US20030050303A1 - Solutions containing epinastin - Google Patents
Solutions containing epinastin Download PDFInfo
- Publication number
- US20030050303A1 US20030050303A1 US10/271,180 US27118002A US2003050303A1 US 20030050303 A1 US20030050303 A1 US 20030050303A1 US 27118002 A US27118002 A US 27118002A US 2003050303 A1 US2003050303 A1 US 2003050303A1
- Authority
- US
- United States
- Prior art keywords
- aqueous solution
- epinastine
- solution
- concentration
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 239000007864 aqueous solution Substances 0.000 claims abstract description 16
- 150000003839 salts Chemical class 0.000 claims abstract description 9
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000002253 acid Substances 0.000 claims abstract description 7
- 239000000243 solution Substances 0.000 claims description 27
- 210000000795 conjunctiva Anatomy 0.000 claims description 13
- 210000004400 mucous membrane Anatomy 0.000 claims description 10
- 210000003979 eosinophil Anatomy 0.000 claims description 9
- 230000004941 influx Effects 0.000 claims description 8
- 210000000440 neutrophil Anatomy 0.000 claims description 8
- 210000001519 tissue Anatomy 0.000 claims description 8
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000872 buffer Substances 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 230000035515 penetration Effects 0.000 claims description 4
- 239000003755 preservative agent Substances 0.000 claims description 4
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 3
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 3
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 2
- WPRAXAOJIODQJR-UHFFFAOYSA-N 1-(3,4-dimethylphenyl)ethanone Chemical compound CC(=O)C1=CC=C(C)C(C)=C1 WPRAXAOJIODQJR-UHFFFAOYSA-N 0.000 claims description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 claims description 2
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 2
- 239000005642 Oleic acid Substances 0.000 claims description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- 229920002125 Sokalan® Polymers 0.000 claims description 2
- 150000003973 alkyl amines Chemical class 0.000 claims description 2
- 150000001408 amides Chemical class 0.000 claims description 2
- 239000002280 amphoteric surfactant Substances 0.000 claims description 2
- 125000000129 anionic group Chemical group 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 125000002091 cationic group Chemical group 0.000 claims description 2
- 229960004926 chlorobutanol Drugs 0.000 claims description 2
- 150000002334 glycols Chemical class 0.000 claims description 2
- -1 heterocyclic amines Chemical class 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 2
- XEBWQGVWTUSTLN-UHFFFAOYSA-M phenylmercury acetate Chemical compound CC(=O)O[Hg]C1=CC=CC=C1 XEBWQGVWTUSTLN-UHFFFAOYSA-M 0.000 claims description 2
- 229920001983 poloxamer Polymers 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 229940069328 povidone Drugs 0.000 claims description 2
- RUOJZAUFBMNUDX-UHFFFAOYSA-N propylene carbonate Chemical compound CC1COC(=O)O1 RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 claims description 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 2
- 150000003462 sulfoxides Chemical class 0.000 claims description 2
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 claims description 2
- 229940033663 thimerosal Drugs 0.000 claims description 2
- WHWZLSFABNNENI-UHFFFAOYSA-N epinastine Chemical compound C1C2=CC=CC=C2C2CN=C(N)N2C2=CC=CC=C21 WHWZLSFABNNENI-UHFFFAOYSA-N 0.000 claims 4
- 229960003449 epinastine Drugs 0.000 claims 3
- 230000002335 preservative effect Effects 0.000 claims 2
- 229960002548 epinastine hydrochloride Drugs 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 description 12
- 235000002639 sodium chloride Nutrition 0.000 description 10
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 6
- 241001465754 Metazoa Species 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 108010058846 Ovalbumin Proteins 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 208000002205 allergic conjunctivitis Diseases 0.000 description 3
- 239000002738 chelating agent Substances 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 229960001340 histamine Drugs 0.000 description 3
- 229940092253 ovalbumin Drugs 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 description 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical group OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 229940125715 antihistaminic agent Drugs 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- 239000003125 aqueous solvent Substances 0.000 description 2
- 208000024998 atopic conjunctivitis Diseases 0.000 description 2
- 150000004683 dihydrates Chemical class 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- VKXSGUIOOQPGAF-UHFFFAOYSA-N epinastine hydrochloride Chemical compound [H+].[Cl-].C1C2=CC=CC=C2C2CN=C(N)N2C2=CC=CC=C21 VKXSGUIOOQPGAF-UHFFFAOYSA-N 0.000 description 2
- 210000003630 histaminocyte Anatomy 0.000 description 2
- 230000002045 lasting effect Effects 0.000 description 2
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 2
- 235000019799 monosodium phosphate Nutrition 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000002504 physiological saline solution Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 1
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 1
- 239000004255 Butylated hydroxyanisole Substances 0.000 description 1
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 1
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 1
- 206010010726 Conjunctival oedema Diseases 0.000 description 1
