# US 10,369,108 B2 · Hot melt granulation formulations of poorly water-soluble active agents

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- Number: US 10,369,108 B2
- Document ID: US10369108B2
- Status: Granted
- Kind: B2
- Application number: 14/211,144
- Filed: 2014-03-14
- Published: 2014-09-18
- Granted: 2019-08-06
- Earliest claimed: 2013-03-15
- Assignees: Mylan Laboratories Limited
- Applicants: Mylan Laboratories, Inc.
- Inventors: Chaoju Xiao; Boyong Li
- Web page: https://patentgrep.com/patent/US10369108B2

## CPC

- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 31/145: having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2) (isothiourea A61K31/155)
- 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

The presently disclosed subject matter is directed to a granule, wherein the granule has an active agent and a wax dispersed therein, and the granule exhibits excellent friability when compressed to form a pharmaceutical composition. The subject matter disclosed herein is also directed to methods of preparing the granules and the pharmaceutical compositions comprising the granules. The compositions and methods disclosed provide granules and pharmaceutical compositions for immediate release of the active agent and do not substantially prolong the release of the active agent from the granule.

## Claims

### Claim 1

An immediate release pharmaceutical composition consisting of granules and extragranular excipients, wherein
the granules consist of disulfiram, a wax material, microcrystalline cellulose, and lactose;
the wax material is present in an amount of about 2% (w/w) to about 7% (w/w) of the granules; and
the disulfiram and the wax material are distributed throughout the granules.

### Claim 2 (depends on 1)

The composition of claim 1, wherein said wax is present in an amount from about 3% to about 5% (w/w) of said granule.

### Claim 3 (depends on 1)

The composition of claim 1, wherein said wax is selected from the group consisting of stearic acid, palmitic acid, carnauba wax, glyceryl behenate, glyceryl monostearate, glyceryl distearate, and gelucire, and combinations thereof.

### Claim 4 (depends on 1)

The composition of claim 1, wherein said wax material comprises at least about 40% w/w stearic acid.

### Claim 5 (depends on 1)

The composition of claim 1, wherein said composition is a tablet.

### Claim 6 (depends on 1)

The composition of claim 1, wherein said wax material is stearic acid.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the extragranular excipients consist of microcrystalline cellulose, lactose, sodium starch glycolate, colloidal silicon dioxide, and magnesium stearate.