WO2005100362A1 - Preparation externe liquide contenant du pranoprofene - Google Patents

Preparation externe liquide contenant du pranoprofene Download PDF

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Publication number
WO2005100362A1
WO2005100362A1 PCT/JP2004/013896 JP2004013896W WO2005100362A1 WO 2005100362 A1 WO2005100362 A1 WO 2005100362A1 JP 2004013896 W JP2004013896 W JP 2004013896W WO 2005100362 A1 WO2005100362 A1 WO 2005100362A1
Authority
WO
WIPO (PCT)
Prior art keywords
external preparation
liquid external
present
pranoprofen
liquid
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.)
Ceased
Application number
PCT/JP2004/013896
Other languages
English (en)
Japanese (ja)
Inventor
Katsuya Shimoo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kobayashi Pharmaceutical Co Ltd
Original Assignee
Kobayashi 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 Kobayashi Pharmaceutical Co Ltd filed Critical Kobayashi Pharmaceutical Co Ltd
Publication of WO2005100362A1 publication Critical patent/WO2005100362A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the present invention relates to a liquid external preparation suitable for alleviating symptoms of an inflammatory disease appearing in the eye or the nasal cavity or for treating the same.
  • Inflammatory diseases such as blepharitis, conjunctivitis, keratitis, rhinitis and the like appearing in the eye and nasal cavity are not only intolerable inflammatory symptoms but also cause excessive secretion of tears and runny nose. Unpleasant symptoms. It is known that pranoprofen, an acidic non-steroidal anti-inflammatory drug based on propionic acid, can effectively alleviate the symptoms of such inflammatory diseases. It is used as an active ingredient (anti-inflammatory agent) in inhalants.
  • Patent Document 1 Japanese Patent Application Laid-Open No. 5-186349
  • Patent Document 2 JP-A-60-184013
  • the present invention has been made to solve the technical problems recognized in the prior art described above, that is, the pain caused by pranoprofen in an affected area such as the eye or nasal cavity without impairing the anti-inflammatory effect exhibited by pranoprofen.
  • the purpose of the present invention is to provide a liquid external preparation that reduces both itchiness. Means for solving the problem
  • the gist of the present invention is a liquid external preparation containing pranoprofen and mucopolysaccharide.
  • an eye wash, an eye drop, and a nasal drop containing the liquid external preparation of the present invention is also provided.
  • a liquid external preparation which reduces both pain and itch due to pranoprofen which has appeared in an affected area such as the eye or nasal cavity, which is the intended purpose, is realized.
  • the pranoprofen-containing solution can be applied to the eyes and nasal cavity where inflammatory symptoms have appeared without a sense of resistance, and it can be expected to contribute to the improvement of therapeutic effects. It not only improves the feeling of use, but also has many synergistic effects in terms of medicinal properties.
  • a liquid external preparation containing pranoprofen and mucopolysaccharide is provided. Provided.
  • Units expressing the amounts of the constituents of the liquid external preparation of the present invention such as pranoprofen and mucopolysaccharide, unless otherwise specified, are referred to as% by weight (wt) unless otherwise specified. %).
  • pranoprofen contained in the liquid external preparation of the present invention is a well-known in the art as an excellent anti-inflammatory agent exhibiting a strong anti-inflammatory action against acute and chronic inflammation. Compound.
  • the amount of pranoprofen in the liquid external preparation of the present invention varies depending on the usage mode of the liquid external preparation of the present invention. That is, when the liquid external preparation of the present invention is used in the form of eyewash, from the viewpoint of obtaining a corresponding anti-inflammatory effect, it is usually about 0.001 to about 0.05% by weight, preferably about 0. 002—prepared in the range of about 0.01% by weight. From the same viewpoint, when the liquid external preparation of the present invention is used in the form of eye drops or nasal drops, it is usually used in an amount of about 0.01 to about 0.5% by weight, preferably about 0.02% by weight. It is prepared in the range of about 0.1% by weight.
  • the mucopolysaccharide used in the liquid external preparation of the present invention is generally a polysaccharide obtained from a viscous secretion of an animal.
  • the mucopolysaccharide has an effect of reducing irritation. It is used as a playing chemical.
  • mucopolysaccharides hyaluronic acid, chondroitin, chondroitin sulfate (salt), henolin and the like can be used in the present invention, but only one of these is not limited thereto. They can be used, or two or more can be used in combination.
  • sodium chondroitin sulfate can be suitably used in the liquid external preparation of the present invention.
  • the amount of the mucopolysaccharide in the liquid external preparation of the present invention also varies depending on the usage mode of the liquid external preparation of the present invention. That is, when the liquid external preparation of the present invention is used in the form of an eyewash, from the viewpoint of obtaining a corresponding corneal Z mucosal protective effect, usually about 0.01 to about 0.1% by weight, preferably It is prepared in the range of about 0.05 to about 0.1% by weight. From the same viewpoint, when the liquid external preparation of the present invention is used in the form of eye drops or nasal drops, it is usually about 0.1 to about 1.0% by weight, preferably about 0.25%. It is prepared in the range of about 0.5% by weight.
