Formulation containing anti-inflammatory androstane derivative

• US 7,541,350 B2
• Filed: 08/13/2004
• Issued: 06/02/2009
• 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: Reed, Kenton Lewis, Buxton, Ian Richard, Biggadike, Keith, Sayani, Amyn Pyarali
• Primary Examiner(s): Badio; Barbara P
• Application Number:
  US10/918,779
• Publication Number:
  US 20050020549A1
• Time in Patent Office: 1,754 Days
• Field of Search: 514/171, 514/172
• US Class Current: 514/172
• 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 31/56 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 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/0078 for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 5/44 Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids

Abstract

There is provided a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I)

or a solvate thereof.

Claims

1. A pharmaceutical formulation comprising an aqueous suspension of particulate unsolvated polymorph Form 1 of compound of formula (I)

2. The pharmaceutical formulation of claim 1, wherein the compound of formula (I) is present within the formulation in an amount between 0.005% and 1% (w/w), based on the total weight of the formulation.

3. A pharmaceutical formulation according to claim 2 wherein the suspending agent is one or more of microcrystalline cellulose and carboxy methylcellulose sodium, the preservative is one or more of EDTA and benzalkonium chloride, the wetting agent is one or more of polyoxyethylene (20) sorbitan monooleate and the isotonicity adjusting agent is dextrose.

4. A method of treating rhinitis comprising the nasal application of a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I)

5. A method of claim 4, wherein the compound of formula (I) is used as unsolvated polymorph Form 1.

6. A method of claim 5, wherein the compound of formula (I) is present within the formulation in an amount between 0.005% and 1% (w/w), based on the total weight of the formulation.

7. The method of claim 5, wherein the suspending agent is one or more of microcrystalline cellulose and carboxy methylcellulose sodium, the preservative is one or more of EDTA and benzalkonium chloride, the wetting agent is one or more of polyoxyethylene (20) sorbitan monooleate and the isotonicity adjusting agent is dextrose.