KR960034348A - 의약 유동성 향상제에 내성을 가지는 압력에 민감한 점착성 조성물 - Google Patents

의약 유동성 향상제에 내성을 가지는 압력에 민감한 점착성 조성물 Download PDF

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KR960034348A
KR960034348A KR1019960007140A KR19960007140A KR960034348A KR 960034348 A KR960034348 A KR 960034348A KR 1019960007140 A KR1019960007140 A KR 1019960007140A KR 19960007140 A KR19960007140 A KR 19960007140A KR 960034348 A KR960034348 A KR 960034348A
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monomer
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penetration enhancer
graft
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제이. 써리얼트 도날드
로저즈 케네스 더블유
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챨스 알. 팍스
어드히시브즈 리서치, 인코포레이티드
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    • 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
    • C09J133/00—Adhesives based on homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides, or nitriles thereof; Adhesives based on derivatives of such polymers
    • C09J133/04—Homopolymers or copolymers of esters
    • C09J133/06—Homopolymers or copolymers of esters of esters containing only carbon, hydrogen and oxygen, the oxygen atom being present only as part of the carboxyl radical
    • 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
    • C08F290/044—Polymers of aromatic monomers as defined in group C08F12/00

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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
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  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Medicinal Preparation (AREA)
  • Adhesives Or Adhesive Processes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Adhesive Tapes (AREA)

Abstract

본 발명은, 경피를 통하여 투여하는 약학적으로 활성이 있는 약제의 피부투과성을 증가시키는 경피 침투 향상제와; 거대분자로 보강된 베이스 중합체(base polymer)의 혼합물로 이루어진, 의약 유동성 향상제에 내성을 가지는 압력에 민감한 점착성 조성물에 관한 것이다. 상기 베이스 중합체는 그라프트(grafted) 중합체성분을 갖는 주쇄(backbone) 중합체를 형성하기 위한 공중합된 단량체 A 와 B를 포함하는 상분리된 그라프트 공중합체 조성물로 이루어진다. 여기서 단량체(monomer) A는 1~14의 탄소원자를 갖는, 바람직하게는 4~12의 탄소원자수를 갖는, 비-3차알콜의 (non-tertiary alcohol) 단량체 아크릴(monomeric acrylic) 또는 메타아크릴릭 에스테르(methacrylic ester)이고 단량체 B는 단량체 A와 공중합가능한 극성을 띤 단량체이다.

Description

의약 유동성 향상제에 내성을 가지는 압력에 민감한 점착성 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (24)

