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HRP20100676T1 - Cvrsti farmaceutski pripravak koji sadrzi benzazepine i postupak njegovog dobivanja - Google Patents

Cvrsti farmaceutski pripravak koji sadrzi benzazepine i postupak njegovog dobivanja Download PDF

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Publication number
HRP20100676T1
HRP20100676T1 HR20100676T HRP20100676T HRP20100676T1 HR P20100676 T1 HRP20100676 T1 HR P20100676T1 HR 20100676 T HR20100676 T HR 20100676T HR P20100676 T HRP20100676 T HR P20100676T HR P20100676 T1 HRP20100676 T1 HR P20100676T1
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Croatia
Prior art keywords
pharmaceutical preparation
solid pharmaceutical
hydroxypropyl cellulose
weight
amount
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HR20100676T
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English (en)
Inventor
Nakagawa Shinsuke
Suzuki Kai
Mukai Tadashi
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Otsuka Pharmaceutical Co.
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Application filed by Otsuka Pharmaceutical Co. filed Critical Otsuka Pharmaceutical Co.
Publication of HRP20100676T1 publication Critical patent/HRP20100676T1/hr

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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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/10Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cvrsti farmaceutski pripravak, naznacen time sto sadrzi: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrzi hidroksipropoksilnu skupinu u kolicini od 50 %, tezinski, ili vecoj; i (c) najmanje jedan clan kojeg se bira iz skupine koju cine karboksimetilceluloza, natrij-karboksimetilskrob, umrezeni povidon i nisko supstituirana hidroksipropilceluloza, prosjecnog promjera cestica od 30 do 70 μm, gdje 90 % cestica ima ukupni promjer od 100 do 200 μm. Patent sadrzi jos 16 patentnih zahtjeva.

Claims (17)

1. Čvrsti farmaceutski pripravak, naznačen time što sadrži: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; i (c) najmanje jedan član kojeg se bira iz skupine koju čine karboksimetilceluloza, natrij-karboksimetilškrob, umreženi povidon i nisko supstituirana hidroksipropilceluloza, prosječnog promjera čestica od 30 do 70 µm, gdje 90 % čestica ima ukupni promjer od 100 do 200 µm.
2. Čvrsti farmaceutski pripravak, naznačen time što sadrži: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; i (c-1) nisko supstituiranu hidroksipropilcelulozu, prosječnog promjera čestica od 30 do 70 µm, gdje 90 % čestica ima ukupni promjer od 100 do 200 µm.
3. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 2, naznačen time što prosječni promjer čestica nisko supstituirane hidroksipropilceluloze je 45 do 65 µm, gdje 90 % čestica ima ukupni promjer od 100 do 200 µm.
4. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 2, naznačen time što čvrsti farmaceutski pripravak je u obliku tablete.
5. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 2, naznačen time što se dobiva postupkom koji se sastoji od: Koraka 1 dobivanja amorfne smjese iz 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepina i/ili njegove soli i hidroksipropilceluloze koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; Koraka 2 miješanja amorfne smjese dobivene u Koraku 1 s nisko supstituiranom hidroksipropilcelulozom, prosječnog promjera čestica od 30 do 70 µm, gdje 90 % čestica ima ukupni promjer od 100 do 200 µm; i Koraka 3 obrade smjese dobivene u Koraku 2 u čvrsti pripravak.
6. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što ga se proizvodi postupkom koji se dodatno sastoji od, između Koraka 1 i Koraka 2, koraka obrade amorfne smjese dobivene u Koraku 1 u granule postupkom granuliranja.
7. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što ga se proizvodi postupkom koji se dodatno sastoji od, između Koraka 2 i Koraka 3, koraka obrade smjese dobivene u Koraku 2 u granule postupkom granuliranja.
8. Postupak proizvodnje čvrstog farmaceutskog pripravka u skladu s patentnim zahtjevom 2, naznačen time što se navedeni postupak sastoji od: Koraka 1 dobivanja amorfne smjese iz 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepina i/ili njegove soli i hidroksipropilceluloze koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; Koraka 2 miješanja amorfne smjese dobivene u Koraku 1 s nisko supstituiranom hidroksipropilcelulozom, prosječnog promjera čestica od 30 do 70 µm, gdje 90 % čestica ima ukupni promjer od 100 do 200 µm; i Koraka 3 obrade smjese dobivene u Koraku 2 u čvrsti pripravak.
9. Postupak u skladu s patentnim zahtjevom 8, naznačen time što Korak 3 se provodi obradom smjese dobivene u Koraku 2 u tablete.
10. Postupak u skladu s patentnim zahtjevom 8 ili 9, naznačen time što se dodatno sastoji, između Koraka 1 i Koraka 2, od koraka obrade amorfne smjese dobivene u Koraku 1 u granule postupkom granuliranja.
11. Postupak u skladu s patentnim zahtjevom 8 ili 9, naznačen time što se dodatno sastoji, između Koraka 2 i Koraka 3, od koraka obrade smjese dobivene u Koraku 2 u granule postupkom granuliranja.
12. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 1, naznačen time što sadrži: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; i (c-2) karboksimetilcelulozu.
13. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 12, naznačen time što udio karboksimetilceluloze je 7 do 15 %, težinski, od ukupne količine čvrstog farmaceutskog pripravka.
14. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 1, naznačen time što sadrži: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; i (c-3) natrij-karboksimetilškrob.
15. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 14, naznačen time što udio natrij-karboksimetilškroba je 0,5 do 15 %, težinski, od ukupne količine čvrstog farmaceutskog pripravka.
16. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 1, naznačen time što sadrži: (a) 7-klor-5-hidroksi-1-[2-metil-4-(2-metilbenzoilamino)benzoil]-2,3,4,5-tetrahidro-1H-benzoazepin i/ili njegovu sol; (b) hidroksipropilcelulozu koja sadrži hidroksipropoksilnu skupinu u količini od 50 %, težinski, ili većoj; i (c-4) umreženi povidon.
17. Čvrsti farmaceutski pripravak u skladu s patentnim zahtjevom 16, naznačen time što udio umreženog povidona je 2 do 15 %, težinski, od ukupne količine čvrstog farmaceutskog pripravka.
HR20100676T 2007-06-21 2010-12-07 Cvrsti farmaceutski pripravak koji sadrzi benzazepine i postupak njegovog dobivanja HRP20100676T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007163551 2007-06-21
PCT/JP2008/061686 WO2008156217A2 (en) 2007-06-21 2008-06-20 Pharmaceutical solid preparation comprising benzazepines and production method thereof

