KR970700021A - 에스트라디올 투과 증강제(estradiol penetration intensifier for transdermal administration) - Google Patents

에스트라디올 투과 증강제(estradiol penetration intensifier for transdermal administration)

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KR970700021A
KR970700021A KR1019960703800A KR19960703800A KR970700021A KR 970700021 A KR970700021 A KR 970700021A KR 1019960703800 A KR1019960703800 A KR 1019960703800A KR 19960703800 A KR19960703800 A KR 19960703800A KR 970700021 A KR970700021 A KR 970700021A
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acid
reservoir
active material
patch according
pressure sensitive
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KR100374087B1 (ko
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라인홀트 메코니
플랭크 사이버트
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플랭크베커, 베르너 웨스링
엘티에스 로프만 써라피에-씨스테메 게엠베하
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    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7069—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Adhesives Or Adhesive Processes (AREA)
  • Materials For Medical Uses (AREA)

Abstract

본 발명은 압력에 민감한 접착제 및 적어도 하나의 투과 증강제를 사용하여 제조되고, 제거할 수 있는 보호층은 투과 증강제가 카르복실산에 기초한 물질로부터 선택되는 특징을 갖고, 뒷면층, 이들과 연결된 활성 물질 함유 저장기로부터 게스타겐과 결합되거나 또는 결합되지 않는 에스트라디올 또는 그의 방출을 위한 활성물질-함유 패취.

Description

에스트라디올 투과 증강제(ESTRADIOL PENETRATION INTENSIFIER FOR TRANSDERMAL ADMINISTRATION)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 투과 증강제가 글리콜산, 말산, 락트산, 타르타르산, 구연산, 만델산, 2-히드록시신남산, 3-히드록시신남산, 트랜스-4-메톡시 신남산, 2-히드록시옥타노산, 트로프산, 갈산, 쉬키므산, 벤질산, 벤젠-1,2,4-프리카르복실산, 디-메틸-3-옥소글루타레이트, 3-메틸-2-옥소-발레리안산, 4-메틸-2-옥소-발레리안산, 2-옥소글루타르산, 피루브산, 4-아미노부티르산, 6-아미노헥사노산, 11-아미노운데카노산, 아스파라긴산, 2-아미노벤조산, 3-아미노벤조산, 4-아미노벤조산, 4-아미노-2-살리실산, 3-페닐프로피온산, 2-페닐부티르산, 4-페닐부티르산, 숙신산, 글루타르산, 3,3-디메틸글루타르산, 아디프산, 피멜산, 아젤레인산, 세박산, 트랜스-2-도데칸디오산, 트리데칸디오산, 테트라데칸디오산, 펜타데칸디오산, 디글리콜산, 피페리딘-4-카르복실산, 피라진-2-카르복실산, 피라진-2, 3-디카르복실산, 피리딘-2-카르복실산 및 니코틴산, 피멜산 모노메틸 에스테르, 말론산 디아미드, 아이프산 디아미드, 숙신산 디아미드, 피라진-2-카르복시아미드로 구성되는 카르복실산에 기초한 물질들의 그룹으로부터 선택되고, 압력에 민감한 접착제, 적어도 하나의 투과 증강제 및 제거할 수 있는 보호층에 의해 보호되고, 뒷면층, 이들과 연결된 활성물질-함유 저장기로 구성되는 게스타겐과 결합되거나 또는 결합되지 않는 에스트라디올 또는 그의 제약학적으로 수용할 수 있는 유도체의 조절된 방출을 위한 활성 물질-함유 패취.
  2. 제1항에 있어서, 저장기가 0.01-20 중량%의 농도의 투과 증강제로 구성됨을 특징으로 하는 활성 물질 패취.
  3. 제1항 또는 제2항에 있어서, 압력에 민감한 접착제가 적어도 6중량%의 농도의 중합체로 구성됨을 특징으로 하는 활성 물질 패취.
  4. 제1항 내지 제3항중의 어느 한 항에 있어서, 압력에 민감한 접착제가 5-94 중량%의 농도의 점착성 수지로 구성됨을 특징으로 하는 활성 물질 패취.
  5. 제1항 내지 제4항중의 어느 한 항에 있어서, 저장기가 전체적으로 2-15 중량%의 농도의 활성 물질로 구성됨을 특징으로 하는 활성 물질 패취.
  6. 제5항에 있어서, 결합된 투여의 경우에 에스트라디올 또는 그의 약학적 수용할수 있는 유도체 대 게스타겐의 몰비가 1 : 1 내지 1 : 10 의 1 양임을 특징으로 하는 활성 물질 패취.
  7. 제1항 내지 제6항중의 어느 한 항에 있어서, 저장기가 산화방지제와 더불어 염료, 충진제, 노화 방지제 및 가소제로 구성되는 그룹의 비 활성성분의 5 중량% 이하로 구성됨을 특징으로 하는 활성 물질 패취.
  8. 제1항 내지 제7항중의 어느 한 항에 있어서, 저장기가 여러층으로 형성됨을 특징으로 하는 활성 물질 패취.
  9. 제1항 내지 제8항중의 어느 한 항에 있어서, 저장기의 두께가 0.02-1.0mm의 범위임을 특징으로 하는 활성 물질 패취.
  10. 제1항 내지 제9항중의 어느 한 항에 있어서, 저장기가 피부에 대해 불충분한 자체 점착성을 갖는 경우에 추가의 압력에 민감한 접착제충 또는 압력에 민감한 접착제 모서리와 더불어 제공됨을 특징으로 하는 활성 물질 패취.
  11. 저장기가 용액, 분삭액 또는 용해물로부터 형성됨을 특징으로 하는 제1항 내지 제10항중의 어느 한 항에 따른 활성물질-함유 패취의 제조 방법.
  12. 인체 및 가축의 약에 치료목적을 위한 약제의 제조를 위한 제1항 내지 제11항중의 어느 한 항에 따른 활성 물질 패취의 사용 방법.
KR1019960703800A 1994-01-13 1995-01-05 에스트라디올투과증강제 KR100374087B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE4400770A DE4400770C1 (de) 1994-01-13 1994-01-13 Wirkstoffhaltiges Pflaster zur Abgabe von Estradiol mit mindestens einem Penetrationsverstärker, Verfahren zu seiner Herstellung und seine Verwendung
DEP4400770.1 1994-01-13

