WO2006096955A1 - Vehicule pour administration topique de composes anti-inflammatoires - Google Patents

Vehicule pour administration topique de composes anti-inflammatoires Download PDF

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Publication number
WO2006096955A1
WO2006096955A1 PCT/CA2005/000393 CA2005000393W WO2006096955A1 WO 2006096955 A1 WO2006096955 A1 WO 2006096955A1 CA 2005000393 W CA2005000393 W CA 2005000393W WO 2006096955 A1 WO2006096955 A1 WO 2006096955A1
Authority
WO
WIPO (PCT)
Prior art keywords
set forth
composition
pharmaceutically active
vehicle
active component
Prior art date
Application number
PCT/CA2005/000393
Other languages
English (en)
Inventor
Joseph Schwarz
Michael Weisspapir
Original Assignee
Alpharx Inc.
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 Alpharx Inc. filed Critical Alpharx Inc.
Priority to EP05714631A priority Critical patent/EP1858556A1/fr
Priority to PCT/CA2005/000393 priority patent/WO2006096955A1/fr
Publication of WO2006096955A1 publication Critical patent/WO2006096955A1/fr

Links

Classifications

    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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

  • Drug loading is high and can easily reach 5-10% or greater, e.g., 5% Ibuprofen gel with isopropyl alcohol, 1% Indomethacin gel based on ethyl alcohol or even 10% Indomethacin ointment with dimethylsulfoxide .
  • Eutectic mixture use in topical applications is rather limited.
  • An example is EMLA cream, developed by Astra- Zeneca.
  • the liquid, formed by mixing two crystalline bases of local anesthetics, Lidocain and Prilocain due to eutectic formation serves as an oil phase in the cream for topical application.
  • the cream, containing 5% of the oil phase, provides excellent stability and anesthetic action.
  • the water phase was prepared by dissolving Diclofenac sodium and TweenTM-80 in hot 85°C purified water.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un véhicule pour l’administration topique d’un principe pharmaceutique actif tel des anti-inflammatoires comprenant un mélange eutectique liquide contenantun composant hydrophobe. Le mélange eutectique contient, par exemple, des composés choisis parmi le camphre, le menthol, le thymol, la résorcine, le phénol ou des dérivés substitués de phénol. L’invention concerne également un procédé d’amélioration de la solubilité dudit principe pharmaceutique actif.
PCT/CA2005/000393 2005-03-16 2005-03-16 Vehicule pour administration topique de composes anti-inflammatoires WO2006096955A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP05714631A EP1858556A1 (fr) 2005-03-16 2005-03-16 Vehicule pour administration topique de composes anti-inflammatoires
PCT/CA2005/000393 WO2006096955A1 (fr) 2005-03-16 2005-03-16 Vehicule pour administration topique de composes anti-inflammatoires

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CA2005/000393 WO2006096955A1 (fr) 2005-03-16 2005-03-16 Vehicule pour administration topique de composes anti-inflammatoires

Publications (1)

Publication Number Publication Date
WO2006096955A1 true WO2006096955A1 (fr) 2006-09-21

Family

ID=36991223

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA2005/000393 WO2006096955A1 (fr) 2005-03-16 2005-03-16 Vehicule pour administration topique de composes anti-inflammatoires

Country Status (2)

