Formulation containing anti-inflammatory androstane derivatives

• US 7,531,528 B2
• Filed: 08/13/2004
• Issued: 05/12/2009
• Est. Priority Date: 08/05/2000
• Status: Expired due to Term

• Current Assignee: GlaxoSmithKline Intellectual Property Management Limited (GSK plc)
• Original Assignee: Glaxo Group Limited (GSK plc)
• Inventors: Buxton, Ian, Sayani, Amyn, Reed, Kenton, Biggadike, Keith
• Primary Examiner(s): Badio; Barbara P
• Application Number:
  US10/918,770
• Publication Number:
  US 20050026888A1
• Time in Patent Office: 1,733 Days
• Field of Search: 514/172
• US Class Current: 514/172
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 5/44 Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids

Abstract

There is provided according to the invention a pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) an ester of fluticasone or a solvate thereof as medicament and (b) a solubilizing agent for assisting the solubilization of the medicament in the aqueous carrier liquid.

Claims

1. A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I)

2. A pharmaceutical formulation according to claim 1 wherein the solubilising agent is a surfactant.

3. A pharmaceutical formulation according to claim 2 wherein the surfactant is selected from the group consisting of a α

-[4-(1,1,3,3-tetramethylbutyl)phenyl]-ω

-hydroxypoly (oxy-1,2-ethanediyl) polymer and a 4-(1,1,3,3-Tetramethylbutyl) phenol polymer with formaldehyde and oxirane.

4. A pharmaceutical formulation according to claim 3 wherein the surfactant is a 4-(1,1,3,3-Tetramethylbutyl)phenol polymer with formaldehyde and oxirane.

5. A pharmaceutical formulation according to claim 2 which further has dissolved therein a hydroxy containing organic co-solvating agent or phosphatidyl choline.

6. A pharmaceutical formulation according to claim 5 wherein the hydroxy containing organic co-solvating agent is dextrose.

7. A pharmaceutical formulation according to claim 1 wherein the formulation further comprises chloride as an isotonic agent.

8. A pharmaceutical formulation according to claim 1 which comprises another therapeutically active agent.

9. A pharmaceutical formulation according to claim 8 wherein the other therapeutically active agent is an anti-histamine or an anti-allergic.

10. A container containing a pharmaceutical formulation according to claim 1, fitted with a metering valve.

11. A device adapted for intranasal delivery of a pharmaceutical formulation comprising a container according to claim 10.

12. A method of treatment of inflammatory and/or allergic conditions of the nasal passages which comprises administering to the nose a pharmaceutical formulation according to claim 1.

13. The method according to claim 12 wherein the administration is once-per-day.

14. A process for preparing a pharmaceutical formulation which comprises:

(a) providing;

(i) a glucocorticoid of formula (I)