WO1998047510A1 - Collyre - Google Patents

Collyre Download PDF

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Publication number
WO1998047510A1
WO1998047510A1 PCT/JP1998/001918 JP9801918W WO9847510A1 WO 1998047510 A1 WO1998047510 A1 WO 1998047510A1 JP 9801918 W JP9801918 W JP 9801918W WO 9847510 A1 WO9847510 A1 WO 9847510A1
Authority
WO
WIPO (PCT)
Prior art keywords
eye drops
drugs
present
hydrochloride
vasoconstrictor
Prior art date
Application number
PCT/JP1998/001918
Other languages
English (en)
Japanese (ja)
Inventor
Ichiro Okudaira
Kenji Tsunoda
Original Assignee
Taisho Pharmaceutical Co., Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Taisho Pharmaceutical Co., Ltd. filed Critical Taisho Pharmaceutical Co., Ltd.
Priority to AU70815/98A priority Critical patent/AU7081598A/en
Publication of WO1998047510A1 publication Critical patent/WO1998047510A1/fr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine

Definitions

  • the present invention relates to eye drops. Specifically, it is an ophthalmic solution that has an excellent effect of reducing and eliminating congestive symptoms of the ocular mucosa, among other symptoms of conjunctivitis.
  • Conjunctivitis is an inflammatory disease of the ocular mucosa, caused by a variety of causes, including bacterial infection, viral infection, allergy, and traumatic disease.
  • antibiotics, antibacterial drugs, antiallergic drugs, etc. are administered according to the etiology of the causative therapy.
  • symptomatic treatment to reduce and eliminate ocular mucosal hyperemia such as conjunctival congestion, subconjunctival hemorrhage, and conjunctival edema at an early stage is not possible from the viewpoint of Q0L and serious symptoms. It is regarded as a therapeutic point from the viewpoint of preventing migration, and is an important factor especially in drug development.
  • vasoconstrictors As such symptomatic treatment, vasoconstrictors, corticosteroids, and the like are currently used, but administration of these drugs alone cannot be said to have obtained sufficient effects from the above viewpoint.
  • An object of the present invention is to provide an ophthalmic solution having a high effect on congestion of the ocular mucosa among various symptoms of conjunctivitis. Disclosure of the invention
  • the present inventors have conducted intensive studies to achieve the above-mentioned object.
  • the inventors have found a dramatic effect on the removal and completed the present invention.
  • the present invention does not include a vasoconstrictor and ketotifen or a salt thereof. Eye drops.
  • the amount of the vasoconstrictor is 0.0005 to 0.5% by weight, and the amount of the ketothiophene or a salt thereof is 0.05 to 1% by weight based on the total amount of the preparation. Agent.
  • vasoconstrictor used in the ophthalmic solution of the present invention examples include naphazolin, tetrahydrozolin, oximetazoline, phenylephrine, efdolins, epinephrine and the like, and salts thereof.
  • examples include hydrochloride and nitrate. These can be used alone or in combination of two or more.
  • the compounding amount of each active ingredient with respect to the total amount of the ophthalmic preparation of the present invention is preferably 0.0005 to 0.5% by weight, particularly 0.001 to 0.35% by weight for the vasoconstrictor. I like it. If the vasoconstrictor is less than 0.0005% by weight, a sufficient decongestant effect cannot be obtained, and if it exceeds 0.5% by weight, resistance to the action is undesirably produced.
  • the content of ketotifen or a salt thereof is preferably from 0.05 to 1% by weight, and particularly preferably from 0.01 to 0.75% by weight.
  • the amount of ketotifin or a salt thereof is less than 0.05% by weight, a sufficient antiallergic effect cannot be obtained, and if it exceeds 1% by weight, side effects such as drowsiness and the like on the central nervous system may occur. It is not preferable.
  • antiallergic drugs in addition to the above active ingredients, if necessary, other antiallergic drugs, antihistamines, local anesthetics, anticholinergics, steroid antiinflammatory drugs, anti-inflammatory enzyme drugs, anti-inflammatory drugs, Bactericides, vitamins, crude drugs and the like can be added.
  • the eye drops of the present invention can be prepared into solid eye drops or liquid eye drops by a conventional method.
  • the excipients used in the preparation of pharmaceuticals include excipients such as crystalline cellulose in the case of solid eye drops, binders such as hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, PVP, and stearyl. There are lubricants such as magnesium phosphate, hardened castor oil and talc, preservatives, etc.
  • surfactants, solubilizers, buffers, etc., as well as preservatives, fragrances (menthol, Camphor and the like, pigments, preservatives and the like can be used.
  • the eye drops of the present invention are usually administered to an adult by dropping, spraying or applying an appropriate amount once or several times to both eyes at a time.
  • Example 2 The above-mentioned components and amounts were weighed and dissolved in purified water (100 m) according to a conventional method to produce. (Example 2)
  • Example 3 The above components and amounts were weighed, and dissolved in 100 ml of purified water by a conventional method to produce. (Example 3)
  • Example 4 The above components and amounts were weighed and dissolved in 100 ml of purified water by a conventional method to produce. (Example 4)
  • the ophthalmic solution of the present invention contains a vasoconstrictor and ketotiphan or a salt thereof, it remarkably reduces and eliminates hyperemia of the ocular mucosa among various symptoms of conjunctivitis.
  • the eye drops of the present invention may further contain other antiallergic drugs, antihistamines, local anesthetics, anticholinergics, steroid anti-inflammatory drugs, anti-inflammatory enzyme drugs, anti-inflammatory drugs, bactericides, and vitamins. Since it can be formulated with minerals, crude drugs, etc., it can be used as a prescription drug or a general therapeutic drug as an over-the-counter drug suited to various symptoms of conjunctivitis.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un collyre contenant un vasoconstricteur et du kétotifène ou l'un de ses sels. De par sa composition, ce collyre permet de soulager, entre autres symptômes de conjonctivite, la congestion de la muqueuse ophtalmique.
PCT/JP1998/001918 1997-04-24 1998-04-24 Collyre WO1998047510A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU70815/98A AU7081598A (en) 1997-04-24 1998-04-24 Eye drops

