Solutions containing epinastin

a technology of epinastin and solution, applied in the field of topically administered aqueous solutions containing epinastin, can solve the problems of ocular and nasal allergic reactions

Inactive Publication Date: 2007-08-23
TRACH VOLKER +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The solutions significantly reduce eosinophil and neutrophil content in the conjunctiva, inhibit mast cell degranulation, and provide a 35% inhibition of late phase reactions, demonstrating a longer duration of activity in animal models.

Problems solved by technology

Moreover, ocular and nasal allergic reactions may be due to the release of other mast cell mediators as well as toxic eosinophilic granule proteins and enzymes.

Method used

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Examples

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Embodiment Construction

[0007] It has been found, surprisingly, that topically administrable aqueous solutions containing epinastin, optionally in the form of its racemate, its enantiomers and possibly in the form of the pharmacologically acceptable acid addition salts thereof, may be used to solve the problem on which the invention is based, since they inhibit the influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva and nasal mucous membrane, thereby reducing or preventing the occurrence of LPR and are accordingly characterized by a longer lasting duration of activity.

[0008] The compound epinastin (3-amino-9,13b-dihydro-1H-dibenz-[c,f]imidazol[1,5-a]azepine) and the acid addition salts thereof were described for the first time in German Patent Application P 30 08 944.2.

[0009] The effect of the topically administered solutions containing epinastin as inhibitors of the influx of eosinophils and neutrophils was demonstrated using the so-called passive ocular anaphylaxis model in ...

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PUM

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Abstract

Topically administered aqueous solutions containing epinastin, optionally in the form of its racemate or its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof.

Description

RELATED APPLICATIONS [0001] This application is a continuation of U.S. Ser. No. 09 / 706,650, filed Nov. 6, 2000.FIELD OF THE INVENTION [0002] The invention relates to topically administered aqueous solutions containing epinastin, optionally in the form of its racemates, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof. BACKGROUND OF THE INVENTION [0003] Allergic reactions of the eye (hereinafter referred to as ocular allergic reactions) signifies a series of differently defined syndromes. The following are examples of ocular allergic reactions, e.g., seasonal allergic conjunctivitis, perennial allergic conjunctivitis, giant cell conjunctivitis, vernal keratoconjunctivitis or atopic keratoconjunctivitis. Examples of allergic reactions of the nose (hereinafter referred to as nasal allergic reactions) include seasonal allergic rhinitis and perennial allergic rhinitis, for example. [0004] The immunological mechanism on which ocula...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/55A61K9/08F01L9/20A61K9/00A61P27/02A61P27/16A61P37/08A61P43/00H01F7/18H02K33/04
CPCA61K9/0043Y10S514/912A61K31/55A61K9/0048Y10T137/0318A61P11/00A61P11/02A61P27/00A61P27/02A61P27/14A61P27/16A61P37/08A61P43/00F01L9/20
InventorTRACH, VOLKERDUSCHLER, GEROLD
OwnerTRACH VOLKER