RU2018121981A - PHARMACEUTICAL COMPOSITION - Google Patents

PHARMACEUTICAL COMPOSITION Download PDF

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Publication number
RU2018121981A
RU2018121981A RU2018121981A RU2018121981A RU2018121981A RU 2018121981 A RU2018121981 A RU 2018121981A RU 2018121981 A RU2018121981 A RU 2018121981A RU 2018121981 A RU2018121981 A RU 2018121981A RU 2018121981 A RU2018121981 A RU 2018121981A
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RU
Russia
Prior art keywords
composition according
polyoxyethylene
tocopheryl
phosphate
main surfactant
Prior art date
Application number
RU2018121981A
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Russian (ru)
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RU2742650C2 (en
RU2018121981A3 (en
Inventor
Махмуд ЭЛЬ-ТАМИМИ
Original Assignee
Фосфейдженикс Лимитед
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Priority claimed from AU2015905089A external-priority patent/AU2015905089A0/en
Application filed by Фосфейдженикс Лимитед filed Critical Фосфейдженикс Лимитед
Priority claimed from PCT/AU2016/051209 external-priority patent/WO2017096427A1/en
Publication of RU2018121981A publication Critical patent/RU2018121981A/en
Publication of RU2018121981A3 publication Critical patent/RU2018121981A3/ru
Application granted granted Critical
Publication of RU2742650C2 publication Critical patent/RU2742650C2/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Dispersion Chemistry (AREA)
  • Biochemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (10)

1. Состав, содержащий основное поверхностно-активное вещество, токолфосфат, воду, активный агент и, необязательно, масло, причем активный агент и/или, необязательно, масло содержится в гидрофобной фазе, при этом основное поверхностно-активное вещество присутствует в количестве в интервале от около 1% мас. до около 30% мас. от общего количества состава, при том, что токолфосфат представляет собой смесь моно(токоферил)фосфата и ди(токоферил)фосфата.1. The composition containing the main surfactant, tophosphate, water, an active agent and, optionally, oil, and the active agent and / or, optionally, oil is contained in a hydrophobic phase, while the main surfactant is present in an amount in the range of from about 1% wt. up to about 30% wt. of the total amount of the composition, despite the fact that tocolphosphate is a mixture of mono (tocopheryl) phosphate and di (tocopheryl) phosphate. 2. Состав по п. 1, отличающийся тем, что представляет собой эмульсию, необязательно, микроэмульсию или наноэмульсию.2. The composition according to p. 1, characterized in that it is an emulsion, optionally a microemulsion or nanoemulsion. 3. Состав по п. 1, отличающийся тем, что основное поверхностно-активное вещество представляет собой неионное, анионное, катионное или цвиттер-ионное поверхностно-активное вещество.3. The composition according to p. 1, characterized in that the main surfactant is a nonionic, anionic, cationic or zwitterionic surfactant. 4. Состав по п. 3, отличающийся тем, что основное поверхностно-активное вещество представляет собой неионное поверхностно-активное вещество, необязательно, выбранное из группы, состоящей из полиэтиленгликоля, пропиленгликоля, полиэтоксилированного касторового масла, гидрогенизированного касторового масла, 2-гидроксиэтил-12-гидроксиоктадеканоата, полиоксиэтиленмоноолеата, полиоксиэтиленмоностеарата, полиоксиэтиленмонолаурата, сорбитанмонолаурата, триэтаноламинолеата, полиоксиэтиленсорбитанмонолаурата, полиоксиэтиленсорбитанмонопальмитата, полиоксиэтиленсорбитанмоностеарата, полиоксиэтиленсорбитантристеарата, полиоксиэтиленсорбитанмоноолеата и полиоксиэтиленсорбитантриолеата.4. The composition according to p. 3, characterized in that the main surfactant is a non-ionic surfactant, optionally selected from the group consisting of polyethylene glycol, propylene glycol, polyethoxylated castor oil, hydrogenated castor oil, 2-hydroxyethyl-12 -hydroxy octadecanoate, polyoxyethylene monooleate, polyoxyethylene monostearate, polyoxyethylene monolaurate, sorbitan monolaurate, triethanolamine oleate, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan mono almitata, polyoxyethylene, polioksietilensorbitantristearata, polyoxyethylene sorbitan monooleate and polyoxyethylene. 5. Состав по п. 4, отличающийся тем, что основное поверхностно-актвиное вещество имеет величину ГЛБ от 8 до 18 или от 8 до 14, и, необязательно, основное поверхностно-активное вещество представляет собой полиоксиэтиленсорбитанмоноолеат.5. The composition according to p. 4, characterized in that the main surfactant has an HLB value of from 8 to 18 or from 8 to 14, and, optionally, the main surfactant is polyoxyethylene sorbitan monooleate. 6. Состав по п. 1, содержащий одно основное поверхностно-активное вещество или комбинацию основных поверхностно-активных веществ.6. The composition according to p. 1, containing one main surfactant or a combination of basic surfactants. 7. Состав по п. 1, отличающийся тем, что активный агент нерастворим в воде или плохо растворим в воде.7. The composition according to p. 1, characterized in that the active agent is insoluble in water or poorly soluble in water. 8. Состав по п. 1, отличающийся тем, что активный агент выбран из группы, состоящей из ампренавира, бексаротена, кальцитриола, клофазимина, циклоспорина, дигоксина, доксеркальциферола, дронабинола, дутастерида, этопозида, изотретиноина, итраконазола, лопинавира, ритонавира, лоратадина, нифедипина, нимодипина, фенобарбитала, прогестерона, рисперидона, саквинавира, сиролимуса, третиноина, вальпроевой кислоты, амиодарона НСl, хлордиазепоксида НСl, диазепама, дигидроэрготамина мезилата, фенолдопама, окситетрациклина, парикальцитола, пентобарбитала натрия, фенитоина натрия, фитонадиона, пропофола, зипрасидона мезилата, доцетаксела, этопозида, фулвестранта, галоперидола деканоата, лейпролида ацетата, виадура, лоразепама, паклитаксела, такролимуса, тенипозида, тестостерона энантата, тестостерона ципионата, эстрадиола ципионата и валрубицина.8. The composition according to p. 1, characterized in that the active agent is selected from the group consisting of amprenavir, bexarotene, calcitriol, clofazimine, cyclosporine, digoxin, doxercalciferol, dronabinol, dutasteride, etoposide, isotretinoin, itraconazole, lopinavira, riton nifedipine, nimodipine, phenobarbital, progesterone, risperidone, saquinavir, sirolimus, tretinoin, valproic acid, amiodarone HCl, chlordiazepoxide Hcl, diazepam, dihydroergotamine mesylate, phenoldopam, oxytetracycline, oxytetracycline tal sodium, phenytoin sodium, phytonadione, propofol, ziprasidone mesylate, docetaxel, etoposide, fulvestrant, haloperidol decanoate, leuprolide acetate, viadur, lorazepam, paclitaxel, tacrolimus, teniposide, testosterone enanthate cytateradiate cytosteridate cytosteridate cytosteridate cytosteridate teternadicate teteridate tibetanadibracytate. 9. Состав по п. 1, отличающийся тем, что гидрофобная фаза не содержит масло.9. The composition according to p. 1, characterized in that the hydrophobic phase does not contain oil. 10. Состав, содержащий 10 мг/мл пропофола, 20% полиоксиэтиленсорбитанмоноолеата, 0,05% раствора смеси моно(токоферил)фосфата и ди(токоферил)фосфата в этаноле и в необходимом количестве воды, или содержащий 10 мг/мл пропофола, 10% полиоксиэтиленсорбитанмоноолеата, 0,05% смеси моно(токоферил)фосфата и ди(токоферил)фосфата в этаноле и в необходимом количестве воды.10. Composition containing 10 mg / ml propofol, 20% polyoxyethylene sorbitan monooleate, 0.05% solution of a mixture of mono (tocopheryl) phosphate and di (tocopheryl) phosphate in ethanol and the required amount of water, or containing 10 mg / ml propofol, 10% polyoxyethylene sorbitan monooleate, 0.05% mixture of mono (tocopheryl) phosphate and di (tocopheryl) phosphate in ethanol and in the required amount of water.
RU2018121981A 2015-12-09 2016-12-09 Pharmaceutical composition RU2742650C2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
AU2015905089 2015-12-09
AU2015905089A AU2015905089A0 (en) 2015-12-09 Formulation
US201662329166P 2016-04-28 2016-04-28
US62/329,166 2016-04-28
PCT/AU2016/051209 WO2017096427A1 (en) 2015-12-09 2016-12-09 Pharmaceutical formulation

