KR850000240A - 경구용 당뇨병 치료제 제형의 제조방법 - Google Patents

경구용 당뇨병 치료제 제형의 제조방법 Download PDF

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KR850000240A
KR850000240A KR1019840003188A KR840003188A KR850000240A KR 850000240 A KR850000240 A KR 850000240A KR 1019840003188 A KR1019840003188 A KR 1019840003188A KR 840003188 A KR840003188 A KR 840003188A KR 850000240 A KR850000240 A KR 850000240A
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basic
active substance
excipient
group
benzoic acid
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KR1019840003188A
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KR910004571B1 (ko
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셉키(외 3) 고트프리드
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웨첼, 좀머
닥터칼토메 게젤샤프트 미트 베슈랭크터 하프퉁
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574Esters of oxyacids of phosphorus
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Steroid Compounds (AREA)

Abstract

내용 없음.

Description

경구용 당뇨병 치료제 제형의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 공복상태인 건강인에게 실시예 2,6,8에 상응하는 제형을 투여하여 그의 혈당치를 비교한 것이다.

Claims (8)

  1. 용매중의 폴리비닐피룰리돈 및 임의의 기타 가용화제의 존재하에서, 산성적으로 반응하는 활성물질을 염기성 부형제의 보조로 용해시키거나, 양(兩)성적으로 반응하는 활성물질을 염기성 또는 산성 부형제의 보조로 용해시키거나, 또는 염기성적으로 반응하는 활성물질을 산성 부형제의 보조로 용해시키고, 이때 염기성 또는 산성 부형제의 대한 활성물질의 몰비가 1:1미만이어야 하며, 생성된 용액을 증발시켜 건고시킨 다음, 다른 부형제로 임의로 더욱 처리하여 목적하는 제형을 제조함을 특징으로 하여 당뇨병 치료작용을 지닌 활성물질을 함유하는 경구용 제형을 제조하는 방법.
  2. 제1항에 있어서 경구용의 당뇨병 치료작용을 지닌 설포닐우레아를 사용함을 특징으로 하는 방법.
  3. 제1항에 있어서, 사용된 경구용의 당뇨병 치료작용을 지닌 활성물질이 a) 일반식(1)의 4-[2-아로일아미노)에틸]-벤조산이거나 b) 일반식(Ⅱ)의 치환된 4-(아르알킬아미노카보닐-메틸)-벤조산이거나 또는 이들 물질의 혼합물임을 특징으로 하는 방법.
    상기식에서, R1은 할로겐원자, 바람직하게는 염소원자를 나타내고, R2는 탄소수 1 내지 3의 알콕시그룹, 또는 피페리딘-1-일 또는 옥타메틸렌이미노 그룹을 나타내며, R3는 탄소수 1 내지 4의 알킬그룹, 바람직하게는 n-프로필그룹, 또는 페닐그룹을 나타내고, R4는 피페리딘-1-일, 피롤리딘-1-일 또는 헥사메틸렌이미노그룹을 나타내며, R5는 수소 또는 할로겐원자, 또는 메틸 도는 메톡시그룹을 나타낸다.
  4. 제1항에 있어서, 1개 이상의 염기성 부형제를 첨가하여, 활성물질 또는 활성물질들을 용매중에 용해시키고, 이때 염기성 부형제에 대한 활성물질의 몰비가 1:1미만이어야 하며, 여기에 폴리비닐피롤리돈 및 임의의 기타 가용화제를 용해시키고, 이 용액을 증발 건고시킨 다음 임의로 기타 부형제로 더욱 처리하여 목적하는 제제를 얻음을 특징으로 하여 글리퀴돈 및/또는 4-[2-(5-클로로-2-옥타메틸렌이미노-벤조일아미노)에틸]벤조산 및/또는 4-[N-(1α-페닐-2-피페리디노-벤질)-아미노카보닐메틸]-벤조산 및/또는 4-[[1-(2-피페리디노-페닐)-1-부틸]-아미노카보닐케틸]-벤조산 및 용성담체를 함유하는 제1항에서와 같은 경구용의 당뇨병 치료작용을 지닌 제형의 제조방법.
  5. 제1항 내지 4항중 어느 하나에 있어서, 염기성 또는 산성 부형에 대한 활성물질의 몰비를 1:1.1내지 1:10으로 유지하며, 이때 또한 염기성 부형제의 혼합물을 사용할 수 있음을 특징으로 하는 방법.
  6. 제1항 내지 5항중 어느 하나에 있어서, 활성물질 또는 활성물질들의 혼합물과 폴리비닐피롤리돈이 1:1내지 1:10중량부의 비율로 함유됨을 특징으로 하는 방법.
  7. 제1항 내지 6항중 어느 하나에 있어서, 사용된 기타의 가용화제가 폴리옥시에틸렌 폴리옥시프로필렌 중합체, 폴리에틸렌글리콜, 폴리에톡실화 소르비탄모노올레이트, 소르비톨, 글리세롤폴리-에틸렌 글리콜옥 시스테아레이트, 폴리옥시에틸렌 지방알코올 에테르 또는 이들 물질의 혼합물임을 특징으로 하는 방법.
  8. 제1항 내지 6항중 어느 하나에 있어서, 사용된 염기가 수산화나트륨 용액, 수산화칼륨 용액, 암모니아3급인산나트륨, 디에탄올아미, L-리신, 에틸렌디아민, 또는 N-메틸-글루카민임을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019840003188A 1983-06-08 1984-06-07 경구용 당뇨병치료 제제를 제조하는 방법 KR910004571B1 (ko)

