# US 10,478,417 B2 · Formulation for effective tocotrienol delivery

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- Number: US 10,478,417 B2
- Document ID: US10478417B2
- Status: Granted
- Kind: B2
- Application number: 16/205,433
- Filed: 2018-11-30
- Published: 2019-04-18
- Granted: 2019-11-19
- Earliest claimed: 2014-11-25
- Assignees: Kl-Kepong Oleomas Sdn Bhd
- Applicants: Kl-Kepong Oleomas Sdn Bhd
- Inventors: Chee Wai Fong; Yee Wei Ung; Jordan Todorov Petkov
- Web page: https://patentgrep.com/patent/US10478417B2

## CPC

- A61K 31/355: Tocopherols, e.g. vitamin E
- A23L 33/15: Vitamins
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- A61K 9/4841: {Filling excipients; Inactive ingredients}
- A61K 9/4858: {Organic compounds}
- A61K 9/4875: {Compounds of unknown constitution, e.g. material from plants or animals (oils, fats, waxes, shellac A61K9/4858)}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

The present invention disclosed a formulation in the form of self-emulsifying drug delivery formulation for improved delivery of tocotrienols comprising a fat-soluble compound, at least one emulsifier, and an oil carrier. The formulation shows an improved bioavailability of tocotrienols.

## Claims

### Claim 1

A method of delivering a tocotrienol to a subject in need of supplementing an intake of a daily allowance of a fat-soluble nutrient, the method comprising administering to the subject a dietary supplement comprising a self-emulsifying formulation comprising a fat-soluble compound selected from tocotrienols and derivatives thereof, wherein the amount of the fat-soluble compound is about 10% to about 50%, by weight of the formulation; two emulsifiers each selected from the group consisting of nonionic surfactants, wherein the emulsifiers are sorbitan monolaurate and polyoxyethylene sorbitan 20 monooleate (Polysorbate 80), wherein the amount of emulsifiers is about 15% to about 45%, by weight of the formulation, wherein the weight ratio of said sorbitan monolaurate to Polysorbate 80 is about 1:1 to about 1:20; and
an oil carrier selected from the group consisting of glycerides, wherein the amount of oil carrier is about 6% to about 56%, by weight of the formulation.

### Claim 2 (depends on 1)

The method as claimed in claim 1, wherein the weight ratio of said sorbitan monolaurate to Polysorbate 80 is about 1:2 to about 1:8.

### Claim 3 (depends on 1)

The method as claimed in claim 1, wherein the fat-soluble compound is tocotrienol.

### Claim 4 (depends on 1)

The method as claimed in claim 1, wherein the oil carrier is comprises glycerol trioleate (GTO) oil.

### Claim 5 (depends on 4)

The method as claimed in claim 4, wherein said glycerol trioleate (GTO) oil includes the main triglycerides (TG) oftriolein (OOO, C18:1).

### Claim 6 (depends on 5)

The method as claimed in claim 5, wherein said oil carrier comprises of the amount of triolein (OOO, C18:1) about 55% to about 99% by weight of said GTO oil.

### Claim 7 (depends on 5)

The method as claimed in claim 5, wherein said oil carrier comprises of the amount of triolein (OOO, C18:1) about 65% to about 85% by weight of said GTO oil.

### Claim 8 (depends on 1)

The method as claimed in claim 1 further comprising fatty acid selected from the group consisting of oleic acid, palmitic acid, stearic acid and mixtures thereof.

### Claim 9 (depends on 1)

The method as claimed in claim 1, wherein the formulation is made into powder form, tablet or filled into a gelatin capsule.

### Claim 10 (depends on 9)

The method as claimed in claim 9, wherein said formulation is filled into a gelatin capsule, in which said gelatin capsule is a hard-shelled gelatin capsule or a soft-shelled gelatin capsule.

### Claim 11 (depends on 1)

The method as claimed in claim 1, wherein the formulation is in a form for oral delivery.

### Claim 12 (depends on 1)

The method as claimed in claim 1, wherein the step of administering is performed orally.

### Claim 13 (depends on 1)

The method as claimed in claim 1, wherein the step of administering is performed parenterally, rectally or topically.