EA010407B1 - Фармацевтические препараты для проникновения через полунепроницаемые барьеры и для неинвазивного введения лекарственных средств in vivo - Google Patents

Фармацевтические препараты для проникновения через полунепроницаемые барьеры и для неинвазивного введения лекарственных средств in vivo Download PDF

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Publication number
EA010407B1
EA010407B1 EA200500632A EA200500632A EA010407B1 EA 010407 B1 EA010407 B1 EA 010407B1 EA 200500632 A EA200500632 A EA 200500632A EA 200500632 A EA200500632 A EA 200500632A EA 010407 B1 EA010407 B1 EA 010407B1
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EA
Eurasian Patent Office
Prior art keywords
aggregates
component
membrane
adaptogenicity
lipid
Prior art date
Application number
EA200500632A
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English (en)
Russian (ru)
Other versions
EA200500632A1 (ru
Inventor
Грегор Цевц
Ульрих Виерл
Original Assignee
Идеа Аг
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
Priority claimed from US10/357,618 external-priority patent/US20040105881A1/en
Application filed by Идеа Аг filed Critical Идеа Аг
Publication of EA200500632A1 publication Critical patent/EA200500632A1/ru
Publication of EA010407B1 publication Critical patent/EA010407B1/ru

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    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • 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
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers
    • A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Anesthesiology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Materials For Medical Uses (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
EA200500632A 2002-10-11 2003-10-09 Фармацевтические препараты для проникновения через полунепроницаемые барьеры и для неинвазивного введения лекарственных средств in vivo EA010407B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US41784702P 2002-10-11 2002-10-11
US10/357,618 US20040105881A1 (en) 2002-10-11 2003-02-04 Aggregates with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin
US10/357,617 US7473432B2 (en) 2002-10-11 2003-02-04 NSAID formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery
PCT/EP2003/011202 WO2004032900A1 (en) 2002-10-11 2003-10-09 Aggregate with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin

Publications (2)

Publication Number Publication Date
EA200500632A1 EA200500632A1 (ru) 2005-12-29
EA010407B1 true EA010407B1 (ru) 2008-08-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA200500632A EA010407B1 (ru) 2002-10-11 2003-10-09 Фармацевтические препараты для проникновения через полунепроницаемые барьеры и для неинвазивного введения лекарственных средств in vivo

Country Status (21)

Country Link
EP (5) EP1815847A3 (OSRAM)
JP (3) JP2006505619A (OSRAM)
KR (1) KR20050055723A (OSRAM)
CN (1) CN1703199B (OSRAM)
AT (1) ATE381316T1 (OSRAM)
AU (1) AU2003273977B2 (OSRAM)
BR (1) BR0315148A (OSRAM)
CA (1) CA2498938A1 (OSRAM)
DE (1) DE60318227T2 (OSRAM)
DK (1) DK1551370T3 (OSRAM)
EA (1) EA010407B1 (OSRAM)
ES (1) ES2298566T3 (OSRAM)
HR (1) HRPK20050421B3 (OSRAM)
IS (1) IS7776A (OSRAM)
MX (1) MXPA05003744A (OSRAM)
NO (1) NO20052281L (OSRAM)
NZ (1) NZ538571A (OSRAM)
PL (1) PL377202A1 (OSRAM)
PT (1) PT1551370E (OSRAM)
SI (1) SI1551370T1 (OSRAM)
WO (1) WO2004032900A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2524649C1 (ru) * 2013-07-24 2014-07-27 Станислав Анатольевич Кедик Способ получения микросфер для приготовления инъецируемой лекарственной формы диклофенака, композиция и лекарственная форма