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KR970700021A true KR970700021A (ko) 1997-01-08
KR100374087B1 KR100374087B1 (ko) 2003-04-23

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US (1) US6090404A (ko)
EP (1) EP0739199B1 (ko)
JP (1) JP3980633B2 (ko)
KR (1) KR100374087B1 (ko)
AT (1) ATE215363T1 (ko)
AU (1) AU707963B2 (ko)
CZ (1) CZ287330B6 (ko)
DE (2) DE4400770C1 (ko)
DK (1) DK0739199T3 (ko)
ES (1) ES2174922T3 (ko)
FI (1) FI118719B (ko)
HU (1) HU222499B1 (ko)
IL (1) IL112145A (ko)
MY (1) MY113680A (ko)
NO (1) NO962933L (ko)
NZ (1) NZ278593A (ko)
PL (1) PL184875B1 (ko)
PT (1) PT739199E (ko)
SI (1) SI0739199T1 (ko)
SK (1) SK280530B6 (ko)
WO (1) WO1995019162A1 (ko)
ZA (1) ZA95226B (ko)

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JP3980633B2 (ja) 2007-09-26
KR100374087B1 (ko) 2003-04-23
NZ278593A (en) 1997-12-19
PT739199E (pt) 2002-09-30
DE59510142D1 (de) 2002-05-08
SI0739199T1 (en) 2002-10-31
ES2174922T3 (es) 2002-11-16
EP0739199B1 (de) 2002-04-03
CZ205396A3 (en) 1996-10-16
ZA95226B (en) 1996-02-07
HUT74455A (en) 1996-12-30
CZ287330B6 (en) 2000-10-11
JPH09511229A (ja) 1997-11-11
FI962702A0 (fi) 1996-06-28
HU9601872D0 (en) 1996-09-30
DK0739199T3 (da) 2002-07-29
PL315527A1 (en) 1996-11-12
IL112145A0 (en) 1995-03-15
SK280530B6 (sk) 2000-03-13
FI118719B (fi) 2008-02-29
SK91596A3 (en) 1997-03-05
DE4400770C1 (de) 1995-02-02
US6090404A (en) 2000-07-18
IL112145A (en) 2000-10-31
HU222499B1 (hu) 2003-07-28
MY113680A (en) 2002-04-30
NO962933L (no) 1996-09-12
NO962933D0 (no) 1996-07-12
PL184875B1 (pl) 2003-01-31
ATE215363T1 (de) 2002-04-15
WO1995019162A1 (de) 1995-07-20
AU707963B2 (en) 1999-07-22
AU1455295A (en) 1995-08-01
EP0739199A1 (de) 1996-10-30

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