EA200601588A1 - Стабилизированные перенасыщенные твёрдые растворы липофильных лекарственных средств - Google Patents
Стабилизированные перенасыщенные твёрдые растворы липофильных лекарственных средствInfo
- Publication number
- EA200601588A1 EA200601588A1 EA200601588A EA200601588A EA200601588A1 EA 200601588 A1 EA200601588 A1 EA 200601588A1 EA 200601588 A EA200601588 A EA 200601588A EA 200601588 A EA200601588 A EA 200601588A EA 200601588 A1 EA200601588 A1 EA 200601588A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- lipofile
- medicines
- stabilized
- solid solutions
- substituted solid
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- 239000006104 solid solution Substances 0.000 title 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 abstract 4
- 238000004090 dissolution Methods 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 239000000377 silicon dioxide Substances 0.000 abstract 2
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 239000012736 aqueous medium Substances 0.000 abstract 1
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 abstract 1
- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 abstract 1
- 229960004845 drospirenone Drugs 0.000 abstract 1
- 229960004766 estradiol valerate Drugs 0.000 abstract 1
- -1 for example Chemical compound 0.000 abstract 1
- 229940088597 hormone Drugs 0.000 abstract 1
- 239000005556 hormone Substances 0.000 abstract 1
- 150000002634 lipophilic molecules Chemical class 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 150000003431 steroids Chemical class 0.000 abstract 1
Classifications
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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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Abstract
Данное изобретение касается фармацевтических композиций с улучшенным растворением липофильных действующих веществ в водной среде. Обнаружено, что фармацевтические композиции, содержащие порошок липофильных соединений, таких как гормоны и стероиды (например, дроспиренон и эстрадиола валерат) в молекулярно диспергированной форме вместе с носителем, определенная площадь поверхности которого составляет по крайней мере 250 м/г, таким как диоксид кремния, например, диоксид кремния, продаваемый под названием Aeroperl, имеют улучшенные свойства растворения липофильного действующего вещества.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US55133004P | 2004-03-10 | 2004-03-10 | |
EP04075714 | 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 |
---|---|
EA200601588A1 true EA200601588A1 (ru) | 2007-02-27 |
EA012746B1 EA012746B1 (ru) | 2009-12-30 |
Family
ID=34928105
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200601588A EA012746B1 (ru) | 2004-03-10 | 2005-03-10 | Порошкообразная композиция и способ ее получения, фармацевтическая лекарственная форма и способ ее получения, применение аморфного кремнезема |
Country Status (32)
Country | Link |
---|---|
US (1) | US8715735B2 (ru) |
EP (2) | EP2087883B1 (ru) |
JP (1) | JP5006185B2 (ru) |
KR (1) | KR101210695B1 (ru) |
CN (1) | CN1984644B (ru) |
AR (1) | AR048500A1 (ru) |
AT (1) | ATE442131T1 (ru) |
AU (1) | AU2005221403B8 (ru) |
BR (1) | BRPI0507342A (ru) |
CA (1) | CA2558582C (ru) |
CR (1) | CR8630A (ru) |
DE (1) | DE602005016551D1 (ru) |
DK (1) | DK1765290T3 (ru) |
EA (1) | EA012746B1 (ru) |
EC (1) | ECSP066902A (ru) |
ES (2) | ES2332229T3 (ru) |
GT (1) | GT200500045A (ru) |
HR (1) | HRP20090614T1 (ru) |
IL (1) | IL177894A0 (ru) |
MY (1) | MY142989A (ru) |
NO (1) | NO20064473L (ru) |
NZ (1) | NZ549793A (ru) |
PA (1) | PA8626101A1 (ru) |
PE (1) | PE20060016A1 (ru) |
PL (1) | PL1765290T3 (ru) |
PT (1) | PT1765290E (ru) |
RS (1) | RS51076B (ru) |
SI (1) | SI1765290T1 (ru) |
SV (1) | SV2005002044A (ru) |
TW (1) | TWI345986B (ru) |
UY (1) | UY28803A1 (ru) |
WO (1) | WO2005087199A2 (ru) |
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CA2516096A1 (en) | 2003-02-19 | 2004-09-02 | Lifecycle Pharma A/S | Use of a silica or silica derivative as a sorption material |
FR2851918B1 (fr) | 2003-03-06 | 2006-06-16 | Poudre impregnee ameliorant la biodisponibilite et/ou la solubilite et procede de fabrication | |
ATE476961T1 (de) | 2004-03-10 | 2010-08-15 | Bayer Schering Pharma Ag | Flüssige zusammensetzungen als mikroemulsionsvorkonzentrat mit molekular dispergiertem drospirenon |
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2005
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