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EP1031346B1 (en) 1999-01-27 2002-05-02 Idea Ag Noninvasive vaccination through the skin
PT1031347E (pt) 1999-01-27 2002-09-30 Idea Ag Transporte/imunizacao transnasal com veiculos muitissimo adaptaveis
MXPA02000053A (es) 1999-07-05 2003-07-21 Idea Ag Un metodo para mejorar el tratamiento a traves de barreras adaptables semipermeables.
DE10053397A1 (de) 2000-10-20 2002-05-02 Schering Ag Verwendung eines dopaminergen Wirkstoffes zur Behandlung von dopaminerg behandelbaren Erkrankungen
US20040105881A1 (en) 2002-10-11 2004-06-03 Gregor Cevc Aggregates with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin
EP1811961A2 (en) * 2004-11-12 2007-08-01 Idea Ag Extended surface aggregates in the treatment of skin conditions
EP2676680A1 (de) * 2007-09-13 2013-12-25 Basf Se Verwendung von Hydrophobin-Polipeptiden als Penetrationsverstärker
PL214538B1 (pl) * 2009-05-28 2013-08-30 P P F Hasco Lek Spolka Akcyjna Kompozycja liposomowa zawierajaca naproksen i sposób wytwarzania kompozycji liposomowej zawierajacej naproksen
CN105434354A (zh) * 2009-06-03 2016-03-30 斯昆申技术控股有限责任公司 用于治疗深部组织疼痛的制剂
US20120232034A1 (en) 2009-08-21 2012-09-13 Henk-Andre Kroon Vesicular formulations
GB2503845A (en) * 2011-03-21 2014-01-08 Gregor Cevc Optimised preparations of highly adaptable aggregates
GB2503844A (en) * 2011-03-21 2014-01-08 Gregor Cevc Drug-free compositions and methods for diminishing peripheral inflammation and pain
GB201205642D0 (en) 2012-03-29 2012-05-16 Sequessome Technology Holdings Ltd Vesicular formulations
CA2889664C (en) * 2012-10-26 2020-12-29 Oxford Nanopore Technologies Limited Droplet interfaces
HK1221412A1 (zh) * 2013-07-31 2017-06-02 Sequessome Technology Holdings Limited 囊泡
EP3760638A3 (en) * 2013-09-26 2021-05-26 National University of Singapore Compositions and methods utilizing lysophosphatidylcholine scaffolds
JP6547625B2 (ja) * 2013-10-25 2019-07-24 凸版印刷株式会社 膜小胞回収デバイス、膜小胞回収方法、及び膜小胞分析方法
ES2879383T3 (es) 2015-06-30 2021-11-22 Sequessome Tech Holdings Limited Fórmulas mixtas
US12364661B2 (en) 2015-11-20 2025-07-22 The Regents Of The University Of California Deformable nano-scale vehicles (DNVS) for trans-blood brain barrier, trans-mucosal, and transdermal drug delivery
JP7280624B2 (ja) * 2017-04-03 2023-05-24 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 経血液脳関門的、経粘膜的及び経皮的薬物送達のための変形可能なナノスケールビヒクル（ｄｎｖ）
GB2571696B (en) 2017-10-09 2020-05-27 Compass Pathways Ltd Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced
US12459965B2 (en) 2017-10-09 2025-11-04 Compass Pathfinder Limited Preparation of psilocybin, different polymorphic forms, intermediates, formulations and their use
KR102149190B1 (ko) 2018-04-09 2020-08-28 경상대학교산학협력단 액중 방전 마이크로젯 약물 전달장치
JP2022529781A (ja) 2019-04-17 2022-06-24 コンパス パスファインダー リミテッド サイロシビンによるうつ病及び他の様々な障害の治療
US12240813B2 (en) 2020-05-19 2025-03-04 Cybin Irl Limited Deuterated tryptamine derivatives and methods of use
KR102209397B1 (ko) 2020-07-21 2021-01-29 경상대학교산학협력단 액중 방전 마이크로젯 약물 전달장치

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EP0475160A1 (de) * 1990-08-24 1992-03-18 Gregor Prof. Dr. Cevc Präparat zur Wirkstoffapplikation in Kleinsttröpfchenform
DE4107153A1 (de) * 1991-03-06 1992-09-10 Gregor Cevc Praeparat zur wirkstoffapplikation in kleinsttroepfchenform
DE4447287C1 (de) * 1994-12-30 1996-11-07 Cevc Gregor Präparat zum Wirkstofftransport durch Barrieren
EP1031347A1 (en) * 1999-01-27 2000-08-30 Idea Ag Transnasal transport/immunisation with highly adaptable carriers