- 206010010741 Conjunctivitis Diseases 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 206010039094 Rhinitis perennial Diseases 0.000 description 1
- 208000036284 Rhinitis seasonal Diseases 0.000 description 1
- 239000004133 Sodium thiosulphate Substances 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 229960004308 acetylcysteine Drugs 0.000 description 1
- 208000030961 allergic reaction Diseases 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 206010069664 atopic keratoconjunctivitis Diseases 0.000 description 1
- XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
- 229940043253 butylated hydroxyanisole Drugs 0.000 description 1
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 description 1
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
- 229940095259 butylated hydroxytoluene Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 230000002327 eosinophilic effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000000744 eyelid Anatomy 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 230000007233 immunological mechanism Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 210000004698 lymphocyte Anatomy 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000005455 negative regulation of mast cell degranulation Effects 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 208000022719 perennial allergic rhinitis Diseases 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 229960004063 propylene glycol Drugs 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 208000017022 seasonal allergic rhinitis Diseases 0.000 description 1
- 230000001932 seasonal effect Effects 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 239000004296 sodium metabisulphite Substances 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 208000018464 vernal keratoconjunctivitis Diseases 0.000 description 1
Classifications
-
- F—MECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
- F01—MACHINES OR ENGINES IN GENERAL; ENGINE PLANTS IN GENERAL; STEAM ENGINES
- F01L—CYCLICALLY OPERATING VALVES FOR MACHINES OR ENGINES
- F01L9/00—Valve-gear or valve arrangements actuated non-mechanically
- F01L9/20—Valve-gear or valve arrangements actuated non-mechanically by electric means
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T137/00—Fluid handling
- Y10T137/0318—Processes
Definitions
- 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.
- Allergic reactions of the eye signifies a series of differently defined syndromes.
- Examples of allergic reactions of the nose include seasonal allergic rhinitis and perennial allergic rhinitis, for example.
- 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.
- 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.
- 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.
- 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.
- the animals pretreated with epinastin solution according to the invention (0.05-0.5%) had a significantly lower content of eosinophils in their conjunctiva.
- the animals pretreated with epinastin solution according to the invention had a significantly lower content of lymphocytes in their conjunctiva (p ⁇ 0.01).
- a roughly 35% inhibition of mast cell degranulation was determined (p ⁇ 0.01).
- the invention relates to topically administered aqueous solutions containing epinastin, 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.
- Suitable aqueous solvents are physiologically acceptable aqueous solvents, physiologically acceptable saline solutions being particularly preferred.
- 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 epinastin, 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.
- the preferred carrier which may be used in the solutions according to the invention is purified water and preferably a physiological saline solution.
- the excipients which may be used according to the invention include viscosity agents such as polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers and hydroxyethylcellulose.
- the preferred preservatives which may be used in the solutions according to the invention include benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate and phenyl mercury nitrate.
- the penetration promoters may be, for example, surfactants, specific organic solvents such as dimethylsulfoxide and other sulfoxides, dimethylacetamide and pyrrolidone, specific amides of heterocyclic amines, glycols such as propyleneglycol, propylene carbonate, oleic acid, alkylamines and derivatives thereof, various cationic, anionic, non-ionogenic and amphoteric surfactants and the like.
- specific organic solvents such as dimethylsulfoxide and other sulfoxides, dimethylacetamide and pyrrolidone
- specific amides of heterocyclic amines such as propyleneglycol, propylene carbonate, oleic acid, alkylamines and derivatives thereof
- various cationic, anionic, non-ionogenic and amphoteric surfactants and the like.
- Substances may be added as necessary or as desired in order to adjust the tonicity of the solution.
- Such substances include salts and especially sodium chloride, potassium chloride, mannitol and glycerol or other suitable physiologically acceptable agents for adjusting tonicity, without restricting the invention to the above.
- buffers and substances may be used to adjust the pH, provided that the preparation obtained is physiologically acceptable.
- These buffers might include acetate buffer, citrate buffer, phosphate buffer and borate buffer.
- physiologically acceptable antioxidants which may be used according to the invention include sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole and butylated hydroxytoluene, without restricting the invention to this list.