  • a pH adjuster can be further added to the liquid external preparation of the present invention for the purpose of further complementing the reduction of pain and itch caused by pranoprofen.
  • the pH adjuster that can be added to the liquid external preparation of the present invention include sodium hydroxide, potassium hydroxide, hydrochloric acid, citric acid (salt), boric acid (salt), phosphoric acid (salt), acetic acid (salt), and tartaric acid.
  • Salt sodium carbonate, sodium carbonate, and the like that can be used in the present invention.These are not limited to these. Any one of these can be used alone, or two or more kinds can be used in combination. Monkey
  • sodium carbonate and Z or citrate (salt) power can be suitably used in the liquid external preparation of the present invention.
  • liquid external preparation of the present invention Unless the action and effect of the liquid external preparation of the present invention are inhibited, other components generally used in preparations applied to the eye or the nasal cavity, for example, chelating agents, solubilizing agents, Preservatives, preservatives, buffers, thickeners, fresheners and the like can be optionally added.
  • chelating agents for example, chelating agents, solubilizing agents, Preservatives, preservatives, buffers, thickeners, fresheners and the like can be optionally added.
  • sodium edetate and citrate can be used in the present invention.
  • the present invention is not limited to these, and any one of these forces may be used, or two or more may be used. The above may be used in combination.
  • solubilizing agent polysorbates, propylene glycol, glycerin, and the like can be used in the present invention. Any one of these can be used. One of these can be used alone, or two or more can be used. Can also be used in combination.
  • preservatives include parabens, chlorhexidine dalconate, chlorobutanol, phenol ethyl alcohol, benzyl alcohol, sodium tetrahydroacetate, sorbic acid, potassium sorbate, cetylpyridinium chloride, and benzethonium chloride.
  • Benzolcombium chloride, chlorhexidine chloride, and the like can be used in the present invention.
  • the powers that can be used in the present invention are not limited to these. More than one type can be used together.
  • organic acids such as boric acid, citric acid, phosphoric acid, tartaric acid, acetic acid, and carbonic acid, amino acids, and salts thereof can be used in the present invention, but are not limited thereto.
  • One of these forces can be used, or two or more Can be used in combination.
  • methyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone, carboxyvinyl polymer, and the like can be used in the present invention. , Or only one type may be used, or two or more types may be used in combination.
  • Examples of the freshener include menthol, camphor, borneol, gelaol, cineol, linalool, eucalyptus oil, bergamot oil, fennel oil, rose oil, and the like, which can be used in the present invention. Only one of these can be used, or two or more of them can be used in combination.
  • a surfactant can be optionally added for the purpose of promoting the solubilization of these cooling agents.
  • surfactants such as polyoxyethylene hydrogenated castor oil, sorbitan monostearate, sorbitan monopalmitate, sorbitan monolaurate, polysorbates, sodium lauryl sulfate and sucrose fatty acid esters can be used in the present invention.
  • the present invention is not limited to these, and any one of these forces can be used alone, or two or more of them can be used in combination.
  • the pH of the liquid external preparation of the present invention is usually adjusted to about 6.5 to about 8.5, preferably about 6.5 to about 8.0.
  • the solvent for the liquid external preparation of the present invention may be any aqueous medium suitable as a solvent for the above-mentioned components. In view of application to the human body, it is preferably an impurity. Water having a low content, for example, purified water, deionized water, distilled water and the like can be suitably used.
  • the liquid external preparation of the present invention can be in the form of eyewash, eye drops or nasal drops.
  • a cup containing a few ml of the eye wash is applied to the periphery of the eye to remove dust or the like adhering to the eye. The garbage is washed away and the inflammation of the eyes is alleviated.
  • the liquid external preparation of the present invention when used in the form of eye drops or nasal drops, it can be applied to the eye or nasal cavity by an ordinary eye drop or nasal drop method.
  • Example 1-2 Each of the liquid external preparations of Example 1-2 and Comparative Examples 1-3 was used as eye drops, and the respective irritative and antipruritic items were evaluated according to the following test methods.
  • the irritancy that appeared when each liquid external preparation was instilled into the left and right eyes of six panelists was evaluated. Specifically, among the "power that has no irritation”, “very slight irritation”, “a little irritation” and “a considerable irritation”, apply each liquid topical agent The panelists selected the appropriate evaluation (expression) as the stimulus that appeared immediately after. The number of people evaluated for each criterion item is directly expressed as a score. It was.
  • Example 1 With the liquid topical preparations of 1-2, it was clear that the irritation was extremely low and the itching caused by pranoprofen was almost completely eliminated.
  • liquid topical preparation of the present invention sufficiently elicits the anti-inflammatory effect exhibited by pranoprofen, while both the pain and itch appearing at the site of application such as the eye and the nasal cavity due to pranoprofen
  • the feeling of use is very good because it can be reduced, and it is also extremely useful as a means to alleviate the symptoms of inflammation.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Otolaryngology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

