# US 2014/0193487 A1 · Compositions and methods for treating centrally mediated nausea and vomiting

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- Number: US 2014/0193487 A1
- Document ID: US20140193487A1
- Status: Published application
- Kind: A1
- Application number: 14/069,885
- Filed: 2013-11-01
- Published: 2014-07-10
- Earliest claimed: 2009-11-18
- Assignees: Helsinn Healthcare SA
- Applicants: Helsinn Healthcare S.A.
- Inventors: Fabio TRENTO; Sergio CANTOREGGI; Giorgia ROSSI; Roberta CANNELLA; Daniele BONADEO
- Web page: https://patentgrep.com/patent/US20140193487A1

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- A61K 9/4858: {Organic compounds}
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/473: ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- 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

Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.

## Claims

### Claim at position 1

1-51. (canceled)

### Claim 52

An oral pharmaceutical dosage form comprising about 0.56 mg of palonosetron hydrochloride and about 300 mg of netupitant as the free base.

### Claim 53

An oral pharmaceutical dosage form in the form of a capsule comprising a hard outer shell, three tablets comprising about 100 mg of netupitant each, and one soft-gel capsule comprising about 0.56 mg of palonosetron hydrochloride, wherein the tablets and soft-gel capsule are housed within the hard outer shell.

### Claim 54 (depends on 53)

The oral dosage form of claim 53, comprising 0.56 mg of palonosetron hydrochloride and 300 mg of netupitant as the free base.

### Claim 55 (depends on 53)

The oral dosage form of claim 53, further comprising (3S)-3-[(3aS)-1-oxo-2,3,3 a,4,5,6-hexahydro-1H-benzo[de]isoquinoline-2-yl]-1-azoniabicyclo[2.2.2]octan-1-olate in an amount that does not exceed 3 wt. %.

### Claim 56 (depends on 53)

The oral dosage form of claim 53, wherein said outer shell of said capsule has an oxygen permeability of less than 1.0×10−3 ml·cm/(cm2·24 hr. atm).

### Claim 57 (depends on 53)

The oral dosage form of claim 53, wherein each of said soft-gel capsules comprises an inner fill composition comprising from about 75 to about 98 wt. % of one or more lipophilic components.

### Claim 58

A dosage form formulated for oral administration comprising a therapeutically effective amount of a) netupitant and b) palonosetron, wherein a single dose of the composition provides a median tmax of netupitant that is about 0.5 hours shorter than is provided by a single dose of a composition having the same amount of netupitant alone.

### Claim 59

A pharmaceutical composition formulated for oral administration comprising a therapeutically effective amount of a) netupitant and b) palonosetron, wherein a single dose of the composition provides a greater area under the curve (AUC) of netupitant than is provided by a single dose of a composition having the same amount of netupitant alone.

### Claim 60 (depends on 59)

The pharmaceutical composition of claim 59, wherein the composition further provides a greater Cmax of netupitant than is provided by a single dose of a composition having the same amount of netupitant alone.

### Claim 61 (depends on 59)

The pharmaceutical composition of claim 59, wherein the composition further provides a shorter tmax of netupitant than is provided by a single dose of a composition having the same amount of netupitant alone.

### Claim 62 (depends on 61)

The pharmaceutical composition of claim 61, wherein the median tmax of netupitant is 0.5 hour shorter than is provided by a single dose of a composition having the same amount of netupitant alone.