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US6165500A (en) * 1990-08-24 2000-12-26 Idea Ag Preparation for the application of agents in mini-droplets
US20020048596A1 (en) * 1994-12-30 2002-04-25 Gregor Cevc Preparation for the transport of an active substance across barriers
CN1320880C (zh) * 1998-12-23 2007-06-13 伊迪亚股份公司 改进的体内局部无创伤用制剂

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0475160A1 (de) * 1990-08-24 1992-03-18 Gregor Prof. Dr. Cevc Präparat zur Wirkstoffapplikation in Kleinsttröpfchenform
DE4107153A1 (de) * 1991-03-06 1992-09-10 Gregor Cevc Praeparat zur wirkstoffapplikation in kleinsttroepfchenform
DE4447287C1 (de) * 1994-12-30 1996-11-07 Cevc Gregor Präparat zum Wirkstofftransport durch Barrieren
EP1031347A1 (en) * 1999-01-27 2000-08-30 Idea Ag Transnasal transport/immunisation with highly adaptable carriers

Non-Patent Citations (2)

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Title
CEVC G. ET AL.: "ULTRAFLEXIBLE VESICLES, TRANSFERSOMES, HAVE AN EXTREMELY LOW PORE PENETRATION RESISTANCE AND TRANSPORT THERAPEUTIC AMOUNTS OF INSULIN ACROSS THE INTACT MAMMALIAN SKIN", BIOCHIMICA ET BIOPHYSICA ACTA. BIOMEMBRANES, AMSTERDAM, NL, vol. 1368, no. 2, 19 January 1998 (1998-01-19), pages 201-215, XP001119925, ISSN: 0005-2736, abstract, page 202, paragraph 2.4, page 203, paragraph 2.5, figures 2-5 *
CEVC G.: "Transfersomes, liposomes and other lipid suspensions on the skin: permeation enhancement, vesicle penetration, and transdermal drug delivery", CRITICAL REVIEWS IN THERAPEUTIC DRUG CARRIER SYSTEMS, XX, XX, vol. 13, no. 3/4, 1996, pages 257-388, XP002107366, ISSN: 0743-4863, the whole document *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2524649C1 (ru) * 2013-07-24 2014-07-27 Станислав Анатольевич Кедик Способ получения микросфер для приготовления инъецируемой лекарственной формы диклофенака, композиция и лекарственная форма

Also Published As

Publication number Publication date
ES2298566T3 (es) 2008-05-16
KR20050055723A (ko) 2005-06-13
EP1551370B1 (en) 2007-12-19
IS7776A (is) 2005-03-30
DE60318227D1 (de) 2008-01-31
EP1551370A1 (en) 2005-07-13
EA200500632A1 (ru) 2005-12-29
NO20052281D0 (no) 2005-05-10
HRP20050421A2 (en) 2005-12-31
EP1829527A2 (en) 2007-09-05
JP4555111B2 (ja) 2010-09-29
AU2003273977A1 (en) 2004-05-04
NO20052281L (no) 2005-07-07
PT1551370E (pt) 2008-02-07
CA2498938A1 (en) 2004-04-22
SI1551370T1 (sl) 2008-06-30
HRPK20050421B3 (en) 2007-06-30
DK1551370T3 (da) 2008-03-03
EP1829528A2 (en) 2007-09-05
PL377202A1 (pl) 2006-01-23
MXPA05003744A (es) 2005-09-20
EP1829527A3 (en) 2008-11-05
EP1829528A3 (en) 2008-11-05
CN1703199B (zh) 2010-04-28
EP1815846A3 (en) 2008-10-22
EP1815847A2 (en) 2007-08-08
EP1815846A2 (en) 2007-08-08
WO2004032900A1 (en) 2004-04-22
BR0315148A (pt) 2005-08-16
JP2005213261A (ja) 2005-08-11
NZ538571A (en) 2007-05-31
DE60318227T2 (de) 2008-12-04
AU2003273977B2 (en) 2007-07-12
JP2009108070A (ja) 2009-05-21
HK1079113A1 (en) 2006-03-31
JP2006505619A (ja) 2006-02-16
CN1703199A (zh) 2005-11-30
WO2004032900A8 (en) 2005-03-31
EP1815847A3 (en) 2008-11-05
ATE381316T1 (de) 2008-01-15

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