KR910011266A - 유체형태의 경구투여용 약학적 제제 - Google Patents

유체형태의 경구투여용 약학적 제제 Download PDF

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KR910011266A
KR910011266A KR1019900022344A KR900022344A KR910011266A KR 910011266 A KR910011266 A KR 910011266A KR 1019900022344 A KR1019900022344 A KR 1019900022344A KR 900022344 A KR900022344 A KR 900022344A KR 910011266 A KR910011266 A KR 910011266A
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weight
parts
formulation
alkyl
water
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KR1019900022344A
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KR0156735B1 (ko
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버나듀스 마리아 보이빙 게리트
데 니즈 헤리크
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에프.쥐.엠. 헤르만스 피.씨.샬크비크
악조 엔.브이
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

유체형태의 경구투여용 약학적 제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 생물학적활성 물질을 유체형태로 경구투여하기 위한 제제로서, 그 조성물이, 1) 1내지 5중량부의 저용해성 형태의 일반식(Ⅰ)화합물, 2)0.3내지 3중량부의 물과 유기 용매중에 용해 가능한 셀룰로즈 유도체, 3)4내지 20중량부의 물에 불용성인 약제학적 허용 중합체, 및 4)40내지 250중량부의 통상적인 조제용 충진제를 포함하는 것을 특징으로 하는 경구 투여용 분말 입자 제제.
    상기식에서, X는 산소 또는 질소, Y는 질소이거나, X가 탄소일 경우, 탄소를 나타낼수도 있으며, R1은 H,OH,O-알킬(C1-4), 알킬(C1-4) 또는 할로겐, R2는 H,OH,O-알킬(C1-4), 알킬(C1-4)또는 할로겐, R3는 H또는 알킬(C1-4)이며, 점선은 Y가 탄소 원자 일때 존재하거나 존재하지 않을 수 있는 부가의 결합을 나타낸다.
  2. 제1항에 있어서, 물에 불용성인 생물학적 활성 물질의 형태가 일반식(Ⅰ)화합물의 유리염기인 것을 특징으로 하는 분말 입자 제제.
  3. 제1항에 있어서, 물에 불용성인 아크릴레이트 중합체가 중합체로서 사용된 것을 특징으로 하는 분말 입자 제제.
  4. 제1항에 있어서, 셀룰로즈 유도체가 히드록시프로필셀룰로즈인 것을 특징으로 하는 분말 입자 제제.
  5. 제1항에 있어서, 만니톨이 충진제로 사용된 것을 특징으로 하는 분말 입자 제제.
  6. 제1항에 있어서, 상기 조성물이 a) 2내지 3중량부의 일반식(Ⅰ)의 유리염기, b) 8내지 15중량부의 물에 저투과성을 갖는 아크릴산과 메타크릴산 에스테르 공중합체를 함유한 아크릴 수지, c)0.8 내지 1.2중량부의 히드록시프로필 셀룰로즈, 및 d) 80 내지 150중량부의 만니톨을 포함하는 것을 특징으로 하는 분말 입자 제제.
  7. 제6항에 있어서, 일반식(Ⅰ)화합물이 마이안세린인 것을 특징으로 하는 분말 입자 제제.
  8. 전술한 항중 어느 한항에 있어서, 상기 조성물이 평균 입자 크기가 50 내지 500㎛인 미립자인 것을 특징으로 하는 분말 입자 제제.
  9. 제8항에 있어서, 조성물의 적어도 75%가 100 내지 300㎛의 입자 크기를 갖는 것을 특징으로 하는 분말 입자제제.
  10. 제8항 또는 제9항의 분말 입자를 제조하는 방법으로서, 성분 (1),(2) 및 (3)을 적당한 유기 용매에 용해시키는 단계, 성분(4)를 산출된 용액과 함께 입자화하는 단계, 용매를 증발시키는 단계, 및 산출된 입자를 소정의 입자크기로 선별하는 단계를 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900022344A 1989-12-30 1990-12-29 유체형태의 경구 투여용 약학적 제제 KR0156735B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
NL8903199 1989-12-30
NL89.03199 1989-12-30

Publications (2)

Publication Number Publication Date
KR910011266A true KR910011266A (ko) 1991-08-07
KR0156735B1 KR0156735B1 (ko) 1998-11-16

Family

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KR1019900022344A KR0156735B1 (ko) 1989-12-30 1990-12-29 유체형태의 경구 투여용 약학적 제제

Country Status (14)

