Olopatadine formulations for topical nasal administration

• US 7,977,376 B2
• Filed: 02/07/2007
• Issued: 07/12/2011
• Est. Priority Date: 06/27/2001
• Status: Expired due to Term

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: Jani, Rajni, Wall, G. Michael, Chowhan, Masood A., Singh, Onkar N., Han, Wesley Wehsin
• Primary Examiner(s): Duffy; Patricia A
• Assistant Examiner(s): Shomer; Isaac
• Application Number:
  US11/703,373
• Publication Number:
  US 20070142458A1
• Time in Patent Office: 1,616 Days
• Field of Search: None
• 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 topically administrable, aqueous, nasal spray solution composition consisting of

a) 0.665% (w/v) olopatadine hydrochloride;

b) a phosphate salt in an amount equivalent to 0.4-0.6% (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) 0.35-0.45% (w/v) NaCl;

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

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

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

g) water;

wherein the composition has an osmolality of 260-330 mOsm/kg.

2. A topically administrable, aqueous, nasal spray solution composition consisting of

a) 0.665% (w/v) olopatadine hydrochloride;

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

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

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

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

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

g) water;

wherein the composition has an osmolality of 260-330 mOsm/kg.