CN1984644B - 亲脂性药物的稳定的过饱和固体 - Google Patents

亲脂性药物的稳定的过饱和固体 Download PDF

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Publication number
CN1984644B
CN1984644B CN2005800150633A CN200580015063A CN1984644B CN 1984644 B CN1984644 B CN 1984644B CN 2005800150633 A CN2005800150633 A CN 2005800150633A CN 200580015063 A CN200580015063 A CN 200580015063A CN 1984644 B CN1984644 B CN 1984644B
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CN
China
Prior art keywords
solvent
composition
norethindrone
steroidal
molecule
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN2005800150633A
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English (en)
Chinese (zh)
Other versions
CN1984644A (zh
Inventor
阿德里安·丰克
托尔斯滕·瓦格纳
拉尔夫·利普
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Bayer Intellectual Property GmbH
Original Assignee
Bayer Schering Pharma AG
Schering AG
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Application filed by Bayer Schering Pharma AG, Schering AG filed Critical Bayer Schering Pharma AG
Publication of CN1984644A publication Critical patent/CN1984644A/zh
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    • 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
    • A61K9/08—Solutions
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate 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
    • A61K9/143—Intimate 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 inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
CN2005800150633A 2004-03-10 2005-03-10 亲脂性药物的稳定的过饱和固体 Expired - Fee Related CN1984644B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US55133004P 2004-03-10 2004-03-10
EP14075714.8 2004-03-10
EP04075714 2004-03-10
US60/551,330 2004-03-10
EP04075714.8 2004-03-10
PCT/IB2005/000748 WO2005087199A2 (en) 2004-03-10 2005-03-10 Stabilised supersaturated solid solutions of steroidal drugs

Publications (2)

Publication Number Publication Date
CN1984644A CN1984644A (zh) 2007-06-20
CN1984644B true CN1984644B (zh) 2010-12-08

Family

ID=34928105

Family Applications (1)

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CN2005800150633A Expired - Fee Related CN1984644B (zh) 2004-03-10 2005-03-10 亲脂性药物的稳定的过饱和固体

Country Status (32)

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US (1) US8715735B2 (enExample)
EP (2) EP2087883B1 (enExample)
JP (1) JP5006185B2 (enExample)
KR (1) KR101210695B1 (enExample)
CN (1) CN1984644B (enExample)
AR (1) AR048500A1 (enExample)
AT (1) ATE442131T1 (enExample)
AU (1) AU2005221403B8 (enExample)
BR (1) BRPI0507342A (enExample)
CA (1) CA2558582C (enExample)
CR (1) CR8630A (enExample)
DE (1) DE602005016551D1 (enExample)
DK (1) DK1765290T3 (enExample)
EA (1) EA012746B1 (enExample)
EC (1) ECSP066902A (enExample)
ES (2) ES2332229T3 (enExample)
GT (1) GT200500045A (enExample)
HR (1) HRP20090614T1 (enExample)
IL (1) IL177894A0 (enExample)
MY (1) MY142989A (enExample)
NO (1) NO20064473L (enExample)
NZ (1) NZ549793A (enExample)
PA (1) PA8626101A1 (enExample)
PE (1) PE20060016A1 (enExample)
PL (1) PL1765290T3 (enExample)
PT (1) PT1765290E (enExample)
RS (1) RS51076B (enExample)
SI (1) SI1765290T1 (enExample)
SV (1) SV2005002044A (enExample)
TW (1) TWI345986B (enExample)
UY (1) UY28803A1 (enExample)
WO (1) WO2005087199A2 (enExample)

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实施例6、12-13.
说明书第2页第49-54行、第3页第1-3行.

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MY142989A (en) 2011-02-14
PL1765290T3 (pl) 2010-02-26
KR101210695B1 (ko) 2012-12-11
EP2087883B1 (en) 2012-07-25
SI1765290T1 (sl) 2010-01-29
KR20060132999A (ko) 2006-12-22
BRPI0507342A (pt) 2007-07-03
AR048500A1 (es) 2006-05-03
JP5006185B2 (ja) 2012-08-22
US8715735B2 (en) 2014-05-06
AU2005221403A1 (en) 2005-09-22
ECSP066902A (es) 2006-12-20
ATE442131T1 (de) 2009-09-15
HK1103660A1 (en) 2007-12-28
WO2005087199A2 (en) 2005-09-22
CA2558582C (en) 2013-07-16
JP2007528389A (ja) 2007-10-11
ES2332229T3 (es) 2010-01-29
DE602005016551D1 (de) 2009-10-22
TWI345986B (en) 2011-08-01
CN1984644A (zh) 2007-06-20
WO2005087199A8 (en) 2007-03-29
DK1765290T3 (da) 2009-11-02
RS51076B (sr) 2010-10-31
NZ549793A (en) 2010-06-25
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PA8626101A1 (es) 2006-07-03
HRP20090614T1 (hr) 2009-12-31
GT200500045A (es) 2005-10-31
UY28803A1 (es) 2005-10-31
AU2005221403B8 (en) 2010-01-07
EP1765290B1 (en) 2009-09-09
EP1765290A2 (en) 2007-03-28
CA2558582A1 (en) 2005-09-22
PE20060016A1 (es) 2006-02-16
ES2390406T3 (es) 2012-11-12
TW200600116A (en) 2006-01-01
NO20064473L (no) 2006-10-10
EA012746B1 (ru) 2009-12-30
US20050207990A1 (en) 2005-09-22
SV2005002044A (es) 2005-11-04
EA200601588A1 (ru) 2007-02-27
AU2005221403B2 (en) 2009-12-10
IL177894A0 (en) 2006-12-31
PT1765290E (pt) 2009-11-23
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CR8630A (es) 2007-06-06

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