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HRP20100676T1 true HRP20100676T1 (hr) 2011-01-31

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US (4) US10905694B2 (hr)
EP (1) EP2167046B1 (hr)
JP (1) JP5289338B2 (hr)
KR (1) KR101526625B1 (hr)
CN (3) CN101686941A (hr)
AR (1) AR067077A1 (hr)
AT (1) ATE489944T1 (hr)
AU (1) AU2008264445B2 (hr)
BR (1) BRPI0813100A2 (hr)
CA (1) CA2689467A1 (hr)
CY (1) CY1111939T1 (hr)
DE (1) DE602008003816D1 (hr)
DK (1) DK2167046T3 (hr)
ES (1) ES2354030T3 (hr)
HK (1) HK1201719A1 (hr)
HR (1) HRP20100676T1 (hr)
IL (1) IL202179A (hr)
MX (1) MX2009014193A (hr)
MY (1) MY147599A (hr)
PL (1) PL2167046T3 (hr)
PT (1) PT2167046E (hr)
RU (1) RU2466717C2 (hr)
SI (1) SI2167046T1 (hr)
TW (1) TWI405574B (hr)
WO (1) WO2008156217A2 (hr)

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CN102228423B (zh) * 2011-06-29 2013-03-06 重庆市庆余堂制药有限公司 托伐普坦口服固体药物组合物及其制备方法
JP6057628B2 (ja) * 2012-09-06 2017-01-11 クリーンケミカル株式会社 人工透析装置のプライミング方法
TWI660748B (zh) 2013-03-01 2019-06-01 日商大塚製藥股份有限公司 用於口服投藥之包含非晶型托伐普坦(Tolvaptan)的懸浮液
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JP7352175B2 (ja) * 2019-12-25 2023-09-28 ニプロ株式会社 トルバプタン製剤
CN111888335A (zh) * 2020-08-21 2020-11-06 福安药业集团重庆礼邦药物开发有限公司 一种托伐普坦的药物固体制剂及制备方法
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EP4321154A1 (en) 2022-08-03 2024-02-14 Sanovel Ilac Sanayi Ve Ticaret A.S. A tablet of tolvaptan and at least one binder processed with spray granulation

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HK1201719A1 (en) 2015-09-11
BRPI0813100A2 (pt) 2014-12-23
KR20100038386A (ko) 2010-04-14
ES2354030T3 (es) 2011-03-09
DK2167046T3 (da) 2011-01-31
MY147599A (en) 2012-12-31
EP2167046B1 (en) 2010-12-01
TWI405574B (zh) 2013-08-21
IL202179A0 (en) 2010-06-16
ATE489944T1 (de) 2010-12-15
US20210113582A1 (en) 2021-04-22
CN103989644A (zh) 2014-08-20
MX2009014193A (es) 2010-01-28
CA2689467A1 (en) 2008-12-24
US10905694B2 (en) 2021-02-02
EP2167046A2 (en) 2010-03-31
CY1111939T1 (el) 2015-11-04
AU2008264445A1 (en) 2008-12-24
US20230321113A1 (en) 2023-10-12
KR101526625B1 (ko) 2015-06-05
PT2167046E (pt) 2011-02-10
CN101686941A (zh) 2010-03-31
IL202179A (en) 2012-10-31
RU2010101797A (ru) 2011-07-27
US20100323006A1 (en) 2010-12-23
CN103463095A (zh) 2013-12-25
AR067077A1 (es) 2009-09-30
JP5289338B2 (ja) 2013-09-11
PL2167046T3 (pl) 2011-05-31
WO2008156217A2 (en) 2008-12-24
US20210069207A1 (en) 2021-03-11
DE602008003816D1 (de) 2011-01-13
RU2466717C2 (ru) 2012-11-20
TW200911270A (en) 2009-03-16
WO2008156217A3 (en) 2009-02-26
AU2008264445B2 (en) 2013-06-27
SI2167046T1 (sl) 2011-03-31
JP2010530355A (ja) 2010-09-09

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