Combination of Azelastine and Steroids

• US 20090318397A1
• Filed: 07/23/2009
• Published: 12/24/2009
• Est. Priority Date: 06/14/2002
• Status: Active Grant

• Current Assignee: Cipla (EU) Limited (Cipla Limited)
• Original Assignee: Cipla (EU) Limited (Cipla Limited)
• Inventors: Lulla, Amar, Malhotra, Geena
• Granted Patent: US 8,304,405 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.

Claims

1. A pharmaceutical formulation which comprises azelastine, or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and ciclesonide.

2. The pharmaceutical formulation according to claim 1, wherein said azelastine is present as azelastine hydrochloride.

3. The formulation according to claim 1, which contains ciclesonide in an amount from about 50 micrograms/ml to about 5 mg/ml of the formulation.

4. The formulation according to claim 1, wherein the formulation has a particle size of less than about 10 μ

m.

5. The formulation according to claim 1, which is a suspension containing 0.0005 to 2% (weight/weight of the formulation) of azelastine or a pharmaceutically acceptable salt of azelastine, and from 0.5 to 1.5% (weight/weight of the formulation) of ciclesonide.

6. The formulation according to claim 5, which contains from 0.001 to 1% (weight/weight of the formulation) azelastine, or salt thereof, and from 0.5% to 1.5% (weight/weight of the formulation) ciclesonide.

7. The formulation according to claim 1, which also contains a surfactant, comprising a polysorbate or poloxamer surfactant.

8. The formulation according to claim 7, which contains from about 50 micrograms to about 1 milligram of surfactant per ml of the formulation.

9. The formulation according to claim 1, which also contains an isotonic agent comprising sodium chloride, saccharose, glucose, glycerine, sorbitol or 1,2-propylene glycol.

10. The formulation according to claim 1, which also contains at least one of a buffer, a preservative and a suspending or thickening agent, wherein said preservative is selected from edetic acid and its alkali salts, lower alkyl p-hydroxybenzoates, chlorhexidine, phenyl mercury borate, or benzoic acid or a salt, a quaternary ammonium compound, or sorbic acid or a salt thereof, the suspending agent or thickening agent is selected from cellulose derivatives, gelatin, polyvinylpyrrolidone, tragacanth, ethoxose (water soluble binding and thickening agents on the basis of ethyl cellulose), alginic acid, polyvinyl alcohol, polyacrylic acid, or pectin, and the buffer comprises a citric acid-citrate buffer.

11. The formulation according claim 10, wherein the buffer maintains the pH of the aqueous phase at from 3 to 7.

12. The formulation according to claim 1, which comprises azelastine hydrochloride and ciclesonide.

13. The formulation according to claim 1, which is in the form of an insufflation powder.

14. The formulation according to claim 1, which is an aqueous suspension or solution.

15. The formulation according to claim 14, which is in the form of an aerosol, an ointment, eye drops, nasal drops, a nasal spray or an inhalation solution.

16. The formulation according to claim 15, which is in the form of nasal drops or nasal spray.

17. The formulation according to claim 15, which is in the form of an aerosol.

18. A pharmaceutical product comprising (i) azelastine, or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and (ii) ciclesonide, as a combined preparation for simultaneous, separate or sequential use in medicine, said (i) azelastine and (ii) ciclesonide being in the form of an aerosol formulation for MDI delivery, in the form of an insufflation powder, or in the form of a nasal spray.

19. The pharmaceutical product according to claim 18, which comprises azelastine hydrochloride and ciclesonide.

20. The pharmaceutical product according to claim 18, wherein said product is formulated for use as a nasal spray in the treatment of seasonal allergic rhinitis, perennial allergic rhinitis.