Pregabalin formulations and use thereof

Patent metadata

Field	Value
Publication number	US-12558331-B2
Application number	US-202017442345-A
Country	US
Kind code	B2
Filing date	Mar 26, 2020
Priority date	Mar 26, 2019
Publication date	Feb 24, 2026
Grant date	Feb 24, 2026

Abstract

The invention relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising pregabalin as an active ingredient and to the use thereof in the treatment and prevention of transportation and veterinary visit anxiety and fear in companion animals, such as cats. The composition is stable, well palatable to animals and can be easily administered by the pet owner.

First claim

The invention claimed is:

1 . A liquid pharmaceutical composition adapted for oral administration comprising:
(i) pregabalin as an active ingredient at a concentration of at least 35 mg/ml; (ii) a flavouring agent; (iii) a preservative; and (iv) water; wherein the pH of the composition is from about 3.0 to about 4.4.

2 . The composition according to claim 1 , wherein the composition is a veterinary liquid pharmaceutical composition adapted for oral administration to a companion animal.

3 . The composition according to claim 1 , wherein the composition comprises 3.5-15%, per weight of the composition, of pregabalin.

4 . The composition according to claim 1 , wherein the flavouring agent is yeast extract, hydrolysed yeast, or ethyl maltol.

5 . The composition according to claim 4 , wherein the flavouring agent is ethyl maltol.

6 . The composition according to claim 1 , wherein the preservative is a benzoic acid salt.

7 . The composition according to claim 6 , wherein the preservative is sodium benzoate.

8 . The composition according to claim 1 , wherein the composition lacks a buffering agent other than pregabalin itself.

9 . The composition according to claim 1 , wherein the composition comprises:
(i) pregabalin as an active ingredient at a concentration of at least 35 mg/ml; (ii) ethyl maltol; (iii) sodium benzoate; and (iv) water; wherein the pH of the composition is from about 3.0 to about 4.4.

10 . The composition according to claim 1 , wherein the composition comprises:
(i) 3.5-15%, per weight of the composition, of pregabalin; (ii) 0.002-1%, per weight of the composition, of the flavouring agent; (iii) 0.01-1%, per weight of the composition, of the preservative; and (iv) 75-96.5%, per weight of the composition, of sterile water; wherein the pH of the composition is from about 3.0 to about 4.4.

11 . The composition according to claim 9 , wherein the composition comprises:
(i) 3.5-15%, per weight of the composition, of pregabalin; (ii) 0.001-0.05%, per weight of the composition, of ethyl maltol; (iii) 0.05-0.5%, per weight of the composition, of a benzoic acid salt; and (iv) 85-96.5%, per weight of the composition, of sterile water, wherein the pH of the composition is from about 3.0 to about 4.4.

12 . A method for the treatment or prevention of transportation and veterinary visit anxiety and fear in a companion animal comprising administering to the companion animal in need thereof an effective amount of the liquid pharmaceutical composition according to claim 1 .

13 . A medicinal kit comprising a) the liquid pharmaceutical composition according to claim 1 , b) a package for containing said composition, and c) instructions for administering said composition to a companion animal for the treatment or prevention of transportation and veterinary visit anxiety and fear.

14 . The composition according to claim 1 , wherein the composition comprises pregabalin as an active ingredient at a concentration of at least 40 mg/ml.

15 . The composition according to claim 1 , wherein the composition comprises pregabalin as an active ingredient at a concentration of at least 45 mg/ml.

16 . The composition according to claim 1 , wherein the pH of the composition is from about 3.2 to about 4.2.

17 . The composition according to claim 1 , wherein the pH of the composition is from about 3.5 to about 4.0.

18 . The composition according to claim 2 , wherein the companion animal is a cat.

Assignees

• Orion Corp

Inventors

• Huhtinen Mirja
• Lamminen Terttu
• Salmia Jukka
• Tervapuro Johanna
• Vercruysse Jurgen

Classifications

• A61K9/08 Primary

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K9/0056 Primary

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title

• A61P25/22

  Anxiolytics · CPC title

• A61K31/197 Primary

  the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205) · CPC title

• A61K47/46

  Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts · CPC title