KR880701536A - 마약성 진통제 및 길항제의 경피 흡수용량 단위 및 투여방법 - Google Patents

마약성 진통제 및 길항제의 경피 흡수용량 단위 및 투여방법

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Publication number
KR880701536A
KR880701536A KR1019880700481A KR880700481A KR880701536A KR 880701536 A KR880701536 A KR 880701536A KR 1019880700481 A KR1019880700481 A KR 1019880700481A KR 880700481 A KR880700481 A KR 880700481A KR 880701536 A KR880701536 A KR 880701536A
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South Korea
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polymer matrix
dosage unit
transdermal administration
polymer
administration according
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KR1019880700481A
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English (en)
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KR950012181B1 (ko
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더블유.치엔 이
치앙 친-치
도요 가부지
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원본미기재
루트저스, 더 스테이트 유니버서티 오브 뉴저지
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Publication of KR880701536A publication Critical patent/KR880701536A/ko
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Publication of KR950012181B1 publication Critical patent/KR950012181B1/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61F—FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F13/00—Bandages or dressings; Absorbent pads
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Sampling And Sample Adjustment (AREA)
  • Measurement Of The Respiration, Hearing Ability, Form, And Blood Characteristics Of Living Organisms (AREA)

Abstract

내용 없음

Description

마약성 진통제 및 길항제의 경피 흡수용량 단위 및 투여방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 피부투과 증진제를 사용하지 않는 중합체 매트릭스 용량단위 중의 각종 하이드로모르폰 함유량(%,W/W)에서 투과속도(mcg/cm2hr)를 예시하는 그래프이다.
제2도는 중합체 매트릭스층이 하이드로모르폰 10%(W/W) 및 일반식 CH3(CH2)nCOOH(여기서 n은 4 내지 6이다)의 피부투과 증진제 10%를 함유하는 용량 단위로부터 투과속도(mcg/cm2hr)를 예시하는 그래프이다.

Claims (21)

