KR850000241A - 경구용 당뇨병 치료제 제형의 제조방법 - Google Patents

경구용 당뇨병 치료제 제형의 제조방법 Download PDF

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KR850000241A
KR850000241A KR1019840003189A KR840003189A KR850000241A KR 850000241 A KR850000241 A KR 850000241A KR 1019840003189 A KR1019840003189 A KR 1019840003189A KR 840003189 A KR840003189 A KR 840003189A KR 850000241 A KR850000241 A KR 850000241A
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basic
active substance
mixture
excipient
excipients
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KR1019840003189A
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KR910004572B1 (ko
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브리클(외 3) 롤프
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베첼, 조머
닥터 칼토메 게젤샤프트 미트 베쉬렌크터르 하프퉁
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • C07C405/0008Analogues having the carboxyl group in the side-chains replaced by other functional groups
    • C07C405/0033Analogues having the carboxyl group in the side-chains replaced by other functional groups containing sulfur
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis

Abstract

내용 없음.

Description

경구용 당뇨병 치료제 제형의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 건강한 지원자의 글루코스 농도 비교를 나타낸다.
제2도는 글라퀴돈의 혈장농도를 나타낸다.

Claims (13)

  1. 용매중 하나 이상의 용해제 및/또는 유화물질 존재하에 산성적으로 반응하는 활성물질을 염기성 부형제로 용해시키거나, 양성적으로 반응하는 활성물질을 염기성 또는 산성 부형제로 용해시키거나, 염기성적으로 반응하는 활성물질을 산성 부형제로 용해시키고, 이때 염기성 또는 산성 부형제에 대한 활성물질의 몰비는 1:1이하로 하여야 하며, 생성된 용액을 수-불용성 담체에 적용시킨 다음에 건조시키고, 이 생성물을 될 수 있는 한 부형제를 가하여 더욱 처리하여 약제학적 제형을 제조함을 특징으로 하여, 항당뇨병 활성물질을 함유하는 경구용 제제 형태를 제조하는 방법.
  2. 제1항에 있어서, 경구용 항당뇨병 활성 설포닐우레아가 사용됨을 특징으로 하는 방법.
  3. 제2항에 있어서, 글리퀴돈이 활성물질로서 사용됨을 특징으로 하는 방법.
  4. 제1항에 있어서, 사용된 경구용 항당뇨병 활성물질이 a) 일반식(Ⅰ)의 4-[2-아로일아미노)에틸]-벤조산, 또는 b) 일반식(Ⅱ)의 치환된 4-(아르알킬아미노카보닐메틸)-벤조산 또는 이들의 혼합물임을 특징으로 하는 방법.
    상기식에서 R1은 할로겐 원자, 바람직하게는 염소원자이고, R2는 탄소수 1내지 3의 알콕시그룹, 바람직하게는 메톡시그룹, 또는 피페리딘-1-일 또는 옥타메틸렌 이미노 그룹이며, R3는 탄소수 1 내지 4의 알킬그룹, 바람직하게는 n-프로필, 또는 페닐그룹이고, R4는 피레리딘-1-일, 피롤리딘-1-일 또는 헥사메틸렌이미노그룹이며, R5는 수소 또는 할로겐원자 또는 메틸 또는 메톡시그룹이다.
  5. 제1항 내지 제4항중의 어느 하나에 있어서, 염기성 부형제(이때, 염기성 부형제의 혼합물도 또한 사용할 수 있다)에 대한 활성물질의 몰비가 1:1.1 내지 1:10중량부로 유지됨을 특징으로 하는 방법.
  6. 제1항 내지 5항 중의 어느 하나에 있어서, 용해물질 총량에 대한 활성물질의 비가 1:1 내지 1:10중량부로 유지됨을 특징으로 하는 방법.
  7. 제1항 내지 6항 중의 어느 하나에 있어서, 사용된 수-불용성 담체가 고도로 분산된 실리콘 다이옥사이드, 미세결정성 셀룰로우즈, 염기성 알루미늄 옥사이드, 마그네슘-알루미늄-트리실리케이트, 교차 결합된 폴리비닐 피롤리돈, 나트륨 카복시메틸 전분, 트리칼슘 포스페이트, 칼슘 하이드로겐 포스페이트, 또는 이들 물질들의 혼합물이고, 사용된 용해제 및/또는 유화물질이 폴리비닐 피롤리돈, 폴리에틸렌 글리콜, 폴리에톡실화된 소르비탄모노-올레이트, 소르비톨, 폴리옥시에틸렌 폴리옥시프로필렌폴리머, 폴리옥시에틸렌 지방알코올 에테르 및 글리세롤 폴리에틸렌 글리콜옥시스테아레이트 또는 이들 물질들의 혼합물임을 특징으로 하는 방법.
  8. 제7항에 있어서, 폴리비닐피롤리돈 및/또는 폴리옥시에틸렌 폴리옥시프로필렌 폴리머가 용해물질로서 사용됨을 특징으로 하는 방법.
  9. 제1항 내지 제8항 중의 어느 하나에 있어서, 사용된 염기성 부형제가 생리적으로 무해한 무기 또는 유기 염기, 특히 수산화나트륨 용액, 수산화칼륨 용액, 암모니아, 3급-나트륨 포스페이트, 디에탄올아민, 에틸렌디아민, L-리신 또는 N-메틸글루카아민임을 특징으로 하는 방법.
  10. 제1항에 있어서, 활성물질 또는 활성물질들의 혼합물 이외에도, 염기성 부형제 또는 염기성 부형제의 혼합물, 하나 이상의 수-불용성 담체 및 임의로 하나 이상의 용해제 및/또는 부형제를 함유하며, 이때 염기성 부형제에 대한 활성물질의 몰비가 1:1이하임을 특징으로 하는 제제 형태의 제조방법.
  11. 제1항에 있어서, 함유된 염기가 생리적으로 허용되는 무기 또는 유기 염기이고, 산이 황산이며, 수-불용성 담체가 고도로 분산된 실리콘 다이옥사이드, 미세결정성 셀룰로오즈, 염기성 알루미늄 옥사이드, 마그네슘-알루미늄-트리실리케이트, 교차 결합된 폴리비닐피롤리돈, 나트륨카복시메틸 전분, 트리칼슘 포스페이트, 칼슘하이드로겐포스페이트 또는 이들 물질들의 혼합물이고, 용해물질이 폴리비닐피롤리돈, 폴리에틸렌 글리콜, 폴리에톡실화된 소르비탄모노-올레이트, 소르비톨, 폴리옥시에틸렌 폴리옥시르로필렌폴리머, 글리세롤폴리에틸렌 글리콜옥시스테아레이트 또는 이들 물질들의 혼합물임을 특징으로 하는 제제 형태의 제조방법.
  12. 제1항, 제10항 및 제11항 중의 어느 하나에 있어서, 염기성 부형제로서 수산화 나트륨 용액, 수산화 칼륨 용액, 암모니아, 3급-나트륨 포스페이트, 디에탈올아민, 에틸렌디아민, L-리신 또는 N-메틸글루카민을 함유하며, 이때 염기성 부형제에 대한 활성물질의 몰비가 1:1.1 내지 1:10임을 특징으로 하는 제제형태의 제조방법.
  13. 제1항 및 제10항 내지 제12항 중의 어느 하나에 있어서, 활성물질과 용해 부형제 또는 이들의 혼합물을 1:1 내지 1:10중량비의 비율로 함유하고, 활성물질과 담체 또는 이들의 혼합물을 1:1 내지 1:12중량부의 비율로 함유함을 특징으로 하는 제제형태의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019840003189A 1983-06-08 1984-06-07 경구용 당뇨병 치료제 제형의 제조방법 KR910004572B1 (ko)

