# US 10,117,939 B2 · Pharmaceutical compositions comprising nebivolol or a nebivolol analogue

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- Number: US 10,117,939 B2
- Document ID: US10117939B2
- Status: Granted
- Kind: B2
- Application number: 14/704,375
- Filed: 2015-05-05
- Published: 2015-08-20
- Granted: 2018-11-06
- Earliest claimed: 2007-01-22
- Assignees: Mylan Pharmaceuticals ULC
- Applicants: Mylan Pharmaceuticals Ulc
- Inventors: Mostafa Akbarieh; Fazal M. Mohideen; Shetal Shah
- Web page: https://patentgrep.com/patent/US10117939B2

## CPC

- A61K 47/38: Cellulose; Derivatives thereof
- A61J 3/10: into the form of compressed tablets (tablet presses B30B11/00)
- 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 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 31/353: 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K 47/02: Inorganic compounds
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- 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
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- 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)
- A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present application provides pharmaceutical compositions comprising as the active medicinal ingredient nebivolol, a nebivolol analog or a pharmaceutically acceptable acid addition salt thereof and a wetting agent. The invention also relates to methods of preparing and using said compositions.

## Claims

### Claim 1

A pharmaceutical composition for oral administration comprising an active ingredient and a wetting agent, wherein the pharmaceutical composition is a solid pharmaceutical composition in the form of a tablet, wherein the active ingredient is nebivolol hydrochloride, the wetting agent is polysorbate 80, the pharmaceutical composition comprises, on a weight percentage basis, from about 0.01% to about 0.04% of the wetting agent and from about 0.5% to about 10% of the active ingredient, and the ratio (w/w) of wetting agent to active ingredient is less than 0.025,
wherein the composition further comprises from about 20% to about 80% of a spray dried mixture of microcrystalline cellulose and lactose and/or lactose monohydrate, from about 1% to about 4% of hydroxypropylmethylcellulose, from about 2% to about 30% of corn starch and/or croscarmellose sodium, from about 0.25% to about 2% of magnesium stearate and from about 0.1% to about 2% of colloidal silicon dioxide, and
wherein the active ingredient is added to the pharmaceutical composition in the form of unmicronized solid particles having a specific surface area of less than 23×103 cm2/g.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1 comprising, on a weight percentage basis, about 2.37% of nebivolol hydrochloride, about 0.03% of polysorbate 80, about 26.36% of a spray dried mixture of microcrystalline cellulose and lactose, about 43.48% of lactose monohydrate, about 2% of hydroxypropylmethylcellulose, about 20% of corn starch, about 5% of croscarmellose sodium, about 0.5% of magnesium stearate and about 0.26% of colloidal silicon dioxide.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the tablet exhibits a dissolution of at least 75% after 15 minutes.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1 consisting essentially of, on a weight percentage basis, from about 0.5% to about 10% of nebivolol hydrochloride, from about 0.01% to about 0.04% of polysorbate 80, from about 20% to about 80% of a spray dried mixture of microcrystalline cellulose and lactose and/or lactose monohydrate, from about 1% to about 4% of hydroxypropylmethylcellulose, from about 2% to about 30% of corn starch and/or croscarmellose sodium, from about 0.25% to about 2% of magnesium stearate and from about 0.1% to about 2% of colloidal silicon dioxide.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1 consisting of, on a weight percentage basis, about 2.37% of nebivolol hydrochloride, about 0.03% of polysorbate 80, about 26.36% of a spray dried mixture of microcrystalline cellulose and lactose, about 43.48% of lactose monohydrate, about 2% of hydroxypropylmethylcellulose, about 20% of corn starch about 5% of croscarmellose sodium, about 0.5% of magnesium stearate and about 0.26% of colloidal silicon dioxide.