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP10785097 1997-04-24
JP9/107850 1997-04-24

Publications (1)

Publication Number Publication Date
WO1998047510A1 true WO1998047510A1 (fr) 1998-10-29

Family

ID=14469654

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1998/001918 WO1998047510A1 (fr) 1997-04-24 1998-04-24 Collyre

Country Status (2)

Country Link
AU (1) AU7081598A (fr)
WO (1) WO1998047510A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008026756A1 (fr) * 2006-08-28 2008-03-06 Senju Pharmaceutical Co., Ltd. Préparation ophtalmique du type à absorption par voie percutanée
EP3653205A3 (fr) * 2011-03-03 2020-08-26 Voom, LLC Oxymethazoline pour administration topique oculaire et ses utilisations

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62277323A (ja) * 1986-02-19 1987-12-02 Sankyo Co Ltd フマル酸ケトチフエン含有点眼液の製法
JPH03128332A (ja) * 1989-07-12 1991-05-31 Eisai Co Ltd α↓1―ブロッカー点眼剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62277323A (ja) * 1986-02-19 1987-12-02 Sankyo Co Ltd フマル酸ケトチフエン含有点眼液の製法
JPH03128332A (ja) * 1989-07-12 1991-05-31 Eisai Co Ltd α↓1―ブロッカー点眼剤

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008026756A1 (fr) * 2006-08-28 2008-03-06 Senju Pharmaceutical Co., Ltd. Préparation ophtalmique du type à absorption par voie percutanée
EP3653205A3 (fr) * 2011-03-03 2020-08-26 Voom, LLC Oxymethazoline pour administration topique oculaire et ses utilisations
US10912765B2 (en) 2011-03-03 2021-02-09 Voom, Llc Compositions and methods for non-surgical treatment of ptosis

Also Published As

Publication number Publication date
AU7081598A (en) 1998-11-13

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