KR970705974A - 경피 약물 전달을 위한 매트릭스(matrix for transdermal drug delivery) - Google Patents

경피 약물 전달을 위한 매트릭스(matrix for transdermal drug delivery)

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KR970705974A
KR970705974A KR1019970701693A KR19970701693A KR970705974A KR 970705974 A KR970705974 A KR 970705974A KR 1019970701693 A KR1019970701693 A KR 1019970701693A KR 19970701693 A KR19970701693 A KR 19970701693A KR 970705974 A KR970705974 A KR 970705974A
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drug delivery
transdermal drug
copolymer
delivery device
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제임스 이 가베
다니엘 씨 듀안
쉐릴 엘 무어
제이미슨 씨 케이스터
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퀄리 테릴 켄트
미네소타 마이닝 앤드 매뉴팩츄어링 캄파니
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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
    • 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
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • 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
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A61K9/7061—Polyacrylates
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F290/00—Macromolecular compounds obtained by polymerising monomers on to polymers modified by introduction of aliphatic unsaturated end or side groups
    • C08F290/02—Macromolecular compounds obtained by polymerising monomers on to polymers modified by introduction of aliphatic unsaturated end or side groups on to polymers modified by introduction of unsaturated end groups
    • C08F290/04—Polymers provided for in subclasses C08C or C08F
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09J—ADHESIVES; NON-MECHANICAL ASPECTS OF ADHESIVE PROCESSES IN GENERAL; ADHESIVE PROCESSES NOT PROVIDED FOR ELSEWHERE; USE OF MATERIALS AS ADHESIVES
    • C09J155/00—Adhesives based on homopolymers or copolymers, obtained by polymerisation reactions only involving carbon-to-carbon unsaturated bonds, not provided for in groups C09J123/00 - C09J153/00
    • C09J155/005—Homopolymers or copolymers obtained by polymerisation of macromolecular compounds terminated by a carbon-to-carbon double bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 거대단량체-함유 아크릴레이트 또는 메타크릴레이트 공중합체, 연화제 및 약물을 포함하는 경피 약물 전달 장치에 관한 것이다. 또한 거대단량체-함유 아크릴레이트 또는 메타크릴레이트 공중합체 및 연화제를 포함하는 감압성 피부 접착제에 관한 것이다.