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Application Number Priority Date Filing Date Title
DE19833320582 DE3320582A1 (de) 1983-06-08 1983-06-08 Gliquidonhaltige zubereitungsformen und verfahren zu ihrer herstellung
DEP3320582.5 1983-06-08

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KR850000240A true KR850000240A (ko) 1985-02-26
KR910004571B1 KR910004571B1 (ko) 1991-07-06

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US (2) US4696815A (ko)
EP (1) EP0128483B1 (ko)
JP (1) JPS6069038A (ko)
KR (1) KR910004571B1 (ko)
AT (1) ATE56365T1 (ko)
AU (1) AU563642B2 (ko)
CA (1) CA1228299A (ko)
DD (1) DD224216A5 (ko)
DE (2) DE3320582A1 (ko)
DK (1) DK162019C (ko)
ES (1) ES8506446A1 (ko)
FI (1) FI85217C (ko)
GB (1) GB2142236B (ko)
GR (1) GR82362B (ko)
HK (1) HK72387A (ko)
HU (1) HU193932B (ko)
IE (1) IE57793B1 (ko)
IL (1) IL72034A (ko)
MY (1) MY100795A (ko)
NO (1) NO168628C (ko)
NZ (1) NZ208417A (ko)
PH (1) PH24567A (ko)
PT (1) PT78710B (ko)
SG (1) SG48187G (ko)
ZA (1) ZA844296B (ko)

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Publication number Publication date
MY100795A (en) 1991-02-28
FI842294A0 (fi) 1984-06-07
DE3320582A1 (de) 1984-12-13
PT78710B (de) 1986-10-21
ES533208A0 (es) 1985-08-01
GB8414529D0 (en) 1984-07-11
GB2142236A (en) 1985-01-16
FI85217C (fi) 1992-03-25
NO168628B (no) 1991-12-09
GR82362B (ko) 1984-12-13
HUT34689A (en) 1985-04-28
IL72034A0 (en) 1984-10-31
SG48187G (en) 1988-01-15
IE57793B1 (en) 1993-04-07
DK281184D0 (da) 1984-06-07
DK281184A (da) 1984-12-09
ES8506446A1 (es) 1985-08-01
EP0128483A3 (en) 1986-07-02
JPH0587492B2 (ko) 1993-12-16
NO842290L (no) 1984-12-10
AU2924084A (en) 1984-12-13
JPS6069038A (ja) 1985-04-19
HK72387A (en) 1987-10-16
EP0128483A2 (de) 1984-12-19
DD224216A5 (de) 1985-07-03
FI85217B (fi) 1991-12-13
ATE56365T1 (de) 1990-09-15
ZA844296B (en) 1986-02-26
DK162019B (da) 1991-09-09
GB2142236B (en) 1987-04-08
IL72034A (en) 1987-09-16
DE3483175D1 (de) 1990-10-18
HU193932B (en) 1987-12-28
EP0128483B1 (de) 1990-09-12
US4696815A (en) 1987-09-29
KR910004571B1 (ko) 1991-07-06
NZ208417A (en) 1987-07-31
AU563642B2 (en) 1987-07-16
PH24567A (en) 1990-08-03
PT78710A (de) 1984-07-01
IE841423L (en) 1984-12-08
CA1228299A (en) 1987-10-20
DK162019C (da) 1992-02-10
NO168628C (no) 1992-03-18
FI842294A (fi) 1984-12-09
US4863724A (en) 1989-09-05

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