EP1372730A1 - Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzung - Google Patents
Verwendung von lipoaminosäuren als absorptionförderer in einer pharmazeutischen zusammensetzungInfo
- 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- Withdrawn
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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- 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
- A61K47/20—Organic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/34—Gestagens
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)
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)
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 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
-
2001
- 2001-05-30 FR FR0107051A patent/FR2828102B1/fr not_active Expired - Fee Related
-
2002
- 2002-03-28 EP EP02724387A patent/EP1372730A1/de not_active Withdrawn
- 2002-03-28 WO PCT/FR2002/001101 patent/WO2002076506A1/fr not_active Application Discontinuation
- 2002-03-28 CA CA002441824A patent/CA2441824A1/fr not_active Abandoned
- 2002-03-28 US US10/473,312 patent/US20040147578A1/en not_active Abandoned
Non-Patent Citations (1)
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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Legal Events
Date | Code | Title | Description |
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PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
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17P | Request for examination filed |
Effective date: 20031001 |
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AK | Designated contracting states |
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AX | Request for extension of the european patent |
Extension state: AL LT LV MK RO SI |
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STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
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18D | Application deemed to be withdrawn |
Effective date: 20091001 |