  1. (a) 경피적으로 전달되는 약제에 대하여 실질적으로 불투과성인 지지층; 및 (b) 상기 지지층에 고착되어 있으며, 모르피난(mophinan) 마약성 진통제 및 길항성 약제 중에서 선택된, 하나 이상의 유효량의 약제가 그안에 미세 분산되어 있는 중합체 매트릭스 디스크층(상기 중합체는 생물학적으로 허용되며, 경피 흡수를 위해 약제를 투과시키고 ; 상기 약제는 중합체 매트릭스 내에서 안정하고, 동시에 경피적으로 흡수됨으로써 적어도 최소한의 유효 1일 용량을 제공한다)으로 이루어진, 경피 투여용 모르피난 마약성 진통제 또는 길항성 약제 중합체 매트릭스 용량단위.
  2. 제 1 항에 있어서, 중합체 매트릭스층이 그 내부에 하나 이상의 유효량이 피부투과 증진제를 분산된 형태로 함유하고 있는 경피 투여용 중합체 매트릭스 용량단위.
  3. 제 1 항에 있어서, 중합체 매트릭스가 실리콘 중합체 또는 공중합체인 경피 투여용 중합체 매트릭스 용량단위.
  4. 제 3항에 있어서, 실리콘 중합체 또는 공중합체가 메틸 실리콘 중합체 또는 공중합체 또는 메틸비닐실리콘 중합체 또는 공중합체인 경피 투여용 중합체 매트릭스 용량단위.
  5. 제 1 항에 있어서, 중합체 매트릭스 디스크층이 하기 일반식 가교 결합된 폴리실옥산 중합체인 경피 투여용 중합체 매트릭스 용량단위 :
    상기 식에서, R은 탄소수 1내지 7의 알킬 또는 알콕시, 비닐 , 페닐 또는 그의 조합이고;n은 약 100 내지 약 5,000이다.
  6. 제 3 항에 있어서, 매트릭스가 약 10 내지 약 200마이크론의 단면크기를 갖는 미세 분산된 부분으로 이루어진 경피 투여용 중합체 매트릭스 용량단위.
  7. 제 1 항에 있어서, 약제가 하이드로모르폰인 경피 투여용 중합체 매트릭스 용량단위.
  8. 제 7 항에 있어서, 하이드로모르폰이 중합체 매트릭스층내에, 매트릭스 중합체 중량에 기준하여 적어도 약 10중량%의 양으로 적하되어 존재하는 경피 투여용 중합체 매트릭스 용량단위.
  9. 제 7 항에 있어서, 하이드로모르폰이 중합체 매트릭스층내에, 매트릭스 중합체 중량에 기준하여 약 10중량%의 양으로 적하되어 존재하는 경피 투여용 중합체 매트릭스 용량단위.
  10. 제 1 항에 있어서, 적어도 약 1.2mg이 유효량의 약제가 24시간내에 경피적으로 전달되는 경피 투여용 중합체 매트릭스 용량단위.
  11. 제10항에 있어서, 약제가 하이드로모르폰인 경피 투여용 중합체 매트릭스 용량단위.
  12. 제11항에 있어서, 적어도 2.4mg의 하이드로모르폰이 24시간내에 경피적으로 전달되는 경피 투여용 중합체 매트릭스 용량단위.
  13. 제 3항에 있어서, 실리콘 중합체는 가교-결합된 실옥산 중합체이며, 적어도 1.2mg의 하이드로모르폰 약제가 24시간내에 경피적으로 전달되는 경피 투여용 중합체 매트릭스 용량단위.
  14. 제13항에 있어서, 경피적으로 전달된 양이 24시간내에 적어도 2.4mg인 경피 투여용 중합체 매트릭스 용량단위.
  15. 제13항에 있어서, 가교-결합된 실리콘 중합체가 폴리디메틸실옥산인 경피 투여용 중합체 매트릭스 용량단위.
  16. 제13항에 있어서, 가교-결합된 실리콘 중합체가 가교-결합된 메틸비닐 실리콘 중합체인 경피 투여용 중합체 매트릭스 용량단위.
  17. 제13항에 있어서, 매트릭스층에 존재하는 피부투과 증진제가 접착성층 또는 두개의 층에 존재하며 이소프로필미리스테이트, 일반식이 CH3(CH2)nCOOH(여기서, n은 4 내지 16의 정수이다)인 포화 지방산, 일반식이 CH3(CH2)nCH2OH(여기서, n은 4 내지 16의 정수이다)인 포화알콜, 아존, 에틸 카프릴레이트, 헥사메틸렌 라우르아미드, 헥사메틸렌 팔미트아미드, 및 에틸카프렐레이트 및 카프릴 알콜의 혼합물 중에서 선택된 경피 투여용 방출-조절 중합체 매트릭스 용량단위.
  18. 제17항에 있어서, 피부투과 증진제가 아존인 경피 투여용 용량단위.
  19. 제17항에 있어서, 피부투과 증진제가 이소프로필 미리스테이트인 경피 투여용 용량단위.
  20. 제17항에 있어서, 피부투과 증진제가 에틸 카프릴레이트인 경피 투여용 용량단위.
  21. 제17항에 있어서, 피부투과 증진제가 에틸 카프릴레이트 및 카프릴 알콜의 혼합물인 경피 투여용 용량단위.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880700481A 1986-09-03 1987-09-02 마약성 진통제 및 길항제의 경피흡수 용량단위 KR950012181B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US903,273 1986-09-03
US06/903,273 US4806341A (en) 1985-02-25 1986-09-03 Transdermal absorption dosage unit for narcotic analgesics and antagonists and process for administration
US903273 1986-09-03
PCT/US1987/002198 WO1988001497A1 (en) 1986-09-03 1987-09-02 Transdermal absorption dosage unit for narcotic analgesics and antagonists and process for administration

Publications (2)

Publication Number Publication Date
KR880701536A true KR880701536A (ko) 1988-11-03
KR950012181B1 KR950012181B1 (ko) 1995-10-14

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KR1019880700481A KR950012181B1 (ko) 1986-09-03 1987-09-02 마약성 진통제 및 길항제의 경피흡수 용량단위

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US (1) US4806341A (ko)
EP (1) EP0290482B1 (ko)
JP (1) JPH02500741A (ko)
KR (1) KR950012181B1 (ko)
AT (1) ATE119380T1 (ko)
AU (1) AU628284B2 (ko)
CA (1) CA1309659C (ko)
DE (1) DE3751140T2 (ko)
DK (1) DK175580B1 (ko)
FI (1) FI98887C (ko)
WO (1) WO1988001497A1 (ko)

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CA1309659C (en) 1992-11-03
FI890995A (fi) 1989-03-02
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ATE119380T1 (de) 1995-03-15
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