EA200601460A1 - Препарат микроэмульсии с высокой концентрацией пропофола для анестезирующих применений - Google Patents

Препарат микроэмульсии с высокой концентрацией пропофола для анестезирующих применений

Info

Publication number
EA200601460A1
EA200601460A1 EA200601460A EA200601460A EA200601460A1 EA 200601460 A1 EA200601460 A1 EA 200601460A1 EA 200601460 A EA200601460 A EA 200601460A EA 200601460 A EA200601460 A EA 200601460A EA 200601460 A1 EA200601460 A1 EA 200601460A1
Authority
EA
Eurasian Patent Office
Prior art keywords
microemulsion
propofol
base composition
prepared
prophopol
Prior art date
Application number
EA200601460A
Other languages
English (en)
Other versions
EA010242B1 (ru
Inventor
Стивен Б. Харрис
Ник Дж. Хуанг
Original Assignee
Биоавейлэбилити, Инк.
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 Биоавейлэбилити, Инк. filed Critical Биоавейлэбилити, Инк.
Publication of EA200601460A1 publication Critical patent/EA200601460A1/ru
Publication of EA010242B1 publication Critical patent/EA010242B1/ru

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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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/113—Multiple emulsions, e.g. oil-in-water-in-oil
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

В изобретении предложены способ и композиция для увеличения растворения и свойств биодоступности пропофола (2,6-диизопропилфенола) для применения в качестве внутривенно вводимого анестетика у млекопитающих. Согласно данному способу получают базовую композицию самомикроэмульгирующейся эмульсии, которую применяют для изготовления препарата микроэмульсии на основе воды. В предпочтительной двухкомпонентной (2) базовой композиции она состоит из поверхностно-активного агента, содержащего полиэтиленгликоль, и жидкого пропофола. Микроэмульсию приготавливают путем смешивания данной базовой композиции с жидкостью-носителем, что приводит к образованию микроэмульсии, содержащей концентрации пропофола вплоть до примерно 4 мас.% пропофола к объему микроэмульсии. В четырехкомпонентной (4) базовой композиции она состоит из поверхностно-активного агента, содержащего полиэтиленгликоль; жидкого пропофола; несмешивающегося с водой растворителя и этанола. Микроэмульсию приготавливают путем смешивания данной базовой композиции с жидкостью-носителем, что приводит к образованию микроэмульсии, содержащей концентрации пропофола вплоть до примерно 10 мас.% пропофола к объему микроэмульсии.
EA200601460A 2004-02-13 2005-02-14 Препарат микроэмульсии с высокой концентрацией пропофола для анестезирующих применений EA010242B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54460404P 2004-02-13 2004-02-13
PCT/US2005/004533 WO2005079758A1 (en) 2004-02-13 2005-02-14 A microemulsion preparation of high concentration propofol for anesthetic uses

Publications (2)

Publication Number Publication Date
EA200601460A1 true EA200601460A1 (ru) 2007-02-27
EA010242B1 EA010242B1 (ru) 2008-06-30

Family

ID=34886055

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200601460A EA010242B1 (ru) 2004-02-13 2005-02-14 Препарат микроэмульсии с высокой концентрацией пропофола для анестезирующих применений

Country Status (14)

Country Link
US (2) US8383687B2 (ru)
EP (1) EP1713444A4 (ru)
JP (1) JP5165249B2 (ru)
KR (1) KR20070005617A (ru)
CN (1) CN100479812C (ru)
AU (1) AU2005215517C1 (ru)
BR (1) BRPI0506812B8 (ru)
CA (1) CA2556185C (ru)
EA (1) EA010242B1 (ru)
IL (2) IL177419A (ru)
NZ (1) NZ549016A (ru)
UA (1) UA85578C2 (ru)
WO (1) WO2005079758A1 (ru)
ZA (1) ZA200606947B (ru)

