# US 11,077,067 B2 · Minimizing agglomeration, aeration, and preserving the coating of pharmaceutical compositions comprising ibuprofen

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- Number: US 11,077,067 B2
- Document ID: US11077067B2
- Status: Granted
- Kind: B2
- Application number: 17/008,108
- Filed: 2020-08-31
- Published: 2020-12-17
- Granted: 2021-08-03
- Earliest claimed: 2019-02-22
- Assignees: Catalent U.K. Swindon Zydis Limited
- Applicants: Catalent U.K. Swindon Zydis Limited
- Inventors: Rosaleen McLaughlin; Simon Andrew Martyn Howes; Craig Wheadon; Jonathon Whitehouse; Adam Parker
- Web page: https://patentgrep.com/patent/US11077067B2

## CPC

- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/5073: {having two or more different coatings optionally including drug-containing subcoatings}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 9/2081: {with microcapsules or coated microparticles according to A61K9/50}
- A61K 9/2095: {Tabletting processes}
- A61K 9/501: {Inorganic compounds}
- A61K 9/5015: {Organic compounds, e.g. fats, sugars}
- A61K 9/5063: {Compounds of unknown constitution, e.g. material from plants or animals (oils, fats, waxes, shellac A61K9/5015)}
- A61K 9/5089: {Processes}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 47/02: Inorganic compounds
- 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 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- 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)
- 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)

## Abstract

Provided are pharmaceutical compositions and methods for preparing pharmaceutical compositions comprising Ibuprofen using solventless mixing methods. Excess coating material that is not bound to coated Ibuprofen may be removed by a sieving process. Coating and dosing ratios can also be optimized to minimize the amount of excess unbound coating material. Additionally, the compositions can be formulated to preserve the functional coating of coated Ibuprofen and to minimize aeration of Ibuprofen when mixed into suspension.

## Claims

### Claim 1

A pharmaceutical composition comprising:
more than 75% w/w coated API, wherein the API coating comprises a first coating material and 0.5-5% w/w silica surrounding, partially embedded in, and/or embedded in the first coating material;
3-7% w/w matrix former;
2-6% w/w structure former;
0.1-2% w/w anti-aerating agent; and
0.01-0.2% w/w viscosity modifier.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the first coating material comprises 10-30% w/w of the coated API.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the first coating material comprises a wax.

### Claim 4 (depends on 3)

The pharmaceutical composition of claim 3, wherein the first coating material comprises one or more of carnauba wax, synthetic wax, or candelilla wax.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1, wherein the matrix former comprises one or more of a water soluble material, a water dispersible material, a polypeptide, a polysaccharide, a polyvinyl alcohol, a polyvinylpyrrolidone, and an acacia.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein the matrix former comprises a polypeptide.

### Claim 7 (depends on 6)

The pharmaceutical composition of claim 6, wherein the polypeptide comprises gelatin.

### Claim 8 (depends on 1)

The pharmaceutical composition of claim 1, wherein the structure former comprises one or more of mannitol, dextrose, lactose, galactose, and cyclodextrin.

### Claim 9 (depends on 8)

The pharmaceutical composition of claim 8, wherein the structure former comprises mannitol.

### Claim 10 (depends on 1)

The pharmaceutical composition of claim 1, wherein the viscosity modifier comprises xanthan gum.

### Claim 11 (depends on 1)

The pharmaceutical composition of claim 1, wherein the anti-aerating agent comprises one or more of a terpene or a terpinol.

### Claim 12 (depends on 11)

The pharmaceutical composition of claim 11, wherein the anti-aerating agent comprises limonene.

### Claim 13 (depends on 1)

The pharmaceutical composition of claim 1, wherein the anti-aerating agent comprises one or more of orange flavor, lemon flavor, grapefruit flavor, lime flavor, strawberry flavor, or peppermint flavor.

### Claim 14 (depends on 1)

The pharmaceutical composition of claim 1, further comprising a sweetener.

### Claim 15 (depends on 1)

The pharmaceutical composition of claim 1, wherein the API comprises Ibuprofen.

### Claim 16

A method of preparing a pharmaceutical composition comprising:
forming a pharmaceutical suspension comprising:
30-50% w/w a coated API, wherein the API coating comprises a first coating material and 0.5-5% w/w silica surrounding, partially embedded in, and/or embedded in the first coating material;
50-70% w/w a matrix solution or suspension comprising:
1-5% w/w a matrix former;
0.5-4% w/w a structure former;
0.01-0.1% w/w a viscosity modifier;
0.1-1% w/w an anti-aerating agent; and
a solvent;
dosing the pharmaceutical suspension into a mold;
freezing the pharmaceutical suspension in the mold; and
freeze drying the dosed pharmaceutical suspension in the mold to form the pharmaceutical composition.

### Claim 17 (depends on 16)

The method of claim 16, wherein the first coating material comprises 10-30% w/w of the coated API.

### Claim 18 (depends on 16)

The method of claim 16, wherein the first coating material comprises one or more of carnauba wax, synthetic wax, or candelilla wax.

### Claim 19 (depends on 16)

The method of claim 16, wherein the matrix former comprises gelatin.

### Claim 20 (depends on 16)

The method of claim 16, wherein the structure former comprises mannitol.

### Claim 21 (depends on 16)

The method of claim 16, wherein the viscosity modifier comprises xanthan gum.

### Claim 22 (depends on 16)

The method of claim 16, wherein the anti-aerating agent comprises one or more of a terpene or a terpinol.

### Claim 23 (depends on 22)

The method of claim 22, wherein the anti-aerating agent comprises limonene.

### Claim 24 (depends on 16)

The method of claim 16, wherein the matrix solution or suspension comprises a sweetener.

### Claim 25 (depends on 16)

The method of claim 16, wherein the API comprises Ibuprofen.

### Claim 26 (depends on 16)

The method of claim 16, wherein the solvent comprises water.