BRPI0506812A - composição base auto-microemulsificável, microemulsão e método de preparação da composição base auto-microemulsificável - Google Patents

composição base auto-microemulsificável, microemulsão e método de preparação da composição base auto-microemulsificável

Info

Publication number
BRPI0506812A
BRPI0506812A BRPI0506812-6A BRPI0506812A BRPI0506812A BR PI0506812 A BRPI0506812 A BR PI0506812A BR PI0506812 A BRPI0506812 A BR PI0506812A BR PI0506812 A BRPI0506812 A BR PI0506812A
Authority
BR
Brazil
Prior art keywords
base composition
microemulsion
self
propofol
composition
Prior art date
Application number
BRPI0506812-6A
Other languages
English (en)
Inventor
Steven B Harris
Nick J Huang
Original Assignee
Bioavailability 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 Bioavailability Inc filed Critical Bioavailability Inc
Publication of BRPI0506812A publication Critical patent/BRPI0506812A/pt
Publication of BRPI0506812B1 publication Critical patent/BRPI0506812B1/pt
Publication of BRPI0506812B8 publication Critical patent/BRPI0506812B8/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/113Multiple emulsions, e.g. oil-in-water-in-oil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

COMPOSIçãO BASE AUTO-MICROEMULSIFICáVEL, MICROEMULSãO E MéTODO DE PREPARAçãO DA COMPOSIçãO BASE AUTOMICROEMULSIFICáVEL. A invenção apresenta um método e uma composição para intensificar as propriedades de dissolução e de biodisponibilidade de propofol (2, 6-diisopropil fenol) para ser utilizado como um anestésico administrado intravenosamente me mamíferos. O método produz uma composição base de emulsão auto-microemulsificável, a qual é utilizada na produção de um preparado de microemulsão à base de água. Em uma composição base de dois (2) componentes preferida, a composição base consiste em um tensoativo. o qual contém polietileno gricol; e propofol líquido. A microemulsão é preparada ao misturar a composição base com um líquido carreador, o que resulta na formação de uma microemulsão que contém concentrações de propofol de até aproximadamente 4% em peso de propofol em relação ao volume de microemulsão. Em uma composição base de quatro (4) componentes, a composição base consiste em: um tensoativo, o qual contém polietileno glicol; propofol líquido; um solvente imiscível em água; e etanol. A microemulsão é preparada ao misturar a composição base com um líquido carreador, o que resulta na formação de uma microemulsão que contém concentrações de propofol de até aproximadamente 10% em peso propofol em relação ao volume da microemulsão.
BRPI0506812A 2004-02-13 2005-02-14 composição base anidra auto-microemulsificável, microemulsão e método de preparação da composição base automicroemulsificável BRPI0506812B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US54460404P 2004-02-13 2004-02-13
US60/544,604 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 (3)

Publication Number Publication Date
BRPI0506812A true BRPI0506812A (pt) 2007-06-05
BRPI0506812B1 BRPI0506812B1 (pt) 2020-12-08
BRPI0506812B8 BRPI0506812B8 (pt) 2021-05-25

Family

ID=34886055

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0506812A BRPI0506812B8 (pt) 2004-02-13 2005-02-14 composição base anidra auto-microemulsificável, microemulsão e método de preparação da composição base automicroemulsificável

Country Status (14)

