Nasal and ophthalmic delivery of aqueous corticosteroid solutions

Patent metadata

Field	Value
Publication number	US-12370352-B2
Application number	US-202117387929-A
Country	US
Kind code	B2
Filing date	Jul 28, 2021
Priority date	Jun 28, 2007
Publication date	Jul 29, 2025
Grant date	Jul 29, 2025

Abstract

The present invention is directed to methods of treating nasal and/or ophthalmic diseases, symptoms, or disorders that are therapeutically responsive to corticosteroid therapy by delivering aqueous solution formulations comprising a corticosteroid to nasal and ophthalmic tissues. The invention is also directed to methods, systems, devices, and compositions for delivering aqueous solution formulations comprising a corticosteroid and an antihistamine to nasal and ophthalmic tissues.

First claim

The invention claimed is:

1. A method for treating an allergic symptom or disorder in a subject in need thereof, comprising: nasally administering by a pump sprayer to the subject a solution comprising a therapeutically effective amount of budesonide, SAE-CD, an antihistamine, and a pharmaceutically acceptable aqueous liquid carrier, wherein the molar ratio of SAE-CD to budesonide is about 47:1, wherein the budesonide is present in an amount of about 30 μg per unit dose, and wherein the antihistamine is present in an amount of about 137 μg per unit dose;
wherein the therapeutically effective amount is administered in one unit dose per nostril;
wherein the antihistamine is azelastine or a pharmaceutically acceptable salt thereof;
wherein the SAE-CD is sulfobutylether β-cyclodextrin; and
wherein the method provides more rapid relief from the allergy symptom or disorder compared to a budesonide suspension at the same unit dose.

2. The method of claim 1 , wherein the allergic symptom or disorder includes a non-nasal symptom selected from the group consisting of: itchy or gritty eyes, tearing or watery eyes, red or burning eyes, itchy ears or palate, and combinations thereof.

3. The method of claim 1 , wherein the allergic symptom or disorder further comprises symptoms selected from the group consisting of runny nose, itchy nose, nasal congestion, sneezing and combinations thereof.

4. The method of claim 1 , wherein the solution is administered to the subject 1-2 times per day.

5. A method for treating an ocular symptom or disorder in a subject in need thereof, comprising: nasally administering by a pump sprayer to the subject a solution comprising a therapeutically effective amount of budesonide, SAE-CD, an antihistamine and a pharmaceutically acceptable aqueous liquid carrier, wherein the molar ratio of SAE-CD to budesonide is about 47:1, wherein the budesonide is present in an amount of about 30 μg per unit dose, and wherein the antihistamine is present in an amount of about 137 μg per unit dose;
wherein the therapeutically effective amount is administered in one unit dose per nostril;
wherein the antihistamine is azelastine or a pharmaceutically acceptable salt thereof;
wherein the SAE-CD is sulfobutylether β-cyclodextrin;
wherein the method provides more rapid relief from the ocular symptom or disorder compared to a budesonide suspension at the same unit dose.

6. The method of claim 5 , wherein the ocular symptom or disorder includes a non-nasal symptom selected from the group consisting of itchy or gritty eyes, tearing or watery eyes, red or burning eyes, itchy ears or palate, and combinations thereof.

7. The method of claim 5 , wherein the solution is administered to the subject 1-2 times per day.

8. A method for treating ocular inflammation in a subject in need thereof, comprising: ophthalmically administering to the subject a solution comprising a therapeutically effective amount of budesonide, SAE-CD, an antihistamine and a pharmaceutically acceptable aqueous liquid carrier, wherein the molar ratio of SAE-CD to budesonide is about 47:1, wherein the budesonide is present in an amount of about 30 μg per unit dose, and wherein the antihistamine is present in an amount of about 137 μg per unit dose;
wherein the therapeutically effective amount is administered in one unit dose per nostril;
wherein the budesonide solution provides more rapid reduction in ocular inflammation compared with a budesonide suspension at the same unit dose;
wherein the SAE-CD is sulfobutylether β-cyclodextrin;
wherein the antihistamine is azelastine or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the solution is administered to the subject 1-2 times per day.

Assignees

• Cydex Pharmaceuticals Inc

Inventors

• Pipkin James D
• Zimmerer Jr Rupert O
• Siebert John M

Classifications

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/57

  substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone · CPC title

• A61K31/335 Primary

  having oxygen as the only ring hetero atom, e.g. fungichromin · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K47/40

  Cyclodextrins; Derivatives thereof · CPC title