Publications (3)

Publication Number Publication Date
RU2018121981A true RU2018121981A (en) 2020-01-09
RU2018121981A3 RU2018121981A3 (en) 2020-03-24
RU2742650C2 RU2742650C2 (en) 2021-02-09

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Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9903547D0 (en) * 1999-02-16 1999-04-07 Novartis Ag Organic compounds
KR100612398B1 (en) * 2000-11-14 2006-08-16 바이탈 헬스 사이언시즈 피티와이 리미티드 Complexes of phosphate derivatives
KR100394770B1 (en) * 2001-06-05 2003-08-14 주식회사 태평양 Stabilization method of nano-emulsion using tocopheryl derivatives and external application for skin containing the stabilized nano-emulsion
KR20070005617A (en) * 2004-02-13 2007-01-10 바이오어베일러빌리티, 아이엔씨. A microemulsion preparation of high concentration propofol for anesthetic uses
JP4847437B2 (en) * 2004-03-03 2011-12-28 バイタル ヘルス サイエンシズ プロプライアタリー リミティド Alkaloid preparation
CA2671495A1 (en) * 2006-12-05 2008-06-19 Novartis Ag Microemulsion dosage forms of valsartan and methods of making the same
WO2011075775A1 (en) * 2009-12-23 2011-06-30 Phosphagenics Limited Carrier composition

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RU2742650C2 (en) 2021-02-09
KR20190032265A (en) 2019-03-27
RU2018121981A3 (en) 2020-03-24

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