Description

경피 약물 전달을 위한 매트릭스(MATRIX FOR TRANSDERMAL DRUGDELIVERY)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. (1) 지지체; 및 (2) (a) (i) 알킬 그룹에 4 내지 10개의 탄소 원자를 함유하는 알킬 아크릴레이트 및 알킬 그룹에 4 내지 10개의 탄소 원자를 함유하는 알킬 메타크릴레이트로 구성된 그룹으로부터 선택된 하나 이상의 A단량체; (ii) 임의로, A 단량체와 공중합할 수 있는 하나 이상의 에틸렌적으로 불포화된 B 단량체; (iii) 상기 정의된 A 및 B 단량체와 공중합할 수 있고, 분자량이 500 내지 500,000인 거대단량체를 포함하는 공중합체; (b) 공중합체에 용해된 연화제; 및 (c) 연화제가 치료 효과가 없을 경우, 치료 효과량의 약물을 포함하고 지지체의 한쪽면에 접착된 매트릭스를 포함하는 경피 약물 전달 장치(여기서 공중합체내의 공단량체의 구조 및 양, 공중합체의 고유 점도, 약물 및 연화제의 양 및 구조는 매트릭스에 2ⅹ10-6㎠/dyne 내지 약4ⅹ10-3㎠/dyne의 컴플라이언스치(compliance value)를 제공하는 것이다).
  2. 제1항에 있어서, 상기 B단량체(들)가 카복실산, 카복실산 에스테르, 하이드록시, 설폰아미드, 우레아, 카바메이트, 카복스아미드, 아민, 옥시, 옥소 및 시아노로 이루어진 그룹으로부터 선택된 작용 그룹을 포함하는 경피 약물 전달 장치.
  3. 제1항에 있어서, 상기 B단량체(들)가 아크릴산, 메타크릴산, 말레산, 하이드록시알킬 그룹에 2 내지 4개의 탄소원자를 함유하는 하이드록시알킬 아크릴레이트, 하이들록시알킬 그룹에 2 내지 4개의 탄소 원자를 함유하는 하이드록시알킬 메타크릴레이트, 아크릴아미드, 메타크릴아미드, 알킬 그룹에 1 내지 8개의 탄소 원자를 함유하는 알킬 치환된 아크릴아미드, 디아세톤 아크릴아미드, 알킬 그룹에 1 또는 2개의 탄소 원자를 갖는 디알킬 아크릴아미드, N-비닐-N-메틸 아세트아미드, N-비닐 발레로락탐, N-비닐 카프롤락탐, N-비닐-2-피롤리돈, 글리시딜 메타크릴레이트, 알콕시 그룹에 1 내지 4개의 탄소 원자를 함유하는 알콕시에틸 아크릴레이트, 알콕시 그룹에 1 내지 4개의 탄소 원자를 함유하는 알콕시에틸 메타크릴레이트, 2-에톡시에톡시에틸 아크릴레이트, 푸르푸릴 메타크릴레이트, 푸르푸릴 아크릴레이트, 테트라하이드로 푸르푸릴 아크릴레이트, 테트라하이드로푸르푸릴 메타크릴레이트, 프로필렌 글리콜모노메타크릴레이트, 프로필렌 글리콜 모노아크릴레이트, 폴리에틸렌 글리콜 아크릴레이트, 폴리에틸렌 옥사이드 메틸 에테르 아크릴레이트, 디(저급)알킬아미노에틸 아크릴레이트, 디(저급)알킬아미노 에틸 메타크릴레이트, 디(저급)알킬아미노프로필 메티크릴아미드, 아크릴로니트릴, 메타크릴로니트릴 및 비닐 아세테이트로 이루어진 그룹으로부터 선택된 경피 약물전달 장치.
  4. 제1항에 있어서, 상기 A 단량체가 공중합체중 모든 단량체의 총중량을 기준으로 약 40 내지 약 95중량%의 양으로 존재하는 경피 약물 전달 장치.
  5. 제1항에 있어서, 상기 A 단량체가 공중합체중 모든 단량체의 총중량을 기준으로 약 50 내지 약 70중량%의 양으로 존재하는 경피 약물 전달 장치.
  6. 제1항에 있어서, 상기 A 단량체가 이소옥틸 아크릴레이트, 2-에틸헥실 아크릴레이트, 부틸 아크릴레이트 및 사이클로헥실 아크릴레이트로 이루어진 그룹으로부터 선택되는 경피 약물 전달 장치.
  7. 제1항에 있어서, 상기 B 단량체가 공중합체의 총중량을 기준으로 0 내지 60중량%의 양을 존재하는 경피 약물 전달 장치.
  8. 제1항에 있어서, 상기 B 단량체가 공중합체의 총중량을 기준으로 25중량% 내지 약 50중량%의 양으로존재하는 경피 약물 전달 장치.
  9. 제1항에 있어서, 상기 B 단량체가 하이드록시에틸 아크릴레이트, 하이드록시에틸 메타크릴레이트, 글리세릴 아크릴레이트, N,N-디메틸 마크릴아미드, 2-에톡시에톡시에틸 아크릴레이트, 2-에톡시에틸 아크릴레이트, 테드라하이드로푸르푸릴 아크릴레이트, 아크릴산, 아크릴아미드 및 비닐 아세테이트로 이루어진 그룹으로부터 선택되는 경피 약물 전달 장치.
  10. 제1항에 있어서, 상기 거대단량체가 5,000 내지 30,000의 분자량을 갖는 경피 약물 전달 장치.
  11. 제1항에 있어서, 상기 거대단량체가 공중합체중 모든 단량체의 총중량을 기준으로 약 15중량% 이하의 양으로 존재하는 경피 약물 전달 장치.
  12. 제1항에 있어서, 상기 거대단량체가 공중합체중 모든 단량체의 총중량을 기준으로 약 5중량% 이하의 양으로 존재하는 경피 약물 전달 장치.