Country Link
US (1) US5238688A (ko)
EP (1) EP0436252B1 (ko)
JP (1) JP3051459B2 (ko)
KR (1) KR0156735B1 (ko)
AT (1) ATE93136T1 (ko)
AU (1) AU634614B2 (ko)
CA (1) CA2033418C (ko)
DE (1) DE69002822T2 (ko)
DK (1) DK0436252T3 (ko)
ES (1) ES2060001T3 (ko)
IE (1) IE63986B1 (ko)
NZ (1) NZ236626A (ko)
PT (1) PT96401B (ko)
ZA (1) ZA9010452B (ko)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5328688A (en) * 1990-09-10 1994-07-12 Arch Development Corporation Recombinant herpes simplex viruses vaccines and methods
DE69913116T2 (de) * 1998-04-02 2004-06-03 Akzo Nobel N.V. Orale flüssige lösung enthaltend das antidepressivum mirtazapine
US6492320B2 (en) * 1999-09-24 2002-12-10 Rohm And Hass Company Multifunctional, granulated pellet aid and process
TWI256309B (en) * 1999-10-13 2006-06-11 Akzo Nobel Nv New formulation of mirtazapine
PL212421B1 (pl) * 2002-03-12 2012-09-28 Bristol Myers Squibb Co Kompozycja farmaceutyczna w postaci zawiesiny kwasowego leku i sposób jej wytwarzania oraz sposób maskowania gorzkiego lub innego nieprzyjemnego smaku leku
US7632521B2 (en) * 2003-07-15 2009-12-15 Eurand, Inc. Controlled release potassium chloride tablets
US7838029B1 (en) 2003-07-31 2010-11-23 Watson Laboratories, Inc. Mirtazapine solid dosage forms
US20070298107A1 (en) * 2003-11-25 2007-12-27 Aurobindo Pharma Ltd. Pharmaceutical Compositions of Mirtazapine
DE102004034043A1 (de) * 2004-07-13 2006-02-09 Krka Tovarna Zdravil, D.D. Feste pharmazeutische Zusammensetzung, die Mirtazapin enthält
US7811604B1 (en) 2005-11-14 2010-10-12 Barr Laboratories, Inc. Non-effervescent, orally disintegrating solid pharmaceutical dosage forms comprising clozapine and methods of making and using the same

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Publication number Priority date Publication date Assignee Title
US4128641A (en) * 1975-07-31 1978-12-05 Hzi Research Center Inc. Tetracyclic psychotropic drug
NL7809726A (nl) * 1978-09-26 1980-03-28 Akzo Nv Nieuwe tetracyclische verbindingen.
JPS5665825A (en) * 1979-10-31 1981-06-03 Mochida Pharmaceut Co Ltd Remedy for peptic ulcer
US4623588A (en) * 1984-02-06 1986-11-18 Biotek, Inc. Controlled release composite core coated microparticles
US4870060A (en) * 1985-03-15 1989-09-26 Janssen Pharmaceutica Derivatives of γ-cylodextrin
DE3612212A1 (de) * 1986-04-11 1987-10-15 Basf Ag Verfahren zur herstellung von festen pharmazeutischen formen
GB8613688D0 (en) * 1986-06-05 1986-07-09 Euro Celtique Sa Pharmaceutical composition
GB2196252B (en) * 1986-09-18 1990-10-17 London Pharmacy Innovation Gastric controlled-release dosage forms
EP0320097B1 (en) * 1987-10-16 2003-06-04 ELAN CORPORATION, Plc Controlled absorption diltiazem formulations
EP0319061A1 (en) * 1987-11-28 1989-06-07 Akzo N.V. Medicament with antiemetic action

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Publication number Publication date
DE69002822D1 (de) 1993-09-23
PT96401B (pt) 1998-06-30
ES2060001T3 (es) 1994-11-16
CA2033418A1 (en) 1991-07-01
AU6839890A (en) 1991-07-04
US5238688A (en) 1993-08-24
ZA9010452B (en) 1991-10-30
AU634614B2 (en) 1993-02-25
ATE93136T1 (de) 1993-09-15
IE63986B1 (en) 1995-06-28
DK0436252T3 (da) 1993-12-27
PT96401A (pt) 1991-10-15
IE904531A1 (en) 1991-07-03
DE69002822T2 (de) 1993-12-23
CA2033418C (en) 2002-05-14
JP3051459B2 (ja) 2000-06-12
NZ236626A (en) 1992-10-28
KR0156735B1 (ko) 1998-11-16
EP0436252A1 (en) 1991-07-10
JPH04210638A (ja) 1992-07-31
EP0436252B1 (en) 1993-08-18

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