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BRPI0604377A (pt) * 2006-10-27 2008-06-24 Cristalia Prod Quimicos Farm microemulsão óleo/água de propofol estável e pronta-para-uso
WO2008101344A1 (en) * 2007-02-22 2008-08-28 Peter Tomlinson Soluble bioactive lipophilic compounds compositions
AR060926A1 (es) * 2007-05-14 2008-07-23 Ciriaco Quiroga Solucion anestesica transparente de propofol, con baja irritacion venosa.
US8722736B2 (en) 2007-05-22 2014-05-13 Baxter International Inc. Multi-dose concentrate esmolol with benzyl alcohol
US8426467B2 (en) * 2007-05-22 2013-04-23 Baxter International Inc. Colored esmolol concentrate
CN101411685B (zh) * 2007-10-19 2011-04-20 上海医药工业研究院 一种静脉麻醉药2,6-二异丙基苯酚微乳组合物及其制备方法
WO2009059989A1 (de) * 2007-11-06 2009-05-14 B. Braun Melsungen Ag Einen hydrophoben wirkstoff enthaltende wässrige emulsionen
CN101756900B (zh) * 2010-02-25 2012-05-30 谢恬 一种榄香烯微乳
JP4834775B2 (ja) * 2010-03-04 2011-12-14 株式会社 資生堂 日焼け止め用組成物
WO2016038734A1 (ja) 2014-09-12 2016-03-17 テルモ株式会社 レミフェンタニル注射液剤
JP2017531011A (ja) 2014-10-16 2017-10-19 ザ ボード オブ トラスティーズ オブ ザ リーランド スタンフォード ジュニア ユニバーシティ 麻酔のための新規の方法、化合物および組成物
WO2016154288A1 (en) * 2015-03-23 2016-09-29 President And Fellows Of Harvard Methods and compositions for injecting high concentration and/or high viscosity active agent solutions
RU2709812C2 (ru) 2015-07-01 2019-12-23 Йиссум Ресерч Девелопмент Компани Оф Де Хебрю Юниверсити Оф Джерусалем Лтд Системы доставки пропофола
KR20190032265A (ko) * 2015-12-09 2019-03-27 포스파제닉스 리미티드 약제학적 제형
CN108601732A (zh) * 2015-12-09 2018-09-28 磷肌酸有限公司 药物制剂
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US11547714B2 (en) 2020-02-05 2023-01-10 Epalex Corporation Fospropofol salts, methods and compositions
US11478490B1 (en) 2021-03-30 2022-10-25 Epalex Corporation Fospropofol formulations
US11439653B1 (en) 2021-03-30 2022-09-13 Epalex Corporation Fospropofol formulations
US11628178B2 (en) 2019-03-26 2023-04-18 Epalex Corporation Fospropofol methods and compositions
WO2021158575A1 (en) * 2020-02-03 2021-08-12 Natural Extraction Systems, LLC Compositions related to bioactive agents that convert from anions to molecules
US11767281B2 (en) 2020-02-06 2023-09-26 Nandkumar Kashinath Chodankar Manufacturing and purification technology for high purity Propofol
WO2022182523A1 (en) * 2021-02-26 2022-09-01 Natural Extraction Systems, LLC Compositions related to bioactive agents that convert from anions to molecules

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GB9405593D0 (en) 1994-03-22 1994-05-11 Zeneca Ltd Pharmaceutical compositions
GB9514878D0 (en) 1995-07-20 1995-09-20 Danbiosyst Uk Vitamin E as a solubilizer for drugs contained in lipid vehicles
SE9503143D0 (sv) 1995-09-12 1995-09-12 Astra Ab New preparation
US5993858A (en) * 1996-06-14 1999-11-30 Port Systems L.L.C. Method and formulation for increasing the bioavailability of poorly water-soluble drugs
CO4810371A1 (es) 1998-02-10 1999-06-30 Gensia Sicor Inc Composicion de propofol que contiene sulfito
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KR20010055736A (ko) 1999-12-13 2001-07-04 이규현 프로포폴의 마이크로에멀젼 주사제 조성물
GB2359747B (en) * 2000-02-29 2002-04-24 Maelor Pharmaceuticals Ltd Anaesthetic formulations
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Also Published As

Publication number Publication date
CN100479812C (zh) 2009-04-22
ZA200606947B (en) 2008-01-08
AU2005215517A1 (en) 2005-09-01
BRPI0506812A (pt) 2007-06-05
US8962696B2 (en) 2015-02-24
IL177419A (en) 2017-01-31
BRPI0506812B1 (pt) 2020-12-08
CA2556185C (en) 2010-09-21
KR20070005617A (ko) 2007-01-10
US8383687B2 (en) 2013-02-26
CN1917858A (zh) 2007-02-21
IL247782A0 (en) 2016-11-30
JP2007522238A (ja) 2007-08-09
CA2556185A1 (en) 2005-09-01
EP1713444A4 (en) 2012-06-20
AU2005215517B2 (en) 2009-10-08
EP1713444A1 (en) 2006-10-25
BRPI0506812B8 (pt) 2021-05-25
EA010242B1 (ru) 2008-06-30
UA85578C2 (ru) 2009-02-10
WO2005079758A1 (en) 2005-09-01
US20130131186A1 (en) 2013-05-23
US20070141090A1 (en) 2007-06-21
IL177419A0 (en) 2006-12-10
NZ549016A (en) 2012-03-30
JP5165249B2 (ja) 2013-03-21
AU2005215517C1 (en) 2011-04-14

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM