Tasipimidine formulations and use thereof

Patent metadata

Field	Value
Publication number	US-2024173254-A1
Application number	US-202218551084-A
Country	US
Kind code	A1
Filing date	Mar 18, 2022
Priority date	Mar 19, 2021
Publication date	May 30, 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 a disorder, condition or disease where an alpha2A agonist is indicated to be useful, for example, for use as a sedative or analgesic agent, and for use in the treatment of anxiety or agitation. The composition is stable at the pH range from about 2.0 to about 5.0.

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 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 liquid pharmaceutical composition adapted for oral administration to a human.

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 . (canceled)

16 . (canceled)

17 . A method for the treatment or prevention of anxiety or agitation in a human, comprising administering to the human subject in need thereof an effective amount of a liquid composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient.

18 . The method according to claim 17 , 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 composition is adapted for oral administration.

19 . The method according to claim 17 , wherein the anxiety or agitation is associated with dementia.

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 mammal, for the treatment or prevention of anxiety or agitation.

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.

Assignees

• Orion Corp

Inventors

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

Classifications

• A61K9/08 Primary

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

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K31/4178 Primary

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

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · 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