WO2012108489A1 - Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles - Google Patents

Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles Download PDF

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Publication number
WO2012108489A1
WO2012108489A1 PCT/JP2012/052932 JP2012052932W WO2012108489A1 WO 2012108489 A1 WO2012108489 A1 WO 2012108489A1 JP 2012052932 W JP2012052932 W JP 2012052932W WO 2012108489 A1 WO2012108489 A1 WO 2012108489A1
Authority
WO
WIPO (PCT)
Prior art keywords
aqueous composition
less
salt
polyhydric alcohol
dihydroxytetrahydrofuran
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/JP2012/052932
Other languages
English (en)
Japanese (ja)
Inventor
孝司 稲垣
吉偉 堀部
雄一郎 中田
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.)
Santen Pharmaceutical Co Ltd
Original Assignee
Santen 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 Santen Pharmaceutical Co Ltd filed Critical Santen Pharmaceutical Co Ltd
Publication of WO2012108489A1 publication Critical patent/WO2012108489A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • 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
    • 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
    • A61K9/0051—Ocular inserts or implants
    • 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
    • A61P27/06—Antiglaucoma agents or miotics

Definitions

  • the polyhydric alcohol blended in the aqueous composition of the present invention is not particularly limited as long as it is a polyhydric alcohol that has two or more alcoholic hydroxyl groups in its molecule and can be used as a pharmaceutical additive.
  • Specific examples include glycerin, propylene glycol, mannitol, polyethylene glycol, trehalose, sucrose, sorbitol, xylitol and the like, preferably glycerin, propylene glycol and mannitol, and particularly preferably glycerin.
  • two or more of these polyhydric alcohols can be used in combination.
  • an isotonic agent that can be used as a pharmaceutical additive within the above osmotic pressure ratio can be appropriately blended.
  • tonicity agents include ionic and nonionic tonicity agents.
  • examples of the ionic tonicity agent include sodium chloride, potassium chloride, calcium chloride, and magnesium chloride
  • examples of the nonionic tonicity agent include glycerin, propylene glycol, mannitol, and sorbitol.
  • the polyhydric alcohol blended in the aqueous composition of the present invention may function as a nonionic tonicity agent, and the polyhydric alcohol is used from the viewpoint of the stability of the hydrophilic drug and the migration of the hydrophilic drug. Is preferred.
  • Example 2 Intraocular pressure lowering effect test>
  • the relationship between the improvement of aqueous humor transfer property of the hydrophilic drug and the actual drug efficacy, that is, the intraocular pressure lowering effect was examined.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne une composition aqueuse contenant un médicament hydrophile, la composition aqueuse contenant le médicament hydrophile et un halogénure de benzalkonium et ayant un rapport de pression osmotique inférieur ou égal à 0,5 en vue d'améliorer la pénétrabilité du médicament au site d'action du médicament, d'obtenir un effet souhaité à une faible dose et d'améliorer la sécurité lors de l'utilisation du médicament. La composition aqueuse contient de préférence un alcool polyhydrique. En outre, l'halogénure de benzalkonium est de préférence un chlorure de benzalkonium.
PCT/JP2012/052932 2011-02-10 2012-02-09 Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles Ceased WO2012108489A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2011027431 2011-02-10
JP2011-027431 2011-11-28

Publications (1)

Publication Number Publication Date
WO2012108489A1 true WO2012108489A1 (fr) 2012-08-16

Family

ID=46638701

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2012/052932 Ceased WO2012108489A1 (fr) 2011-02-10 2012-02-09 Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles

Country Status (3)

Country Link
JP (1) JP2012180346A (fr)
TW (1) TW201309343A (fr)
WO (1) WO2012108489A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022075472A1 (fr) * 2020-10-09 2022-04-14 アイ・セラピーズ・エル・エル・シー Préparation liquide de brimonidine

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2919755T3 (pl) * 2012-11-19 2018-07-31 Bausch & Lomb Incorporated Wodna ciekła kompozycja zawierająca kwas 2-amino-3-(4-bromobenzoilo)fenylooctowy
CA2935055C (fr) 2014-01-10 2021-08-24 Santen Pharmaceutical Co., Ltd. Composition pharmaceutique contenant un compose acide pyridylamino-acetique

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02503201A (ja) * 1988-02-08 1990-10-04 インサイト・ビジョン・インコーポレーテッド 眼用懸濁液
JPH10503470A (ja) * 1994-03-31 1998-03-31 レイラス オイ 減少した粘度を有する眼科治療用組成物
JPH11130675A (ja) * 1997-08-29 1999-05-18 Santen Pharmaceut Co Ltd クロマン誘導体含有点眼液
JP2005519978A (ja) * 2002-03-28 2005-07-07 スキャンポ・アーゲー 高眼圧症および緑内障の処置方法
JP2005206598A (ja) * 2003-12-26 2005-08-04 Rohto Pharmaceut Co Ltd 粘度低下が防止された組成物
JP2005298448A (ja) * 2004-04-15 2005-10-27 Rohto Pharmaceut Co Ltd アズレン含有水性液剤
JP2010524933A (ja) * 2007-04-16 2010-07-22 参天製薬株式会社 アデノシン誘導体を有効成分として含有する緑内障治療剤

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02503201A (ja) * 1988-02-08 1990-10-04 インサイト・ビジョン・インコーポレーテッド 眼用懸濁液
JPH10503470A (ja) * 1994-03-31 1998-03-31 レイラス オイ 減少した粘度を有する眼科治療用組成物
JPH11130675A (ja) * 1997-08-29 1999-05-18 Santen Pharmaceut Co Ltd クロマン誘導体含有点眼液
JP2005519978A (ja) * 2002-03-28 2005-07-07 スキャンポ・アーゲー 高眼圧症および緑内障の処置方法
JP2005206598A (ja) * 2003-12-26 2005-08-04 Rohto Pharmaceut Co Ltd 粘度低下が防止された組成物
JP2005298448A (ja) * 2004-04-15 2005-10-27 Rohto Pharmaceut Co Ltd アズレン含有水性液剤
JP2010524933A (ja) * 2007-04-16 2010-07-22 参天製薬株式会社 アデノシン誘導体を有効成分として含有する緑内障治療剤

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022075472A1 (fr) * 2020-10-09 2022-04-14 アイ・セラピーズ・エル・エル・シー Préparation liquide de brimonidine
JP2022063252A (ja) * 2020-10-09 2022-04-21 千寿製薬株式会社 ブリモニジンの液体製剤

Also Published As

Publication number Publication date
TW201309343A (zh) 2013-03-01
JP2012180346A (ja) 2012-09-20

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