# US 2010/0166873 A1 · Eutectic-Based Self-Nanoemulsified Drug Delivery System

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- Number: US 2010/0166873 A1
- Document ID: US20100166873A1
- Status: Published application
- Kind: A1
- Application number: 12/493,406
- Filed: 2009-06-29
- Published: 2010-07-01
- Earliest claimed: 2001-11-14
- Assignees: Jarrow Formulas, Inc.
- Inventors: Mansoor A. Khan; Sami Nazzal
- Web page: https://patentgrep.com/patent/US20100166873A1

## CPC

- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- 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 31/12: Ketones
- A61K 31/355: Tocopherols, e.g. vitamin E
- 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
- A61P 39/06: Free radical scavengers or antioxidants
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/4858: {Organic compounds}
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A eutectic-based self-nanoemulsified drug delivery system (SNEDDS) is formulated from polyoxyl 35 castor oil (Cremophor), medium chain mono- and diglycerides (capmul), essential oils, and a pharmacologically effective drug. The preferred pharmacologically effective drug is a poorly water soluble drug, such as ubiquinone (CoQ10). The SNEDDS can be further incorporated into a powder to produce a solid dosage form. The solid dosage form contains the SNEDDS, a copolymer of vinylpyrrolidone and vinyl acetate (Kollidon VA 64), maltodextrin, and microcrystalline cellulose (MCC).

## Claims

### Claim 1

Method of making a self-nanoemulsified drug delivery system (SNEDDS) comprising the steps of:
(a) admixing a pharmacologically effective drug and a sufficient amount of a volatile essential oil to reduce the melting point of to 37° C. or below;
(b) warming the mixture to 37° C. to solubilize the drug; and
(c) admixing at least one surfactant.

### Claim 2 (depends on 1)

The method of claim 1, wherein step (c) further comprises the addition of a co-surfactant.

### Claim 3 (depends on 2)

The method of claim 2, wherein the surfactant is a high HLB, and the co-surfactant is a low HLB surfactant.

### Claim 4 (depends on 2)

The method of claim 2, wherein the ratio of surfactant to co-surfactant is at least about 0.5.

### Claim 5

A method of forming a compressible SNEDDS powder comprising the steps of:
(a) admixing a pharmacologically effective drug and a sufficient amount of a volatile essential oil to reduce the melting point of the drug to 37° C. or below;
(b) warming the mixture to 37° C. to solubilizer the drug;
(c) admixing at least one surfactant to form an emulsion;
(d) cooling the emulsion from (c) to form a SNEDDS paste;
(e) admixing the SNEDDS paste and a pyrrolidone copolymer;
(f) admixing maltodextrin and the mixture from (e) to form granules; and
(g) admixing microcrystalline cellulose (MCC) and the granules from (f).

### Claim 6 (depends on 5)

The method of claim 5, wherein step (c) further comprises the addition of a co-surfactant.

### Claim 7 (depends on 6)

The method of claim 6, wherein the ratio of surfactant to co-surfactant is at least 0.5.

### Claim 8 (depends on 7)

The method of claim 7, wherein the surfactant is a high HLB, and the co-surfactant is a low HLB surfactant.

### Claim 9 (depends on 5)

The method of claim 5, wherein the copolymer is a vinylpyrrolidone and vinyl acetate copolymer.

### Claim 10 (depends on 5)

A compressed, solid dosage form comprising the powder of claim 5.

### Claim 11 (depends on 5)

The method of claim 5, wherein the amount of copolymer added is from about 3% to about 35% by weight relative to the weight of the SNEDDS paste.

### Claim 12 (depends on 5)

The method of claim 5, wherein the amount of MCC added is from about 11% to about 47% by weight relative to the weight of the SNEDDS paste.

### Claim 13 (depends on 5)

The method of claim 5, wherein the amount of maltodextrin added is from about 35% to about 82% by weight relative to the weight of the SNEDDS paste.

### Claim 14 (depends on 5)

The method of claim 5, wherein the amount of a pharmacologically effective drug is sufficient to effectuate a pharmacological effect.

### Claim 15 (depends on 5)

The method of claim 5, wherein the amount of a pharmacologically effective drug is from about 19% to about 26% by weight.