  1. (1) 경피를 통하여 투여하는 약학적으로 활성이 있는 약제에 피부투과도를 향상시키는 경피침투 향상제와; (2) 단량체 A가 1~14의 탄소원자수를 갖는, 일반적으로는 4~12의 탄소원자수를 갖는, 비-3차 알콜의 단량체의 아크릴릭 또는 메타크릴릭 에스테르이고, 단량체 B가 단량체 A와 공중합할 수 있는 극성을 띤 단량체일때, 그라프트된 중합체 성분을 갖는 주쇄 중합체를 형성하는 공중합된 단량체인 A와 B 로 구성되는, 상분리된 그라프트 공중합체를 구성하는 베이스 중합체 성분을 갖는 거대분자(macromer)로 보강된 베이스 중합체로 이루어진, 의약 유동 향상제에 내성이 있는 압력에 민감한 점착성 조성물.
  2. 제1항에 있어서, 상기 경피 침투 향상제는 솔비톨류(sorbitols), 에톡실레이티드 알킬 페놀류, 글리세롤, 프로필렌 글리콜, 폴리에틸렌 글리콜류, 지방산 에스테르류, 알콜류 및 아민류로 이루어진 군으로부터 선택된 조성물.
  3. 제1항에 있어서, 상기 그라프트 중합체 성분은 중합된 모노알케닐(monoalkenyl)-치환된 방향족 탄화수소인 조성물.
  4. 제3항에 있어서, 상기 중합된 모노알케닐-치환된 방향족 탄화수소는 폴리스티렌(polystyrene)을 구성하는 조성물.
  5. 제1항에 있어서, 상기 그라프트 중합체 성분의 분자량이 약 30,000~60,000인조성물.
  6. 제1항에 있어서, 그라프트 중합체 성분은 평균으로 중합체 주쇄당 1.5~2.5그라프트 성분량으로 존재하는 조성물.
  7. 제6항에 있어서, 상기 그라프트 중합체 성분은 평균으로 중합체 주쇄당 약 2중합체 성분량이 존재하는 조성물.
  8. 제1항에 있어서, 상기 단량체 B는 아크릴릭산, 메타크릴릭산, 이타코닉산, 아크릴아미드, 메틸아크릴아미드, 아크릴로니트릴(acrylonitrile), 메타크릴로니트릴(methacrylonitrile), 디아세톤 아크릴아미드 및 아크릴산의 2-카르복실 에틸 에스테르류로 이루어진 군으로부터 선택되는 것을 특징으로 하는 조성물.
  9. 제1항에 있어서, 상기 베이스 중합체는 중량비로 상기 단량체 A의 약 50~80%임을 특징으로 하는 조성물.
  10. 제1항에 있어서, 상기 단량체 A는 1-페탄올, 2-펜탄올, 3-펜탄올, 2-메틸-1-부탄올, 1-메틸-1-펜틴올, 2-메틸-1-펜틴올, 3-메틸-1-펜틴올, 2-에틸-1-부탄올, 3,5,5-트리메틸-1-헥산올, 3-헵탄올, 2-옥탄올, 1-데칸올, 1-도데칸올 등으로 이루어진 그룹으로부터 선택된 비-3차 알콜을 갖는 아크릴릭산 또는 메타크릴릭산의 에스테르를 포함함을 특징으로 하는 조성물.
  11. 제1항에 있어서, 상기 경피 침투 향상체는 중량비로 상기 조성물내에 약 40%까지 존재함을 특징으로 하는 조성물.
  12. 제11항에 있어서, 상기 경피 침투 향상제는 중량비로 상기 조성물내에 5~30%의 양이 존재함을 특징으로 하는 조성물.
  13. 활성이 있는 약제에 불침투성인 탄력성 있는 지지(backing) 물질을 구성하는 적어도 하나의 약물학적으로 활성이 있는 약제와 상기 지지(backing) 물질의 적어도 한 부위에 있는 점착성층을 갖는 경피 투여 시스템(transdermal delivery system)에 있어서, (1) 약제학적으로 활성이 있는 경피 투여용 약제에 대하여 피부투과도를 향상시키기 위한 경피 침투향상제와; (2) 단량체 A가 1~14의 탄소원자를, 일반적으로 4~12의 탄소원자수를, 갖는 비-3차 알콜의 단량체인 아크릴릭 또는 메타크릴릭 에스테르이고, 단량체 B가 단량체 A와 공중합할 수 있는 극성을 띤 단량체 일때, 그라프트된 중합체 성분을 갖는 주쇄 중합체를 형성하는 공중합할 수 있는 단량체 A 와 B로 이루어진 상분리된 그라프트 공중합체를 구성하는 베이스 중합체 성분을 갖는 거대분자 보강된 베이스 중합체로 이루어진, 압력이 민감한 점착성 조성물을 구성하는 점착층을 가지는 것을 특징으로 하는 경피투여시스템.
  14. 제13항에 있어서, 상기 경피침투 향상제는 소비톨류, 에톡실레이티드 알킬페놀류, 글리세롤, 프로필렌, 글리콜, 폴리에틸렌 글리콜류, 지방상 에스테르류, 알콜류 및 아민류로 이루어진 군으로부터 선택된 것임을 특징으로 하는 것을 특징으로 하는 경피투여 시스템.
  15. 제13항에 있어서, 상기 그라프트 중합체 성분은 중합된 모노알케닐-치환된 방향족 탄화수소인 것을 특징으로 한는 경피투여시스템.
  16. 제15항에 있어서, 상기 중합된 모노알케닐-치환된 방향족 탄화수소는 폴리스티렌(polystyrene)을 구성함을 특징으로 하는 경피투여시스템.
  17. 제13항에 있어서, 상기 그라프트 중합체 성분의 분자량은 30,000~60,000임을 특징으로 하는 경피투여시스템.
  18. 제13항에 있어서, 그라프트 중합체 성분은 평균적으로 중합체 주쇄당 1.5~25그라프트 성분량으로 존재하는 것을 특징으로 하는 경피투여시스템.
  19. 제18항에 있어서, 상기 그라프트 중합체 성분은 평균적으로 중합체 주쇄당 약 2중합체 성분의 양으로 존재함을 특징으로 하는 경피투여시스템.
  20. 제13항에 있어서, 상기 단량체 B는 아크릴릭산, 메타크릴릭산, 이타코틱산, 아크릴아미드, 메틸아크릴아미드, 아크릴로니트릴, 메타크릴로니트릴, 디아세톤 아크릴아미드 및 아크릴릭 산의 2-카르복실에틸 에스테르류로부터 선택되는 것을 특징으로 하는 경피투여시스템.
  21. 제13항에 있어서, 상기 베이스 중합체는 중량비로 상기 단량체 A의 약 50~80%임을 특징으로 하는 경피투여 시스템.
  22. 제13항에 있어서, 상기 단량체 A는 1-페탄올, 2-펜탄올, 3-펜탄올, 2-메틸-1-부탄올, 1-메틸-1-펜틴올, 2-메틸-1-펜틴올, 3-메틸-1-펜틴올, 2-에틸-1-부탄올, 3,5,5-트리메틸-1-엑산올, 3-헵탄올, 2-옥탄올, 1-데칸올, 1-도데칸올 등으로 이루어진 그룹으로부터 선택된 비-3차 알콜을 갖는 아크릴릭산 또는 메타크릴릭산의 에스테르를 포함함을 특징으로 하는 경피투여시스템.
  23. 제13항에 있어서, 상기 경피 침투 향상체는 중량비로 상기 조성물내에 약 40%까지 존재함을 특징으로 하는 경피투여시스템.
  24. 제23항에 있어서, 상기 경피 침투 향상제는 중량비로 상기 조성물내에 5~30%의 양이 존재함을 특징으로 하는 경피투여시스템.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960007140A 1995-03-17 1996-03-16 의약유동성향상제에내성을가지는압력에민감한점착조성물 KR100418489B1 (ko)

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US08/405,872 US5573778A (en) 1995-03-17 1995-03-17 Drug flux enhancer-tolerant pressure sensitive adhesive composition
US08/405872 1995-03-17
US08/405,872 1995-03-17

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KR960034348A true KR960034348A (ko) 1996-10-22
KR100418489B1 KR100418489B1 (ko) 2005-02-02

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CA2171911C (en) 2005-06-14
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US5573778A (en) 1996-11-12
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CA2171911A1 (en) 1996-09-18
EP0732100A2 (en) 1996-09-18
ES2204996T3 (es) 2004-05-01
KR100418489B1 (ko) 2005-02-02
AU4808596A (en) 1996-09-26
EP0732100A3 (en) 1998-07-08
ATE243509T1 (de) 2003-07-15
EP0732100B1 (en) 2003-06-25

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