Tasipimidine formulations and use thereof

Patent metadata

Field	Value
Publication number	US-2024165083-A1
Application number	US-202218551059-A
Country	US
Kind code	A1
Filing date	Mar 18, 2022
Priority date	Mar 19, 2021
Publication date	May 23, 2024
Grant date	—

Abstract

The present disclosure relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient and to the use thereof in the treatment and prevention of situational anxiety and fear in companion animals, such as dogs. The composition is stable at the pH range from about 2.0 to about 5.0 and it can be easily administered by the pet owners.

First claim

1 . A liquid pharmaceutical composition comprising:
a) tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient at a concentration of at least 0.04 mg/ml; b) a buffering agent; c) a preservative; and d) water; wherein the pH of the composition is from about 2.0 to about 5.0; and wherein the liquid pharmaceutical composition is adapted for oral administration.

2 . The composition according to claim 1 , wherein the active ingredient is tasipimidine sulfate.

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

4 . The composition according to claim 1 , wherein the composition comprises about 0.004-0.3%, per weight of the composition, of tasipimidine, or a pharmaceutically acceptable salt thereof.

5 . The composition according to claim 1 , wherein the buffering agent is citric acid/sodium citrate buffer.

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 comprises:
a) tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient at a concentration of at least 0.04 mg/ml; b) citric acid/sodium citrate buffer; c) sodium benzoate; and d) water; wherein the pH of the composition is from about 2.0 to about 5.0.

9 . The composition according to claim 1 , wherein the composition comprises;
a) 0.004-0.3%, per weight of the composition, of tasipimidine, or a pharmaceutically acceptable salt thereof; b) 0.05-4.5%, per weight of the composition, of a buffering agent; c) 0.01-1%, per weight of the composition, of a preservative; and d) 96-98%, per weight of the composition, of purified water; wherein the pH of the composition is from about 2.0 to about 5.0.

10 . The composition according to claim 9 , wherein the composition comprises:
a) 0.01-0.1%, per weight of the composition, of tasipimidine or a pharmaceutically acceptable salt thereof; b) 2.0-2.7%, per weight of the composition, of citric acid/citrate buffer; c) 0.02-0.5%, per weight of the composition, of a benzoic acid salt; and d) 97-97.9%, per weight of the composition, of purified water; wherein the pH of the composition is from about 2.0 to about 5.0.

11 . The composition according to claim 1 , wherein the buffer concentration is about 0.005-1 M.

12 . (canceled)

13 . (canceled)

14 . (canceled)

15 . A method for the treatment or prevention of situational anxiety and fear in a companion animal, comprising administering to the subject in need thereof an effective amount of a composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient.

16 . The method according to claim 15 , wherein the composition comprises:
a) tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient at a concentration of at least 0.04 mg/ml; b) a buffering agent; c) a preservative; and d) water; wherein the pH of the composition is from about 2.0 to about 5.0; and wherein the liquid pharmaceutical composition is adapted for oral administration.

17 . The method according to claim 15 , wherein the situational anxiety is noise anxiety, veterinary visit anxiety, transportation anxiety, or separation anxiety.

18 . (canceled)

19 . (canceled)

20 . A medicinal kit comprising a) a liquid pharmaceutical composition adapted for oral administration comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient, b) a package for containing said composition, and c) instructions for administering said composition to a companion animal, for the treatment or prevention of situational anxiety and fear.

21 . The composition according to claim 1 wherein the concentration of tasipimidine, or a pharmaceutically acceptable salt thereof, is at least 0.25 mg/ml.

22 . The composition according to claim 1 wherein the pH of the composition is from about 2.9 to 3.1.

23 . The composition according claim 1 , wherein the composition comprises about 0.02-0.05%, per weight of the composition, of tasipimidine, or a pharmaceutically acceptable salt thereof.

24 . The composition according to claim 1 , wherein the buffer concentration about 0.1 M.

25 . The method for the treatment or prevention of situational anxiety and fear in a companion animal according to claim 15 , wherein the companion animal is a dog.

Assignees

• Orion Corp

Inventors

• Kujala Johanna
• Lehtisalo Jenni
• Salmia Jukka
• Sinervo Kai

Classifications

• A61K31/4178 Primary

  not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin · CPC title

• A61K9/0095 Primary

  Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006) · CPC title

• A61K9/08 Primary

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

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61P25/22

  Anxiolytics · CPC title