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

Landscapes

  • 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
US60/551,330 2004-03-10
EP04075714.8 2004-03-10
EP04075714 2004-03-10
EP14075714.8 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)

Application Number Title Priority Date Filing Date
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)

Country Link
US (1) US8715735B2 (https=)
EP (2) EP1765290B1 (https=)
JP (1) JP5006185B2 (https=)
KR (1) KR101210695B1 (https=)
CN (1) CN1984644B (https=)
AR (1) AR048500A1 (https=)
AT (1) ATE442131T1 (https=)
AU (1) AU2005221403B8 (https=)
BR (1) BRPI0507342A (https=)
CA (1) CA2558582C (https=)
CR (1) CR8630A (https=)
DE (1) DE602005016551D1 (https=)
DK (1) DK1765290T3 (https=)
EA (1) EA012746B1 (https=)
EC (1) ECSP066902A (https=)
ES (2) ES2332229T3 (https=)
GT (1) GT200500045A (https=)
HR (1) HRP20090614T1 (https=)
IL (1) IL177894A0 (https=)
MY (1) MY142989A (https=)
NO (1) NO20064473L (https=)
NZ (1) NZ549793A (https=)
PA (1) PA8626101A1 (https=)
PE (1) PE20060016A1 (https=)
PL (1) PL1765290T3 (https=)
PT (1) PT1765290E (https=)
RS (1) RS51076B (https=)
SI (1) SI1765290T1 (https=)
SV (1) SV2005002044A (https=)
TW (1) TWI345986B (https=)
UY (1) UY28803A1 (https=)
WO (1) WO2005087199A2 (https=)

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US4254099A (en) * 1978-10-18 1981-03-03 Beiersdorf Aktiengesellschaft Pharmaceutical tablet composition
EP0336014A1 (en) * 1988-04-08 1989-10-11 VECTORPHARMA INTERNATIONAL S.p.A. Pharmaceutical compositions with controlled release, and a method for their preparation
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Tomoyuki watanabe,et al.Prediction of apparent equilicrium solubility of indomethacincompounded with silica by 13C solid state NMR.Internation journal of pharmaceutics248.2002,248123-129. *
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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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Publication number Publication date
ES2390406T3 (es) 2012-11-12
EP2087883A1 (en) 2009-08-12
EP2087883B1 (en) 2012-07-25
GT200500045A (es) 2005-10-31
DK1765290T3 (da) 2009-11-02
AU2005221403B2 (en) 2009-12-10
JP5006185B2 (ja) 2012-08-22
PT1765290E (pt) 2009-11-23
ES2332229T3 (es) 2010-01-29
WO2005087199A3 (en) 2009-01-15
RS51076B (sr) 2010-10-31
IL177894A0 (en) 2006-12-31
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CN1984644A (zh) 2007-06-20
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