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DEP3320583.3 1983-06-08
DE19833320583 DE3320583A1 (de) 1983-06-08 1983-06-08 Neue galenische zubereitungsformen von oralen antidiabetika und verfahren zu ihrer herstellung

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KR850000241A true KR850000241A (ko) 1985-02-26
KR910004572B1 KR910004572B1 (ko) 1991-07-06

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US (2) US4708868A (ko)
EP (1) EP0128482B1 (ko)
JP (1) JPS6075435A (ko)
KR (1) KR910004572B1 (ko)
AT (1) ATE49886T1 (ko)
AU (1) AU562803B2 (ko)
CA (1) CA1228300A (ko)
DD (1) DD223360A5 (ko)
DE (2) DE3320583A1 (ko)
DK (1) DK162018C (ko)
ES (1) ES8601697A1 (ko)
FI (1) FI85218C (ko)
GB (1) GB2142235B (ko)
GR (1) GR82363B (ko)
HK (1) HK72287A (ko)
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IE (1) IE57792B1 (ko)
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IE57792B1 (en) 1993-04-07
NO168629B (no) 1991-12-09
HU192407B (en) 1987-06-29
NZ208416A (en) 1987-06-30
GB2142235A (en) 1985-01-16
ZA844295B (en) 1986-02-26
IE841422L (en) 1984-12-08
US4873080A (en) 1989-10-10
GB8414528D0 (en) 1984-07-11
KR910004572B1 (ko) 1991-07-06
MY100764A (en) 1991-02-15
ES533207A0 (es) 1985-11-16
GR82363B (ko) 1984-12-13
FI842295A0 (fi) 1984-06-07
CA1228300A (en) 1987-10-20
HK72287A (en) 1987-10-16
DK162018C (da) 1992-02-10
JPH0548206B2 (ko) 1993-07-20
JPS6075435A (ja) 1985-04-27
DK280884D0 (da) 1984-06-07
ES8601697A1 (es) 1985-11-16
FI85218C (fi) 1992-03-25
IL72033A (en) 1987-08-31
ATE49886T1 (de) 1990-02-15
PT78711A (de) 1984-07-01
HUT34349A (en) 1985-03-28
DK162018B (da) 1991-09-09
AU562803B2 (en) 1987-06-18
EP0128482A3 (en) 1986-06-25
SG48087G (en) 1987-08-28
EP0128482B1 (de) 1990-01-31
NO168629C (no) 1992-03-18
IL72033A0 (en) 1984-10-31
FI842295A (fi) 1984-12-09
PT78711B (de) 1986-10-21
DE3481170D1 (de) 1990-03-08
US4708868A (en) 1987-11-24
DD223360A5 (de) 1985-06-12
FI85218B (fi) 1991-12-13
AU2924184A (en) 1984-12-13
DK280884A (da) 1984-12-09
EP0128482A2 (de) 1984-12-19
NO842291L (no) 1984-12-10
GB2142235B (en) 1987-04-08
DE3320583A1 (de) 1984-12-13

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