# US 10,307,385 B2 · Gelling formulation containing ketamine

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- Number: US 10,307,385 B2
- Document ID: US10307385B2
- Status: Granted
- Kind: B2
- Application number: 14/423,882
- Filed: 2013-08-30
- Published: 2015-08-13
- Granted: 2019-06-04
- Earliest claimed: 2012-08-31
- Assignees: Assistance Publique-Hopitaux de Paris
- Applicants: Assistance Publique—Hopitaux de Paris
- Inventors: Vincent Boudy; Annick Tibi; Benoît D'Hayer; Marie-Caroline Husson; Sandrine Graff De Faget
- Web page: https://patentgrep.com/patent/US10307385B2

## CPC

- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- 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)
- A61P 23/00: Anaesthetics
- A61P 23/02: Local anaesthetics
- 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

A gelling formulation containing ketamine or a pharmaceutically acceptable salt thereof in water, a poloxamer and one or more pharmaceutically acceptable mucoadhesive agents is provided. Also provided is a method of using the formulation for pain treatment.

## Claims

### Claim 1

A liquid gelling formulation comprising ketamine or a pharmaceutically acceptable salt thereof, 15 to 20 g/100 ml of a poloxamer, from 1 to 2 g/100 ml of at least one pharmaceutically acceptable mucoadhesive agents, and water.

### Claim 2 (depends on 1)

The liquid gelling formulation as claimed in claim 1, wherein the ketamine is the S-(+) enantiomer of ketamine or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The liquid gelling formulation as claimed in claim 1, comprising from 2 to 20 g/100 ml of ketamine or of a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The liquid gelling formulation as claimed in claim 1, comprising from 16 to 19 g/100 ml of poloxamer.

### Claim 5 (depends on 1)

The liquid gelling formulation as claimed in claim 1, wherein the poloxamer is chosen from poloxamer 407, poloxamer 188, or a mixture thereof.

### Claim 6 (depends on 1)

The liquid gelling formulation as claimed in claim 1, also comprising one or more pharmaceutically acceptable excipients chosen from taste-masking agents, acidic agents, basic agents, preservatives, sodium chloride and potassium chloride.

### Claim 7 (depends on 1)

The liquid gelling formulation as claimed in claim 1, characterized in that the gelling formulation as a whole is sterile.

### Claim 8 (depends on 1)

The liquid gelling formulation as claimed in claim 1, characterized in that it is intended for sublingual administration.

### Claim 9 (depends on 1)

The liquid gelling formulation as claimed in claim 1, characterized in that it is intended to be sprayed in the form of a liquid spray into the buccal cavity.

### Claim 10 (depends on 1)

A pharmaceutical composition comprising formulation as claimed in claim 1.

### Claim 11 (depends on 1)

A method of treating an individual suffering from pain comprising the step of administering the liquid gelling formulation of claim 1.

### Claim 12 (depends on 11)

The method as claimed in claim 11, wherein the formulation is sprayed in the form of a liquid spray into the buccal cavity.

### Claim 13 (depends on 1)

A method for preparing a liquid gelling formulation as claimed in claim 1, said method comprising the steps of:
i) dissolving, under cold conditions, the poloxamer in water;
ii) adding and dissolving one or more mucoadhesive agents;
iii) adding and dissolving ketamine or a salt thereof to and in the solution obtained in step i), at ambient temperature; and
iv) recovering the formulation obtained.

### Claim 14 (depends on 1)

A method for preparing a liquid gelling formulation as claimed in claim 1, said method comprising the steps of:
i) dissolving ketamine or a salt thereof in water, at ambient temperature;
ii) adding and dissolving one or more mucoadhesive agents at a temperature between +40° C. and +70° C.;
iii) adding and dissolving the poloxamer to and in the solution obtained in step i) cooled beforehand, at a temperature between +8° C. and +16° C.; and
iv) recovering the formulation obtained.

### Claim 15 (depends on 14)

The method of claim 14, wherein the step of dissolving ketamine or a salt thereof in water is at a temperature between +15° C. and +25° C.

### Claim 16 (depends on 13)

The method of claim 13, wherein the step of
dissolving the poloxamer in water is at a temperature between +8° C. and +16° C., the step of adding and dissolving one or more mucoadhesive agents is at a temperature between +40° C. and +70° C., and the step of adding and dissolving ketamine or a salt thereof to and in the solution obtained in step i), is at a temperature between +15° C. and +25° C.

### Claim 17 (depends on 1)

A pharmaceutical composition consisting of the formulation as claimed in claim 1.