Sustained release intranasal formulation and method of use thereof

• US 4,581,225 A
• Filed: 01/28/1985
• Issued: 04/08/1986
• Est. Priority Date: 04/25/1984
• Status: Expired due to Fees

• Current Assignee: Abtco Incorporated
• Original Assignee: Eli Lilly and Company
• Inventors: Campanale, Kristina M., Wilson, Harve C., Su, Kenneth S. E.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/695,491
• Time in Patent Office: 435 Days
• Field of Search: 424/45
• US Class Current: 424/45
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/0043 Nose

Abstract

Administration of a catecholamine by a novel intranasal delivery system provides prolonged blood levels of the drug.

Claims

1. A sustained release intranasal formulation comprising from about 0.5 to about 20.0 percent by weight of a catecholamine, from about 0.005 to about 5.0 percent by weight of an emulsifying agent suspended in from about 40.0 to about 97.0 percent by weight of a suitable freon aerosol propellant dispersion medium and from about 0.5 to about 50.0 percent by weight of a sustained release agent of the formula

View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)

2. A formulation of claim 1 wherein the catecholamine is dobutamine hydrochloride.

3. A formulation of claim 1 wherein the emulsifying agent is poloxyethylene 20 sorbitan trioleate.

4. A formulation of claim 1 wherein R¹ is C₈ -C₁₀ alkyl.

5. A formulation of claim 4 wherein the sustained release agent is oleic acid.

6. A formulation of claim 1 wherein R¹ is C₈ -C₁₀ alkenyl.

7. A formulation of claim 6 wherein the sustained release agent is linoleic acid.

8. A method for increasing cardiac contractibility in a warm-blooded animal in need of such therapy comprising administering to said animal a therapeutically effective amount of a sustained release intranasal formulation of claim 1.

9. A method of claim 8 wherein the intranasal formulat contains dobutamine as the catecholamine.

10. A method of claim 8 wherein the intranasal formulation contains oleic acid as the sustained release agent.