  13. 제1항에 있어서, 상기 거대단량체가 하기 일반식의 화합물인 경피 약물 전달 장치:
    상기 식에서, X는 A 및 B 단량체와 공중합할 수 있는 에틸렌적으로 불포화된 그룹을 포함하는 잔기이고, R2는 수소 원자 또는 저급 알킬 그룹이고, R3는 저급 알킬 그룹 또는 자유-라디칼 개시제의 잔기이고, n은 20 내지 500의 정수이고, 각 R4는, -CN 및 -CO2R6(여기서, R5는 수소 원자 또는 저급 알킬그룹이고, R6는 저급 알킬 그룹이다)로 이루어진 그룹으로부터 독립적으로 선택된 1가 라디칼이다.
  14. 제1항에 있어서, 상기 거대단량체가 폴리메틸메타크릴레이트 거대단량체, 스티렌/아크릴로니트릴 거대 단량체 및 폴리스티렌 거대단량체로 이루어진 그룹으로부터 선택된 경피 약물 전달 장치.
  15. 제1항에 있어서, 연화제가 매트릭스의 총중량을 기준으로 20중량%보다 많고 얄 60중량%보다 적은 양으로 존재하는 경피 약물 전달 장치.
  16. 제1항에 있어서, 상기 연화제가 C8-C22지방산, C8-C22지방알콜, C8-C22지방산의 저급 알킬 에스테르, C8-C22지방산의 모노글리세라이드, C6-C8이산의 디(저급)알킬 에스테르, 테트라하이드로푸르푸릴 알콜, 폴리에틸렌 글리콜 에테르, 폴리에틸렌 글리콜, 프로필렌 글리콜, 에톡시에톡시 에탄올, 디에틸렌 글리콜 모노메틸 에테르, N,N-디메틸도데실아민-N-옥사이드, 2-(2-에톡시에톡시)에탄올 및 이들의 조합으로 이루어진 그룹으로부터 선택되는 경피 약물 전달 장치.
  17. 제1항에 있어서, 상기 연화제가 디메틸 설폭사이드, 글리세롤, 에탄올, 에틸 아세테이트, 아세토아세트산 에스테르, N-메틸 피롤리돈, 이소프로필 알콜, 폴리에틸렌, 옥사이드의 알킬아릴 에테르, 폴리에틸렌, 옥사이드 모노메틸 에테르 및 폴리에틸렌 옥사이드 디메틸 에테르로 이루어진 그룹으로부터 선택된 경피 약물 전달 장치.
  18. 제1항에 있어서, 상기 연화제가 니코틴, 니트로글리세린, 클로르페니르아민, 니코틴산 벤질 에스테르, 오르페나드린, 스코폴아민 및 발프로산으로 이루어진 그룹으로부터 선택되는 경피 약물 전달 장치.
  19. (1) (a) 알킬 그룹에 4 내지 10개의 탄소 원자를 함유하는 알킬 아크릴레이트 및 알킬 그룹에 4 내지 10개의 탄소 원자를 함유하는 알킬 메타크릴레이트로 구성된 그룹으로 부터 선택된 하나이상의 A단량체; (b) 임의로, A단량체와 공중합할 수 있는 하나 이상의 에틸렌적으로 불포화된 B단량체; (c) 상기 정의된 A 및 B 단량체와 공중합할 수 있고, 분자량이 500 내지 500,000인 거대단량체를 포함하는 공중합체; 및 (2) 공중합체에 용해된 연화제를 포함하는 감압성 피부 접착제(여기서 공중합체내의 공단량체의 구조 및 양, 공중합체의 고유 점도, 연화제의 양 및 구조는 감압성 피부 접착제에 2ⅹ10-6㎠/dyne 내지 약 4ⅹ10-3㎠/dyne의 컴플라이언스치를 제공하는 것이다).
  20. 제19항에 있어서, 상기 B단량체(들)가 카복실산, 카복실산 에스테르, 하이드록시, 설폰아미드, 우레아, 카바메이트, 카복스아미드, 아민, 옥시, 옥시 및 시아노로 이루어진 그룹으로부터 선택된 작용 그룹을 포함하는 감압성 피부 접착제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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US7097853B1 (en) 2006-08-29
US20060099242A1 (en) 2006-05-11
PT781122E (pt) 2000-11-30
CA2198390A1 (en) 1996-03-21
DE69517816T2 (de) 2000-12-28
ES2147858T3 (es) 2000-10-01
AU3639795A (en) 1996-03-29
NZ293849A (en) 1998-10-28
DK0781122T3 (da) 2000-10-30
WO1996008229A3 (en) 1996-07-25
JPH10508296A (ja) 1998-08-18
DE69517816D1 (de) 2000-08-10
AU702593B2 (en) 1999-02-25
JP4102901B2 (ja) 2008-06-18
WO1996008229A2 (en) 1996-03-21
EP0781122A2 (en) 1997-07-02
GR3033859T3 (en) 2000-10-31
EP0781122B1 (en) 2000-07-05
ATE194281T1 (de) 2000-07-15
CA2198390C (en) 2009-08-11
KR100382706B1 (ko) 2003-10-10

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