EP1372730A1 - Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzung - Google Patents

Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzung

Info

Publication number
EP1372730A1
EP1372730A1 EP02724387A EP02724387A EP1372730A1 EP 1372730 A1 EP1372730 A1 EP 1372730A1 EP 02724387 A EP02724387 A EP 02724387A EP 02724387 A EP02724387 A EP 02724387A EP 1372730 A1 EP1372730 A1 EP 1372730A1
Authority
EP
European Patent Office
Prior art keywords
acid
dispersed system
amino acid
phase
dispersed
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP02724387A
Other languages
English (en)
French (fr)
Inventor
Nicolas Calvet
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Physica Sarl
Original Assignee
Physica Sarl
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 FR0104187A external-priority patent/FR2828101A1/fr
Application filed by Physica Sarl filed Critical Physica Sarl
Publication of EP1372730A1 publication Critical patent/EP1372730A1/de
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/34Gestagens

Definitions

  • the pulmonary administration has other particularities.
  • the constitution of the pulmonary alveoli is very specific and allows the active ingredient to pass directly into the blood, hence the interest of the method.
  • the pulmonary administration is therefore distinguished from the administrations at the level of the mucous membranes as previously mentioned, as well as the cutaneous or oral administrations.
  • the bioavailability of the active ingredients, when the drugs are administered by these routes, is often limited.
  • a second approach consisted in the administration, directly in a liquid form, of very poorly soluble compounds already solubilized, organized in emulsified systems preferentially of the oil in water type.
  • These systems were originally developed to provide parenteral nutrition (Intralipid ® systems of the type, Japanese Patent No. 55 476) have been extended to the oral route, for the solubilization of hydrophobic insoluble active compounds.
  • Such systems mainly concern active lipop iles molecules and have the drawback of being difficult to adapt to oral unit presentations.
  • Recently, more sophisticated systems, constituting a "pre-concentrate" of surfactants and co-solvent have been developed.
  • the invention relates to the use in a pharmaceutical composition
  • a pharmaceutical composition comprising at least one active principle, of at least one lipoamino acid constituted by the association between a fatty acid and an amino acid, the fatty acid comprising from 4 to 40 carbon atoms and the amino acid may be a natural, synthetic or modified amino acid, which may be in native or salified form; the lipoamino acid being either a promoter of intestinal absorption or a promoter of pulmonary absorption, depending on whether the composition is respectively in a galenic form suitable for oral administration or in a galenic form suitable for administration in the lungs.
  • aspartic acid glutamic acid, alanine, arginine, carnitine, choline, cysteine, glycine, histidine , Isoleucine, leucine, lysine, methionine, phenylalanine, proline, ornithine, taurine, threonine, tryptophan, tyrosine, serine or valine.
  • Examples 1 to 8 describe formulations of dispersed systems comprising one or more lipoamino acids (in bold) and their preparation process. These dispersed systems are more particularly of the water in oil type (Examples 2 to 7), that is to say with a hydrophilic dispersed phase and a lipophilic dispersing phase. While Example 8 describes an oil-in-water dispersed system, that is to say with a lipophilic dispersed phase and a hydrophilic dispersing phase.
  • a hydrophilic phase consisting of at least one hydrophilic compound and of the active ingredient (s), heated between 40 and 80 ° C.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP02724387A 2001-03-28 2002-03-28 Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzung Withdrawn EP1372730A1 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
FR0104187 2001-03-28
FR0104187A FR2828101A1 (fr) 2001-03-28 2001-03-28 Utilisation des lipoaminoacides dans une composition pharmaceutique comme promoteurs d'absorption et systeme disperse a usage pharmaceutique contenant de tels composes
FR0107051 2001-05-30
FR0107051A FR2828102B1 (fr) 2001-03-28 2001-05-30 Utilisation des lipoaminoacides dans une composition pharmaceutique comme promoteur et systeme disperse a usage pharmaceutique contenant de tels composes
PCT/FR2002/001101 WO2002076506A1 (fr) 2001-03-28 2002-03-28 Utilisation de lipoaminoacides comme promoteurs d'absorption dans une composition pharmaceutique

Publications (1)

Publication Number Publication Date
EP1372730A1 true EP1372730A1 (de) 2004-01-02

Family

ID=26212940

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02724387A Withdrawn EP1372730A1 (de) 2001-03-28 2002-03-28 Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzung

Country Status (5)