[PROBLEMES] Fournir une préparation externe liquide capable de soulager à la fois la douleur et la démangeaison des parties affectées, comme la partie oculaire et la cavité nasale, à cause du pranoprofène. [MOYENS POUR RESOUDRE LES PROBLEMES] Il est prévu une préparation externe liquide comprenant du pranoprofène et un mucopolysaccharide.
PCT/JP2004/013896 2004-03-31 2004-09-24 Preparation externe liquide contenant du pranoprofene Ceased WO2005100362A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2004108401A JP2005289899A (ja) 2004-03-31 2004-03-31 プラノプロフェンを含有する液状外用剤
JP2004-108401 2004-03-31

Publications (1)

Publication Number Publication Date
WO2005100362A1 true WO2005100362A1 (fr) 2005-10-27

Family

ID=35149938

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2004/013896 Ceased WO2005100362A1 (fr) 2004-03-31 2004-09-24 Preparation externe liquide contenant du pranoprofene

Country Status (2)

Country Link
JP (1) JP2005289899A (fr)
WO (1) WO2005100362A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4831944B2 (ja) * 2004-04-28 2011-12-07 ロート製薬株式会社 プラノプロフェン含有組成物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60184013A (ja) * 1984-03-01 1985-09-19 Yoshitomi Pharmaceut Ind Ltd 点眼剤
JPH05186349A (ja) * 1991-12-30 1993-07-27 Teika Seiyaku Kk プラノプロフェン点眼剤組成物
JPH0952826A (ja) * 1995-08-10 1997-02-25 Showa Yakuhin Kako Kk 消炎点眼剤
JP2003183157A (ja) * 2001-12-19 2003-07-03 Lion Corp 眼科用組成物

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0717863A (ja) * 1993-06-30 1995-01-20 Kaken Pharmaceut Co Ltd プラノプロフェン点眼液
JP2001253822A (ja) * 1999-10-22 2001-09-18 Lion Corp 角膜細胞回復剤組成物
JP5147156B2 (ja) * 2003-08-08 2013-02-20 ロート製薬株式会社 角膜障害抑制剤
JP5078215B2 (ja) * 2003-08-27 2012-11-21 ロート製薬株式会社 プラノプロフェン含有組成物
JP4789479B2 (ja) * 2004-02-23 2011-10-12 ロート製薬株式会社 プラノプロフェン含有水性組成物
JP2005239682A (ja) * 2004-02-27 2005-09-08 Taisho Pharmaceut Co Ltd 眼科用剤
JP2005247799A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 点眼剤
JP2005247804A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 点眼剤
JP2005247798A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 点眼剤
JP2005247797A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 点眼剤
JP2005247803A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 点眼剤及びその容器
JP2005247795A (ja) * 2004-03-08 2005-09-15 Zeria Pharmaceut Co Ltd 安定な点眼剤

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60184013A (ja) * 1984-03-01 1985-09-19 Yoshitomi Pharmaceut Ind Ltd 点眼剤
JPH05186349A (ja) * 1991-12-30 1993-07-27 Teika Seiyaku Kk プラノプロフェン点眼剤組成物
JPH0952826A (ja) * 1995-08-10 1997-02-25 Showa Yakuhin Kako Kk 消炎点眼剤
JP2003183157A (ja) * 2001-12-19 2003-07-03 Lion Corp 眼科用組成物

Also Published As

Publication number Publication date
JP2005289899A (ja) 2005-10-20

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