Country Link
EP (1) EP1858556A1 (fr)
WO (1) WO2006096955A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009071408A1 (fr) * 2007-12-06 2009-06-11 Unilever Plc Composition de soin personnel
WO2009071422A1 (fr) * 2007-12-06 2009-06-11 Unilever Plc Composition de soin personnel
WO2011063531A1 (fr) 2009-11-27 2011-06-03 Nuvo Research Inc. Formulations topiques d'ibuprofène
US8613961B1 (en) * 2013-01-09 2013-12-24 NU Technology, LLC Dermatological cream with natural ingredients base
JP2014001203A (ja) * 2012-05-23 2014-01-09 Q P Corp 脂肪乳剤および医薬品組成物中の非ステロイド性抗炎症薬の含有量を高める方法
WO2014145710A1 (fr) * 2013-03-15 2014-09-18 Dr. Reddy's Laboratories, Inc. Composition de diclofénac parentérale
US9023399B2 (en) 2012-11-16 2015-05-05 NU Technology, LLC Water-soluble anti-inflammatory cream with natural ingredients base
WO2015090262A1 (fr) * 2013-12-16 2015-06-25 Epinamics Gmbh Composition pharmaceutique dermique et/ou transdermique contenant un composé terpénoïde
US9084754B2 (en) 2009-12-23 2015-07-21 Nuvo Research Inc. Highly permeating terbinafine formulation
WO2016069952A1 (fr) * 2014-10-31 2016-05-06 Sreedhar Rao Rayudu Composition anti-acné et méthodes d'utilisation
WO2020188547A1 (fr) * 2019-03-21 2020-09-24 Universidade Nova De Lisboa Système eutectique profond thérapeutique à base de terpène, son procédé d'obtention et ses utilisations
EP4112042A1 (fr) * 2021-06-30 2023-01-04 GSK Consumer Healthcare SARL Nanoémulsion comprenant du diclofénac

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040063794A1 (en) * 2002-09-27 2004-04-01 Alpharx Inc. Vehicle for topical delivery of anti-inflammatory compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040063794A1 (en) * 2002-09-27 2004-04-01 Alpharx Inc. Vehicle for topical delivery of anti-inflammatory compounds

Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA018416B1 (ru) * 2007-12-06 2013-07-30 Унилевер Н.В. Композиция для ухода за волосами и/или волосистой частью головы
WO2009071422A1 (fr) * 2007-12-06 2009-06-11 Unilever Plc Composition de soin personnel
WO2009071408A1 (fr) * 2007-12-06 2009-06-11 Unilever Plc Composition de soin personnel
US8501743B2 (en) 2007-12-06 2013-08-06 Conopco, Inc. Personal care composition
US8298553B2 (en) 2007-12-06 2012-10-30 Conopco, Inc. Personal care composition
CN101868221B (zh) * 2007-12-06 2012-12-26 荷兰联合利华有限公司 个人护理组合物
EP2504034A4 (fr) * 2009-11-27 2014-03-19 Nuvo Res Inc Formulations topiques d'ibuprofène
WO2011063531A1 (fr) 2009-11-27 2011-06-03 Nuvo Research Inc. Formulations topiques d'ibuprofène
EP2504034A1 (fr) * 2009-11-27 2012-10-03 Nuvo Research Inc. Formulations topiques d'ibuprofène
US9084754B2 (en) 2009-12-23 2015-07-21 Nuvo Research Inc. Highly permeating terbinafine formulation
JP2014001203A (ja) * 2012-05-23 2014-01-09 Q P Corp 脂肪乳剤および医薬品組成物中の非ステロイド性抗炎症薬の含有量を高める方法
US9023399B2 (en) 2012-11-16 2015-05-05 NU Technology, LLC Water-soluble anti-inflammatory cream with natural ingredients base
US8613961B1 (en) * 2013-01-09 2013-12-24 NU Technology, LLC Dermatological cream with natural ingredients base
US10369101B2 (en) 2013-03-15 2019-08-06 Latitude Pharmaceuticals Inc. Parenteral diclofenac composition
WO2014145710A1 (fr) * 2013-03-15 2014-09-18 Dr. Reddy's Laboratories, Inc. Composition de diclofénac parentérale
WO2015090262A1 (fr) * 2013-12-16 2015-06-25 Epinamics Gmbh Composition pharmaceutique dermique et/ou transdermique contenant un composé terpénoïde
WO2016069952A1 (fr) * 2014-10-31 2016-05-06 Sreedhar Rao Rayudu Composition anti-acné et méthodes d'utilisation
WO2020188547A1 (fr) * 2019-03-21 2020-09-24 Universidade Nova De Lisboa Système eutectique profond thérapeutique à base de terpène, son procédé d'obtention et ses utilisations
EP4112042A1 (fr) * 2021-06-30 2023-01-04 GSK Consumer Healthcare SARL Nanoémulsion comprenant du diclofénac
WO2023275002A1 (fr) * 2021-06-30 2023-01-05 Gsk Consumer Healthcare Sarl Nanoémulsion comprenant du diclofénac

Also Published As

Publication number Publication date
EP1858556A1 (fr) 2007-11-28

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