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE112008002914A5 (de) * 2007-11-06 2010-09-30 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
US20180022698A1 (en) 2014-10-16 2018-01-25 The Board Of Trustees Of The Leland Stanford Junior University Novel methods, compounds, and compositions for anesthesia
HK1250055A1 (zh) * 2015-03-23 2018-11-23 哈佛大学校长及研究员协会 用於注射高浓度和/或高粘度活性剂溶液的组合物和方法
WO2017002117A1 (en) * 2015-07-01 2017-01-05 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Delivery systems for propofol
MX383940B (es) 2015-12-09 2025-03-14 Phosphagenics Ltd Formulación farmacéutica que contiene tocol fosfato.
RU2742650C2 (ru) * 2015-12-09 2021-02-09 Фосфейдженикс Лимитед Фармацевтический состав
IL267006B2 (en) 2016-12-21 2024-11-01 Phosphagenics Ltd Process for phosphorylation of a complex alcohol with p4o10 at high temperatures, and products thereof
US11478490B1 (en) 2021-03-30 2022-10-25 Epalex Corporation Fospropofol formulations
US11628178B2 (en) 2019-03-26 2023-04-18 Epalex Corporation Fospropofol methods and compositions
US11547714B2 (en) 2020-02-05 2023-01-10 Epalex Corporation Fospropofol salts, methods and compositions
US11439653B1 (en) 2021-03-30 2022-09-13 Epalex Corporation Fospropofol formulations
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
US12349706B2 (en) 2020-07-31 2025-07-08 Natural Extraction Systems, LLC Compositions and methods related to excipients and cannabinoid formulations
EP4271414A4 (en) 2020-12-31 2024-11-27 The Governing Council of the University of Toronto FULLY DILUABLE SELF-MICROEMULSIFYING DELIVERY SYSTEMS (SMEDDS) FOR POORLY WATER-SOLUBLE POLAR SOLUTES
WO2022182523A1 (en) * 2021-02-26 2022-09-01 Natural Extraction Systems, LLC Compositions related to bioactive agents that convert from anions to molecules

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE370726T1 (de) 1998-02-10 2007-09-15 Sicor Inc Propofolhaltiges arzneimittel enthaltend sulfite
WO1999049848A1 (en) * 1998-04-01 1999-10-07 Rtp Pharma Inc. Anticancer compositions
AU5574200A (en) * 1999-06-21 2001-01-09 Kuhnil Pharm. Co., Ltd. Anesthetic composition for intravenous injection comprising propofol
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
EP1292282A2 (en) * 2000-06-16 2003-03-19 RTP Pharma Inc. Improved injectable dispersions of propofol
US6623765B1 (en) * 2000-08-01 2003-09-23 University Of Florida, Research Foundation, Incorporated Microemulsion and micelle systems for solubilizing drugs
IN188917B (pt) 2000-12-07 2002-11-23 Bharat Surums & Vaccines Ltd
KR100441167B1 (ko) 2001-12-27 2004-07-21 씨제이 주식회사 마이크로에멀젼 예비 농축액 조성물
KR100482269B1 (ko) * 2002-10-08 2005-04-14 센츄론(주) 2,6-디이소프로필페놀을 활성성분으로 하는 수용액상의마취용 주사제 및 그 제조방법
US7326735B2 (en) 2003-04-30 2008-02-05 Parnell Laboratories (Aust) Pty Limited Formulations for anaesthetic use
KR101055736B1 (ko) * 2008-09-30 2011-08-11 엘지전자 주식회사 김치냉장고

Also Published As

Publication number Publication date
US8383687B2 (en) 2013-02-26
US20130131186A1 (en) 2013-05-23
JP5165249B2 (ja) 2013-03-21
IL177419A0 (en) 2006-12-10
EA010242B1 (ru) 2008-06-30
EP1713444A1 (en) 2006-10-25
IL177419A (en) 2017-01-31
CN100479812C (zh) 2009-04-22
CA2556185C (en) 2010-09-21
BRPI0506812B8 (pt) 2021-05-25
US20070141090A1 (en) 2007-06-21
ZA200606947B (en) 2008-01-08
WO2005079758A1 (en) 2005-09-01
CN1917858A (zh) 2007-02-21
KR20070005617A (ko) 2007-01-10
UA85578C2 (ru) 2009-02-10
AU2005215517B2 (en) 2009-10-08
CA2556185A1 (en) 2005-09-01
AU2005215517C1 (en) 2011-04-14
EP1713444A4 (en) 2012-06-20
AU2005215517A1 (en) 2005-09-01
JP2007522238A (ja) 2007-08-09
IL247782A0 (en) 2016-11-30
US8962696B2 (en) 2015-02-24
EA200601460A1 (ru) 2007-02-27
BRPI0506812B1 (pt) 2020-12-08
NZ549016A (en) 2012-03-30

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
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B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B12B Appeal against refusal [chapter 12.2 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

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