- carrier components which may be incorporated in the solutions according to the invention are chelating agents.
- the preferred chelating agent is disodium edetate (Na-EDTA), although other chelating agents may also be used instead of or in conjunction with disodium edetate.
- topically administered aqueous solutions according to the invention may be applied either to the conjunctiva or to the nasal mucous membrane. Solutions for ophthalmic use are of equal importance to solutions for nasal application for the purposes of the present invention.
- the invention relates not only to the solutions according to the invention mentioned hereinbefore but also to the use of the above-mentioned topically administered aqueous solutions for inhibiting the influx of neutrophils and eosinophils into the tissue of the ocular conjunctiva or the tissue of the nasal mucous membrane.
- the present invention also relates to the use of epinastin, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof, for producing the topically administered aqueous solutions according to the invention for treating disorders of the ocular conjunctiva or the nasal mucous membranes in which there is therapeutic value in inhibiting the influx of neutrophils and cosinophils into the tissue of the ocular conjunctiva or the nasal mucous membrane in allergic reactions.
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- Pulmonology (AREA)
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Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/271,180 US20030050303A1 (en) | 1999-11-12 | 2002-10-15 | Solutions containing epinastin |
| US11/215,165 US20050288274A1 (en) | 1999-11-12 | 2005-08-30 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/734,507 US20070197503A1 (en) | 1999-11-12 | 2007-04-12 | Solutions containing epinastin |
| US11/734,512 US20070185082A1 (en) | 1999-11-12 | 2007-04-12 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/863,008 US7429602B2 (en) | 1999-11-12 | 2007-09-27 | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US12/394,684 US20090239842A1 (en) | 1999-11-12 | 2009-02-27 | Solutions containing epinastin |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19954516.2 | 1999-11-12 | ||
| DE19954516A DE19954516A1 (de) | 1999-11-12 | 1999-11-12 | Epinastin-haltige Lösungen |
| US16777199P | 1999-11-29 | 1999-11-29 | |
| US70665000A | 2000-11-06 | 2000-11-06 | |
| US10/271,180 US20030050303A1 (en) | 1999-11-12 | 2002-10-15 | Solutions containing epinastin |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US70665000A Continuation | 1999-11-12 | 2000-11-06 |
Related Child Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US11/215,165 Continuation US20050288274A1 (en) | 1999-11-12 | 2005-08-30 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/734,512 Continuation US20070185082A1 (en) | 1999-11-12 | 2007-04-12 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/734,507 Continuation US20070197503A1 (en) | 1999-11-12 | 2007-04-12 | Solutions containing epinastin |
| US11/863,008 Continuation US7429602B2 (en) | 1999-11-12 | 2007-09-27 | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US12/394,684 Continuation US20090239842A1 (en) | 1999-11-12 | 2009-02-27 | Solutions containing epinastin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| US20030050303A1 true US20030050303A1 (en) | 2003-03-13 |
Family
ID=7928843
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US10/271,180 Abandoned US20030050303A1 (en) | 1999-11-12 | 2002-10-15 | Solutions containing epinastin |
| US11/215,165 Abandoned US20050288274A1 (en) | 1999-11-12 | 2005-08-30 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/734,507 Abandoned US20070197503A1 (en) | 1999-11-12 | 2007-04-12 | Solutions containing epinastin |
