comprising a liquid carrier for carrying the Vitamin C delivery means, the Vitamin B complex delivery means, and the oil-soluble vitamin and oil-soluble carotenoid delivery means.

### Claim 24 (depends on 23)

The blend of claim 23, where the liquid carrier comprises water, glycerin, and ethanol.

### Claim 25 (depends on 24)

The blend of claim 24, where the liquid carrier comprises an ethanol to glycerin ratio from 1:1 to 1:4.

### Claim 26 (depends on 24)

The blend of claim 24, where the ratio of the at least one oil-soluble carotenoid to the ethanol is from 1:63 to 1:313 in the blend.

### Claim 27

An aqueous, intra-oral, transparent nanoemulsion blend for delivering oil- and water-soluble components of a vitamin supplement to the cells of a mammal when orally administered, the blend comprising:
at least two different bilayer water-core liposomes, where
a first bilayer water-core liposome comprises at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, ethanol, and glycerin, where a capsule interior of the first bilayer water-core liposome comprises Vitamin C dissolved in water, and
a second bilayer water-core liposome comprising at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, a first polyethylene glycol surfactant form, ethanol, and glycerin, where a capsule interior of the second bilayer water-core liposome comprises a Vitamin B complex dissolved in water;
at least one monolayer surfactant bound particle, where
the at least one monolayer surfactant bound particle comprises at least one amphiphilic fat chosen from glycerophospholipids, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidic acid, a second polyethylene glycol surfactant form, an associating oil, oil-soluble vitamins, and oil-soluble carotenoids; and
a continuous phase comprising water, glycerin, and ethanol,
where the first bilayer water-core liposome, the second bilayer water-core liposome, and the at least one monolayer surfactant bound particle have average particle diameters from 10 to 60 nanometers in the continuous phase, and,
where the blend is a stable dispersion.

### Claim 28 (depends on 27)

The blend of claim 27, where the Vitamin C comprises sodium ascorbate and comprises from 100 to 140 mg per 5 mL of the blend.

### Claim 29 (depends on 27)

The blend of claim 27, where the capsule interior of the second bilayer water-core liposome further comprises anhydrous betaine.

### Claim 30 (depends on 29)

The blend of claim 29, where the anhydrous betaine comprises from 20 to 30 mg per 5 mL of the blend.

### Claim 31 (depends on 27)

The blend of claim 27, where the Vitamin B complex is a methyl B complex comprising Vitamins B1-B3, B5-B7, B9, and B12.

### Claim 32 (depends on 27)

The blend of claim 27, where the Vitamin B complex comprises from 40 to 100 mg per 5 mL of the blend.

### Claim 33 (depends on 27)

The blend of claim 27, where the capsule interior of the second bilayer water-core liposome further comprises milk thistle extract and EDTA.

### Claim 34 (depends on 27)

The blend of claim 27, where the oil-soluble vitamins of the at least one monolayer surfactant bound particle comprise at least one tocotrienol isomer of Vitamin E and at least one tocopherol isomer of Vitamin E.

### Claim 35 (depends on 34)

The blend of claim 34, where the at least one tocotrienol isomer of Vitamin E and the at least one tocopherol isomer of Vitamin E comprise from 20 to 50 mg per 5 mL of the blend.

### Claim 36 (depends on 34)

The blend of claim 34, where the at least one tocotrienol isomer of Vitamin E and the at least one tocopherol isomer of Vitamin E are present in a ratio from 1:0.5 to 1:3.

### Claim 37 (depends on 27)

The blend of claim 27, where the oil-soluble vitamins of the at least one monolayer surfactant bound particle comprise Vitamin K1 and Vitamin K2.

### Claim 38 (depends on 37)

The blend of claim 37, where the Vitamin K1 comprises from 35 to 55 mcg per 5 mL of the blend and the Vitamin K2 comprises from 35 to 55 mcg per 5 mL of the blend.

### Claim 39 (depends on 27)

The blend of claim 27, where the oil-soluble vitamins of the at least one monolayer surfactant bound particle comprise Vitamin A and Vitamin D3.

### Claim 40 (depends on 39)

The blend of claim 39, where the Vitamin A includes from 10% to 20% by weight beta carotene.

### Claim 41 (depends on 27)

The blend of claim 27, where the oil-soluble carotenoids are selected from the group consisting of lutein, zeaxanthin, lycopene, and combinations thereof.

### Claim 42 (depends on 27)

The blend of claim 27, where the oil-soluble carotenoids comprise from 3.2 to 7.9 mg per 5 mL of the blend.

### Claim 43 (depends on 27)

The blend of claim 27, where the oil-soluble carotenoids comprise from 2 to 6 mg of lutein per 5 mL of the blend.

### Claim 44 (depends on 27)

The blend of claim 27, where the oil-soluble carotenoids comprise from 0.7 to 1.0 mg of lycopene per 5 mL of the blend.

### Claim 45 (depends on 27)

The blend of claim 27, where the oil-soluble carotenoids comprise from 0.5 to 0.9 mg of zeaxanthin per 5 mL of the blend.

### Claim 46 (depends on 27)

The blend of claim 27, where the associating oil is selected from the group consisting of medium chain triglycerides, citrus oil, and combinations thereof.

### Claim 47 (depends on 27)

The blend of claim 27, where the at least one amphiphilic fat includes at least 30% phosphatidylcholine by weight.

### Claim 48 (depends on 27)

The blend of claim 27, where the first polyethylene glycol surfactant form is selected from the group consisting of tocopheryl polyethylene glycol succinate 1000, polysorbate 40, polysorbate 60, polysorbate 80, and combinations thereof.

### Claim 49 (depends on 27)

The blend of claim 27, where the first polyethylene glycol surfactant form is tocopheryl polyethylene glycol succinate 1000.

### Claim 50 (depends on 27)

The blend of claim 27, where the second polyethylene glycol surfactant form is selected from the group consisting of tocopheryl polyethylene glycol succinate 1000, polysorbate 40, polysorbate 60, polysorbate 80, and combinations thereof.

### Claim 51 (depends on 27)

The blend of claim 27, where the second polyethylene glycol surfactant form is tocopheryl polyethylene glycol succinate 1000.

### Claim 52 (depends on 27)

The blend of claim 27, where the first and the second polyethylene glycol surfactant forms are the same.

### Claim 53 (depends on 27)

The blend of claim 27, where the first and second bilayer water-core liposomes and the at least one monolayer surfactant bound particle have average particle diameters from 10 to 50 nm.

### Claim 54 (depends on 27)

The blend of claim 27, where the continuous phase comprises an ethanol to glycerin ratio from 1:1 to 1:4.

### Claim 55 (depends on 27)

The blend of claim 27, where the ratio of the oil-soluble carotenoids to the ethanol is from 1:63 to 1:313 in the blend.

### Claim 56 (depends on 27)

The blend of claim 27 where at least 60% of the Vitamin C, the Vitamin B complex, the oil-soluble vitamins, and the oil-soluble carotenoids are delivered to a bloodstream by transmucosal absorption through the mouth, when 0.5 mL of the blend is intra-orally administered to a human for a mouth-residency time of 2 minutes.

### Claim 57 (depends on 27)

The blend of claim 27 where at least 80% of the Vitamin C, the Vitamin B complex, the oil-soluble vitamins, and the oil-soluble carotenoids are delivered to a bloodstream by transmucosal absorption through the mouth, when 0.5 mL of the blend is intra-orally administered to a human for a mouth-residency time of 2 minutes.
