WO2012108489A1 - Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles - Google Patents
Composition aqueuse présentant une meilleure pénétrabilité des médicaments hydrophiles Download PDFInfo
- 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
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, ocular 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.
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.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2011-027431 | 2011-02-10 | ||
JP2011027431 | 2011-02-10 |
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 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)
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101748057B1 (ko) * | 2012-11-19 | 2017-06-15 | 보오슈 앤드 롬 인코포레이팃드 | 2-아미노-3-(4-브로모벤조일)페닐아세트산을 함유하는 수성 액체 조성물 |
SG11201605366QA (en) | 2014-01-10 | 2016-08-30 | Santen Pharmaceutical Co Ltd | Pharmaceutical composition containing pyridylaminoacetic acidcompound |
Citations (7)
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 |
-
2012
- 2012-02-09 TW TW101104139A patent/TW201309343A/zh unknown
- 2012-02-09 WO PCT/JP2012/052932 patent/WO2012108489A1/fr active Application Filing
- 2012-02-09 JP JP2012025660A patent/JP2012180346A/ja active Pending
Patent Citations (7)
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 (1)
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 |
Also Published As
Publication number | Publication date |
---|---|
TW201309343A (zh) | 2013-03-01 |
JP2012180346A (ja) | 2012-09-20 |
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