| US11/734,512 Abandoned US20070185082A1 (en) | 1999-11-12 | 2007-04-12 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/863,008 Expired - Lifetime US7429602B2 (en) | 1999-11-12 | 2007-09-27 | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US12/394,684 Abandoned US20090239842A1 (en) | 1999-11-12 | 2009-02-27 | Solutions containing epinastin |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US11/215,165 Abandoned US20050288274A1 (en) | 1999-11-12 | 2005-08-30 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/734,507 Abandoned US20070197503A1 (en) | 1999-11-12 | 2007-04-12 | Solutions containing epinastin |
| US11/734,512 Abandoned US20070185082A1 (en) | 1999-11-12 | 2007-04-12 | Treating rhinitis by topically administering an epinastine solution to the nasal mucous membrane |
| US11/863,008 Expired - Lifetime US7429602B2 (en) | 1999-11-12 | 2007-09-27 | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US12/394,684 Abandoned US20090239842A1 (en) | 1999-11-12 | 2009-02-27 | Solutions containing epinastin |
Country Status (40)
| Country | Link |
|---|---|
| US (6) | US20030050303A1 (cs) |
| EP (1) | EP1231920B1 (cs) |
| JP (1) | JP2003514021A (cs) |
| KR (1) | KR100758842B1 (cs) |
| CN (1) | CN1292752C (cs) |
| AR (1) | AR026424A1 (cs) |
| AT (1) | ATE353218T1 (cs) |
| AU (2) | AU784017B2 (cs) |
| BG (1) | BG65775B1 (cs) |
| BR (1) | BR0015477A (cs) |
| CA (1) | CA2391076C (cs) |
| CO (1) | CO5251448A1 (cs) |
| CY (1) | CY1106375T1 (cs) |
| CZ (1) | CZ302483B6 (cs) |
| DE (2) | DE19954516A1 (cs) |
| DK (1) | DK1231920T3 (cs) |
| EA (1) | EA006937B1 (cs) |
| EE (1) | EE05395B1 (cs) |
| ES (1) | ES2281359T3 (cs) |
| HK (1) | HK1052303B (cs) |
| HR (1) | HRP20020404B1 (cs) |
| HU (1) | HU229502B1 (cs) |
| IL (2) | IL149501A0 (cs) |
| ME (1) | MEP36708A (cs) |
| MX (1) | MXPA02004556A (cs) |
| MY (1) | MY130441A (cs) |
| NO (1) | NO329417B1 (cs) |
| NZ (1) | NZ519425A (cs) |
| PE (1) | PE20010826A1 (cs) |
| PL (1) | PL198879B1 (cs) |
| PT (1) | PT1231920E (cs) |
| RS (1) | RS50173B (cs) |
| SA (1) | SA01210658B1 (cs) |
| SI (1) | SI1231920T1 (cs) |
| SK (1) | SK287343B6 (cs) |
| TR (1) | TR200201270T2 (cs) |
| TW (1) | TWI225401B (cs) |
| UA (1) | UA74563C2 (cs) |
| WO (1) | WO2001035962A1 (cs) |
| ZA (1) | ZA200203683B (cs) |
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| US20040247686A1 (en) * | 2003-04-04 | 2004-12-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions comprising epinastine for the treatment of skin diseases |
| US20050084527A1 (en) * | 2002-08-02 | 2005-04-21 | Boehringer Ingelheim International Gmbh | Pharmaceutical formulations containing combinations of epinastine, pseudoephedrine, and methylephedrine |
| US20060073172A1 (en) * | 2004-10-01 | 2006-04-06 | Schneider L W | Stabilized ophthalmic solution for the treatment of glaucoma and lowering intraocular pressure |
| US20070197503A1 (en) * | 1999-11-12 | 2007-08-23 | Volker Trach | Solutions containing epinastin |
| US7378082B1 (en) | 2007-11-05 | 2008-05-27 | Inspire Pharmaceuticals, Inc. | Method for treating allergic rhinitis without adverse effects |
| US20080194544A1 (en) * | 2007-02-08 | 2008-08-14 | Ramesh Krishnamoorthy | Aqueous formulations of epinastine for treating allergic rhinitis |
| US20090143359A1 (en) * | 2005-07-08 | 2009-06-04 | Akiharu Isowaki | Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine |
| CN112969465A (zh) * | 2018-10-31 | 2021-06-15 | 参天制药株式会社 | 抑制软性隐形眼镜变质的眼科用组合物 |
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| EP1468696A1 (en) * | 2003-04-17 | 2004-10-20 | Boehringer Ingelheim International GmbH | Combinations of epinastine and antiphlogisitcs as new pharmaceutical compositions for the treatment of skin diseases |
| WO2008098122A2 (en) * | 2007-02-08 | 2008-08-14 | Inspire Pharmaceuticals, Inc. | Method for treating allergic rhinitis without adverse effects |
| WO2011019940A2 (en) * | 2009-08-12 | 2011-02-17 | Seros Medical, Llc | Deuterated water and riboflavin solution for extending singlet oxygen lifetimes in treatment of ocular tissue and method for use |
