| Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane -> Monitor Keywords |
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Treating rhinitis by topically administering an epinastine solution to the nasal mucous membraneRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Seven-membered Consisting Of One Nitrogen And Six Carbons, Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The CyclosTreating rhinitis by topically administering an epinastine solution to the nasal mucous membrane description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070185082, Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane. Brief Patent Description - Full Patent Description - Patent Application Claims
RELATED APPLICATIONS [0001] This application is a continuation of U.S. Ser. No. 10/271,180, filed Oct. 15, 2002, which is a continuation of U.S. Ser. No. 09/706,650, filed Nov. 6, 2000, now abandoned, which claims priority to German Application No. 199 54 516.2, filed Nov. 12, 1999, and claims benefit of U.S. Provisional Application Ser. No. 60/167,771, filed on Nov. 29, 1999, each of which is hereby incorporated by reference. FIELD OF THE INVENTION [0002] The invention relates to topically administered aqueous solutions containing epinastine, 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 ocular and nasal allergic reactions are based comprises, inter alia, inflammatory processes caused by histamine. The allergic reactions produced by the release of histamine occur at an early stage of the ocular and nasal allergic reactions mentioned above. 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. The influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva and the nasal mucous membrane leads to a late phase reaction, hereinafter referred to as LPR. LPR normally occurs within a period of 3-6 hours after the initial histamine-mediated allergic reaction. LPR is also characterized by the occurrence of vasodilation and chemosis and by the swelling of the conjunctiva and the nasal mucous membrane. [0005] Whereas histamine-produced allergic reactions can be counteracted by administering antihistamines, the influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva and the nasal mucous membrane remains unaffected by administering pure antihistamines. Problem of the Invention [0006] The problem of the present invention is therefore to provide topically administrable solutions which inhibit the influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva and the nasal mucous membrane, thereby reducing or preventing the occurrence of LPR and are therefore characterized by a longer lasting duration of activity. DETAILED DESCRIPTION OF THE INVENTION [0007] It has been found, surprisingly, that topically administrable aqueous solutions containing epinastine, 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 epinastine (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 epinastine as inhibitors of the influx of eosinophils and neutrophils was demonstrated using the so-called passive ocular anaphylaxis model in rats. DESCRIPTION OF EMBODIMENT [0010] 72 hours after the rats have been sensitized by injecting antiserum into the eyelids of the test animals, a fresh provocation was induced in them by intravenous administration of ovalbumin. Some of the experimental animals were pretreated by the administration of solution containing epinastine according to the invention into the conjunctival sac 15 minutes before the ovalbumin is administered. Two hours after the administration of ovalbumin the experimental animals were killed and the conjunctiva was investigated for its content of eosinophils and neutrophils and the mast cell granulation was determined. Results [0011] The animals pretreated with epinastine solution according to the invention (0.05-0.5%) had a significantly lower content of eosinophils in their conjunctiva. The animals pretreated with epinastine solution according to the invention had a significantly lower content of lymphocytes in their conjunctiva (p<0.01). In the animals pretreated with epinastine solution according to the invention, a roughly 35% inhibition of mast cell degranulation was determined (p<0.01). [0012] Consequently, the invention relates to topically administered aqueous solutions containing epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable addition salts thereof, in a concentration of 0.005 to 0.5, preferably 0.02 to 0.1, most preferably 0.03 to 0.07 mg/ml of solution. [0013] The abovementioned topically administered aqueous solutions containing epinastine hydrochloride are preferred according to the invention. [0014] Suitable aqueous solvents are physiologically acceptable aqueous solvents, physiologically acceptable saline solutions being particularly preferred. [0015] According to the invention, topically administered solutions are preferably prepared which typically contain 0.005 to 0.5, preferably 0.02 to 0.1, most preferably 0.03 to 0.07 mg/ml of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof, as well as physiological saline solutions as the main carriers. The pH of the solutions according to the invention should preferably be maintained within the range from 6.5 to 7.2 by means of a suitable buffer system. The preparations may also contain conventional, pharmaceutically acceptable excipients, preservatives, stabilizers, and/or penetration promoters. [0016] The preferred carrier which may be used in the solutions according to the invention is purified water and preferably a physiological saline solution. [0017] Without restricting the subject matter of the invention to the following, the excipients which may be used according to the invention include viscosity agents such as polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers, and hydroxyethylcellulose. Continue reading about Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane... 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