# US 11,433,021 B2 · Palonosetron for the treatment or prevention of nausea and vomiting

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- Number: US 11,433,021 B2
- Document ID: US11433021B2
- Status: Granted
- Kind: B2
- Application number: 16/961,017
- Filed: 2019-01-11
- Published: 2020-11-05
- Granted: 2022-09-06
- Earliest claimed: 2018-01-12
- Assignees: Orion Corporation
- Applicants: Orion Corporation
- Inventors: Jouko Levijoki; Sari Pappinen; Lasse Saloranta
- Web page: https://patentgrep.com/patent/US11433021B2

## CPC

- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/473: ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/38: Cellulose; Derivatives thereof
- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

The invention relates to a method for treating or preventing nausea and vomiting. The method comprises administering an eye drop composition comprising palonosetron or a pharmaceutically acceptable salt thereof to the eye of the subject. The ocular administration results in fast systemic absorption, improved bioavailability compared to oral route and extended elimination time.

## Claims

### Claim 1

A method for the treatment or prevention of nausea and vomiting in a subject comprising administering to the eye of the subject in need thereof an effective amount of an eye drop composition comprising palonosetron or a pharmaceutically acceptable salt thereof as a sole active ingredient.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the palonosetron or the pharmaceutically acceptable salt thereof is administered to the eye in an amount ranging from 0.5 μg/kg to 500 μg/kg.

### Claim 3 (depends on 2)

The method according to claim 2, wherein the palonosetron or the pharmaceutically acceptable salt thereof is administered to the eye in an amount ranging from 1 μg/kg to 300 μg/kg.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the treatment or prevention of nausea and vomiting is associated with chemotherapy-induced nausea and vomiting (CINV), radiotherapy-induced nausea and vomiting (RINV), post-operative nausea, and vomiting (POVN) or motion sickness.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the subject to be treated is a human.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the subject to be treated is a companion animal chosen from a dog and a cat.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the composition comprises:
(a) 0.01% to 5%, per weight of the composition, of the palonosetron or the pharmaceutically acceptable salt thereof as a sole active ingredient;
(b) 0.5% to 25% per weight of the composition, of cyclodextrin;
(c) 0.1% to 10%, per weight of the composition, of a tonicity adjusting agent;
(d) 0.05% to 5%, per weight of the composition, of a buffering agent; and
(e) 70% to 99%, per weight of the composition, of sterile water.

### Claim 8 (depends on 7)

The method according to claim 7, wherein the tonicity adjusting agent is sodium chloride or mannitol.

### Claim 9 (depends on 7)

The method according to claim 7, wherein the cyclodextrin is a member selected from the group consisting of hydroxypropyl-β-cyclodextrin, hydroxypropyl-γ-cyclodextrin and sulfobutylether-β-cyclodextrin.

### Claim 10 (depends on 7)

The method according to claim 7, wherein the composition has a pH between 3.5 and 7.0.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the composition has a pH between 4.0 and 6.0.

### Claim 12 (depends on 10)

The method according to claim 10, wherein the buffering agent is citric acid/sodium citrate.

### Claim 13 (depends on 10)

The method according to claim 10, wherein the thickening agent is at least one member selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, polyethylene glycol, polyacrylic acid and a cellulose derivative.