| TWI544922B (zh) | 2011-05-19 | 2016-08-11 | 愛爾康研究有限公司 | 高濃度歐羅派特錠（ｏｌｏｐａｔａｄｉｎｅ）眼用組成物 |
| EP2630952A1 (en) * | 2012-02-23 | 2013-08-28 | Novagali Pharma S.A. | Self-preserved oil dispersions comprising boric acid |
| KR101891144B1 (ko) * | 2012-12-19 | 2018-08-23 | 에스에이알코드 바이오사이언스 인코포레이티드 | Lfa-1 저해제 제형 |
| CN104491876A (zh) * | 2014-12-23 | 2015-04-08 | 中国药科大学 | 含玻璃酸钠的依匹斯汀滴眼液及其制备方法 |
| ITUB20153950A1 (it) * | 2015-09-28 | 2017-03-28 | Tred Srl | Dispositivo nasale in grado di attivare il riflesso rino-palatale per l'igienizzazione rinofaringea |
| JP6134853B1 (ja) * | 2016-10-28 | 2017-05-24 | 参天製薬株式会社 | エピナスチン含有点眼液 |
| JP6635974B2 (ja) * | 2017-04-24 | 2020-01-29 | 参天製薬株式会社 | エピナスチン含有点眼液 |
| WO2018203424A1 (ja) * | 2017-05-01 | 2018-11-08 | 参天製薬株式会社 | 点眼剤 |
| JP7599838B2 (ja) * | 2019-04-10 | 2024-12-16 | 参天製薬株式会社 | エピナスチン又はその塩を含有する水性医薬組成物 |
| JP6736752B2 (ja) * | 2019-12-17 | 2020-08-05 | 参天製薬株式会社 | エピナスチン含有点眼液 |
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| JP7114668B2 (ja) * | 2020-10-08 | 2022-08-08 | 参天製薬株式会社 | エピナスチン又はその塩を含有する花粉破裂抑制剤 |
| CN115448927A (zh) * | 2022-10-20 | 2022-12-09 | 重庆瑞泊莱医药科技有限公司 | 一种氢溴酸依匹斯汀晶型ii及其制备方法 |
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- 2000-10-14 IL IL14950100A patent/IL149501A0/xx unknown
- 2000-10-14 PL PL364028A patent/PL198879B1/pl unknown
- 2000-10-14 UA UA2002064760A patent/UA74563C2/uk unknown
- 2000-10-14 WO PCT/EP2000/010122 patent/WO2001035962A1/de active IP Right Grant
- 2000-10-14 BR BR0015477-6A patent/BR0015477A/pt not_active Application Discontinuation
- 2000-10-14 HK HK03104651.9A patent/HK1052303B/zh not_active IP Right Cessation
- 2000-10-14 PT PT00972763T patent/PT1231920E/pt unknown
- 2000-10-14 HR HR20020404A patent/HRP20020404B1/xx not_active IP Right Cessation
- 2000-10-14 CZ CZ20021956A patent/CZ302483B6/cs not_active IP Right Cessation
- 2000-10-14 TR TR2002/01270T patent/TR200201270T2/xx unknown
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- 2000-10-14 JP JP2001537955A patent/JP2003514021A/ja active Pending
- 2000-10-14 HU HU0203773A patent/HU229502B1/hu unknown
- 2000-10-14 ME MEP-367/08A patent/MEP36708A/xx unknown
- 2000-10-14 DK DK00972763T patent/DK1231920T3/da active
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- 2000-10-14 AT AT00972763T patent/ATE353218T1/de active
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Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070197503A1 (en) * | 1999-11-12 | 2007-08-23 | Volker Trach | Solutions containing epinastin |
| US20080009476A1 (en) * | 1999-11-12 | 2008-01-10 | Volker Trach | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US7429602B2 (en) | 1999-11-12 | 2008-09-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Treating conjunctivitis by topically administering an epinastine solution to the conjunctiva |
| US20090239842A1 (en) * | 1999-11-12 | 2009-09-24 | Volker Trach | Solutions containing epinastin |
| US20050084527A1 (en) * | 2002-08-02 | 2005-04-21 | Boehringer Ingelheim International Gmbh | Pharmaceutical formulations containing combinations of epinastine, pseudoephedrine, and methylephedrine |
| US20040247686A1 (en) * | 2003-04-04 | 2004-12-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions comprising epinastine for the treatment of skin diseases |
| US20060073172A1 (en) * | 2004-10-01 | 2006-04-06 | Schneider L W | Stabilized ophthalmic solution for the treatment of glaucoma and lowering intraocular pressure |
| US20090143359A1 (en) * | 2005-07-08 | 2009-06-04 | Akiharu Isowaki | Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine |
| US20080194544A1 (en) * | 2007-02-08 | 2008-08-14 | Ramesh Krishnamoorthy | Aqueous formulations of epinastine for treating allergic rhinitis |
| US7378082B1 (en) | 2007-11-05 | 2008-05-27 | Inspire Pharmaceuticals, Inc. | Method for treating allergic rhinitis without adverse effects |
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