Olopatadine formulations for topical nasal administration

• US 20070142458A1
• Filed: 02/07/2007
• Published: 06/21/2007
• Est. Priority Date: 06/27/2001
• Status: Active Grant

• Current Assignee: Novartis Ag
• Original Assignee: Alcon Incorporated
• Inventors: Jani, Rajni, Chowhan, Masood, Han, Wesley, Wall, G., Singh, Onkar
• Granted Patent: US 7,977,376 B2
• Time in Patent Office: Days
• US Class Current: 514/450
• 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 31/14 Quaternary ammonium compounds, e.g. edrophonium, choline betaines A61K31/205
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/335 having oxygen as the only ring hetero atom, e.g. fungichromin
• CPC Class Codes: A61K 33/42 Phosphorus; Compounds thereof
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: Y10S 424/81 involving autoimmunity, allergy, immediate hypersensitivity, delayed hypersensitivity, immunosuppression, immunotolerance, or anergy

Abstract

Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the nose are disclosed. The aqueous formulations contain approximately 0.6% (w/v) of olopatadine.

Claims

1. A composition consisting essentially of

a) 0.54-0.62% (w/v) olopatadine free base or an equivalent amount of a pharmaceutically acceptable salt of olopatadine;

b) a phosphate salt in an amount equivalent to 0.2-0.8% (w/v) dibasic sodium phosphate, wherein the phosphate salt selected from the group consisting of monobasic sodium phosphate;

dibasic sodium phosphate;

tribasic sodium phosphate;

monobasic potassium phosphate;

dibasic potassium phosphate; and

tribasic potassium phosphate;

c) 0.3-0.6% (w/v) NaCl;

d) a pH-adjusting agent in an amount sufficient to cause the composition to have a pH of 3.6-3.8;

e) 0.005-0.015% (w/v) benzalkonium chloride;

f) 0.005-0.015% (w/v) edetate disodium; and

g) water.

2. A composition consisting essentially of

a) 0.6% (w/v) olopatadine free base or an equivalent amount of a pharmaceutically acceptable salt of olopatadine;

b) 0.4-0.6% (w/v) dibasic sodium phosphate;

c) 0.35-0.45% (w/v) NaCl;

d) a pH-adjusting agent in an amount sufficient to cause the composition to have a pH of 3.6-3.8, wherein the pH-adjusting agent is selected from the group consisting of NaOH and HCl;

e) 0.01% (w/v) benzalkonium chloride;

f) 0.01% (w/v) edetate disodium; and

g) water.