Country Link
US (1) US20040147578A1 (de)
EP (1) EP1372730A1 (de)
CA (1) CA2441824A1 (de)
FR (1) FR2828102B1 (de)
WO (1) WO2002076506A1 (de)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2834215B1 (fr) * 2001-12-27 2004-07-16 Physica Composes amphiphiles a usage pharmaceutique ou cosmetique
ATE445644T1 (de) * 2005-04-15 2009-10-15 Rappaport Family Inst For Res Anwendung von molekülen und verfahren zur behandlung von mit mcp-1/ccr2 assoziierten krankheiten
ITRM20080551A1 (it) * 2008-10-15 2010-04-16 Univ Catania Derivati anfifilici del poliossietilenglicole (peg), procedimento di preparazione e loro usi nella preparazione di sistemi farmaceutici.
FR2959936B1 (fr) * 2010-05-14 2012-08-03 Physica Pharma Composition nasales a visee systemique a base de cocoyl proline ou d 'au moins un de ses constituants
FR2971943B1 (fr) * 2011-02-24 2013-08-02 Physica Pharma Compositions pharmaceutiques a action locale administrables par application cutanee
FR2971941B1 (fr) 2011-02-24 2013-08-02 Physica Pharma Compositions pharmaceutiques administrables par voie cutanee et destinees au traitement local de la dermatite atopique canine
JP6030630B2 (ja) * 2011-04-14 2016-11-24 ノヴォ ノルディスク アー/エス 経口ペプチド送達のための脂肪酸アシル化アミノ酸
PT2782584T (pt) 2011-11-23 2021-09-02 Therapeuticsmd Inc Preparações e terapias de substituição para hormonoterapias naturais combinadas
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
CN104717972A (zh) * 2012-10-17 2015-06-17 诺和诺德A/S(股份有限公司) 用于口服肽递送的脂肪酸酰化氨基酸
JP6285447B2 (ja) * 2012-10-17 2018-02-28 ノヴォ ノルディスク アー/エス 経口ペプチド送達用の脂肪酸アシル化d−アミノ酸
EP2908845A1 (de) * 2012-10-17 2015-08-26 Novo Nordisk Health Care AG Fettsäureacylierte aminosäuren zur wachstumshormonverabreichung
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
WO2015162195A1 (en) * 2014-04-23 2015-10-29 Novo Nordisk A/S Fatty acid acylated amino acids for oral peptide delivery
JP2017516768A (ja) 2014-05-22 2017-06-22 セラピューティックスエムディー インコーポレーテッドTherapeuticsmd, Inc. 天然の併用ホルモン補充療法剤及び療法
US10098894B2 (en) 2014-07-29 2018-10-16 Therapeuticsmd, Inc. Transdermal cream
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations

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US4442090A (en) * 1980-11-09 1984-04-10 Kyoto Yakuhin Kogyo Kabushiki Kaisha Absorption-promoting compounds, compositions thereof with pharmaceuticals and/or bases for rectal administration and method of use
JPS5788126A (en) * 1980-11-19 1982-06-01 Kyoto Yakuhin Kogyo Kk Agent for promoting peroral and transvaginal absorption and preparation containing the same
EP0093551B1 (de) * 1982-04-30 1991-01-16 Ajinomoto Co., Inc. Pharmazeutische Zusammensetzung
JPS5980326A (ja) * 1982-10-29 1984-05-09 Kobayashi Kooc:Kk W/o/w型エマルジヨンの製造方法
US4837026A (en) * 1985-10-03 1989-06-06 Rajakhyaksha Vithal J Transdermal and systemic preparation and method
JP2911496B2 (ja) * 1989-09-11 1999-06-23 帝國製薬株式会社 生理活性ポリペプチド含有高吸収性経膣剤
JP3202777B2 (ja) * 1992-01-24 2001-08-27 リンテック株式会社 経皮吸収促進剤及びテープ製剤
JPH05310552A (ja) * 1992-05-13 1993-11-22 Kanebo Ltd 皮膚外用剤
WO1995025504A1 (en) * 1994-03-18 1995-09-28 Pharmavene, Inc. Emulsified drug delivery systems

Non-Patent Citations (1)

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Title
See references of WO02076506A1 *

Also Published As

Publication number Publication date
WO2002076506A1 (fr) 2002-10-03
CA2441824A1 (fr) 2002-10-03
FR2828102B1 (fr) 2004-07-09
FR2828102A1 (fr) 2003-02-07
US20040147578A1 (en) 2004-07-29

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