Compositions comprising azelastine and methods of use thereof

Inactive Publication Date: 2007-01-25
MEDA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0023] The present invention also provides methods of treating or preventing allergic rhinitis, non-allergic vasomotor rhinitis or allergic conjunctivitis in an animal, such as a human, suffering from or predisposed there

Problems solved by technology

Despite its effectiveness, azelastine hydrochloride possesses a strong bitter taste.
This bitter taste is so intense that it was found to be unpleasant even at a dilution of 1×106 (see U.S. Pat. No. 5,164,194).
However, subsequent clinical studies have shown that the bitter taste of azelastine hydrochloride is, indeed, an undesired element as a porti

Method used

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  • Compositions comprising azelastine and methods of use thereof
  • Compositions comprising azelastine and methods of use thereof
  • Compositions comprising azelastine and methods of use thereof

Examples

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example 1

Azelastine Hydrochloride Nasal Solution

[1224] In one exemplary composition of the invention, a nasal spray formulation containing azelastine hydrochloride was prepared using hypromellose as a thickener, sorbitol as an isotonicity agent and sweetener, and sucralose as both a sweetener and a taste-masking agent.

Ingredient%Azelastine Hydrochloride0.150Hypromellose 2900, USP 40000.100Edetate Disodium, USP0.050Sorbitol 70%, USP6.400Sodium Citrate, USP, Dihydrate0.068Sucralose, NF0.150Benzalkonium Chloride 50% Solution, NF0.025Water Purified or DeionizedQ.S. to 100%

[1225] Following preparation, the composition was filtered, and was packaged into high density polyethylene bottles fitted with a screw cap and comprising a VP3 metered-dose spray pump designed for intranasal application in a volume of about 0.14 ml (Valois). For use, one or two sprays were administered to each nostril two times per day, or as prescribed.

example 2

Azelastine Hydrochloride Nasal Solution

[1226] In another exemplary composition provided by the present invention, a nasal spray formulation containing azelastine hydrochloride was prepared using hypromellose as a thickener and sucralose and menthol as taste-masking agents:

Ingredient%Azelastine Hydrochloride0.100Hypromellose 2900, USP 40000.300Edetate Disodium, USP0.050Sodium Citrate, USP, Dihydrate0.068Sucralose, NF0.050Propylene Glycol, USP1.895Menthol, USP0.050Benzalkonium Chloride 50%, NF0.025Water Purified or DeionizedQ.S. to 100%

[1227] Following preparation, the composition was filtered, and was packaged into high density polyethylene bottles fitted with a screw cap and comprising a VP3 metered-dose spray pump designed for intranasal application in a volume of about 0.14 ml (Valois). For use, one or two sprays were administered to each nostril two times per day, or as prescribed.

example 3

Azelastine Hydrochloride Nasal Solution

[1228] In another exemplary composition of the invention, a nasal spray formulation containing azelastine hydrochloride was prepared using hypromellose as a thickener, sodium chloride as an isotonicity agent, and sucralose as both a sweetener and a taste-masking agent.

Ingredient%Azelastine Hydrochloride0.100Hypromellose 2900, USP 40000.100Edetate Disodium, USP0.050Citric Acid Anhydrous, USP0.044Dibasic Sodium Phosphate Heptahydrate, USP0.486Sodium Chloride, USP0.687Sucralose, NF0.150Benzalkonium Chloride 50% Solution, NF0.025Water Purified or DeionizedQ.S. to 100%

[1229] Following preparation, the composition was filtered, and was packaged into high density polyethylene bottles fitted with a screw cap and comprising a VP3 metered-dose spray pump designed for intranasal application in a volume of about 0.14 ml (Valois). For use, one or two sprays were administered to each nostril about two times per day, or as prescribed.

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Abstract

The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent. The invention also provides methods of treating or preventing certain disorders, or symptomatic relief therefrom, by administering the compositions of the invention to a patient, e.g., for the symptomatic relief of allergic rhinitis, non-allergic vasomotor rhinitis, allergic conjunctivitis, as well as other disorders. The compositions and methods of the present invention provide significant value in terms of patient acceptability, convenience, and compliance.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] The present application is a continuation-in-part of U.S. application Ser. No. 11 / 284,109, filed Nov. 22, 2005, which claims the benefit of the filing date of U.S. Provisional Patent Application No. 60 / 630,274, filed Nov. 24, 2004, the disclosures of each of which are incorporated herein by reference in their entireties.BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention is in the fields of pharmaceuticals, formulations chemistry and pharmacology. The invention generally relates to compositions comprising azelastine or pharmaceutically acceptable salts or esters thereof, including azelastine hydrochloride. In certain embodiments, the invention provides pharmaceutical compositions comprising azelastine hydrochloride formulated for use as nasal sprays and / or ocular solutions or drops, as well as dosage formulations for oral and pulmonary delivery. The invention also relates to methods of use of such c...

Claims

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Application Information

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IPC IPC(8): A61K31/7012A61K31/56A61K31/55A61K31/573
CPCA61K9/0043A61K9/0048A61K9/0056A61K9/0073A61K9/7007A61K45/06A61K31/55A61K2300/00A61K31/56A61K31/573A61K31/58A61P11/02A61P27/14A61P29/00A61P37/08
Inventor DANG, PHUONG GRACELAWRENCE, BRIAN D.BALWANI, GULD'ADDIO, ALEXANDER D.
Owner MEDA PHARMA INC
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