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RU2015114540A - PARTICLES OF LEFG-FUSION DERIVATIVE PROPIONIC ACID FOR USE IN ORAL DOSED FORMS - Google Patents

PARTICLES OF LEFG-FUSION DERIVATIVE PROPIONIC ACID FOR USE IN ORAL DOSED FORMS Download PDF

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RU2015114540A
RU2015114540A RU2015114540A RU2015114540A RU2015114540A RU 2015114540 A RU2015114540 A RU 2015114540A RU 2015114540 A RU2015114540 A RU 2015114540A RU 2015114540 A RU2015114540 A RU 2015114540A RU 2015114540 A RU2015114540 A RU 2015114540A
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Prior art keywords
propionic acid
particles
wax
derivative
acid derivative
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RU2015114540A
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Russian (ru)
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Саумитра БАГЧИ
Мурали К. ВУППАЛА
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МакНЕЙЛ-ППС, ИНК.
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Priority claimed from US13/789,797 external-priority patent/US20140256810A1/en
Application filed by МакНЕЙЛ-ППС, ИНК. filed Critical МакНЕЙЛ-ППС, ИНК.
Publication of RU2015114540A publication Critical patent/RU2015114540A/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
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K9/141Intimate 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
    • A61K9/145Intimate 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 organic compounds
    • 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
    • A61K9/141Intimate 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
    • A61K9/148Intimate 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 compounds of unknown constitution, e.g. material from plants or animals
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Botany (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

1. Способ производства частиц производного пропионовой кислоты, включающий:плавление производного пропионовой кислоты и воска при перемешивании;диспергирование расплавленной смеси производного пропионовой кислоты/воска в горячей воде;перенос горячей дисперсии производного пропионовой кислоты/воска/горячей воды в другой контейнер, содержащий холодную воду, где диспергированные капли смеси производного пропионовой кислоты/воска застывают и образуют мелкодисперсные/сферические частицы; ифильтрование и сушку мелкодисперсных/сферических частиц.2. Способ по п. 1, в котором указанное производное пропионовой кислоты выбрано из группы, состоящей из ибупрофена, напроксена, беноксапрофена, напроксена натрия, флурбипрофена, фенопрофена, фенбупрофена, кетопрофена, индопрофена, пирпрофена, карпофена, оксапрофена, пранопрофена, микропрофена, тиоксапрофена, супропрофена, алминопрофена, тиапрофеновой кислоты, флупрофена и буклоксовой кислоты.3. Способ по п. 1, в котором указанный воск представляет собой глицерилбегенат.4. Способ производства дозированной формы, включающий:смешивание частиц производного пропионовой кислоты по п. 1 с эксципиентами дозированной формы; ипрессование смеси в дозированную форму.5. Частицы производного пропионовой кислоты, приготовленные способом по п. 1.6. Дозированная форма, приготовленная способом по п. 2.7. Способ лечения, включающий введение дозированной формы по п. 6.8. Фармацевтический состав с быстрым высвобождением, содержащий частицы производного пропионовой кислоты по п. 5.9. Фармацевтический состав с быстрым высвобождением по п. 8, причем указанный состав представляет собой жевательную таблетку.10.1. A method of manufacturing particles of a propionic acid derivative, comprising: melting a propionic acid derivative and wax with stirring; dispersing a molten propionic acid derivative / wax mixture in hot water; transferring the hot dispersion of the propionic acid derivative / wax / hot water to another container containing cold water where dispersed drops of a propionic acid / wax derivative mixture solidify and form finely divided / spherical particles; filtering and drying fine / spherical particles. 2. The method of claim 1, wherein said propionic acid derivative is selected from the group consisting of ibuprofen, naproxen, benoxaprofen, naproxen sodium, flurbiprofen, phenoprofen, fenbuprofen, ketoprofen, indoprofen, pirprofen, carpofen, oxaprofen, microprofenoprofenofenoprofenofenoprofenofenoprofenofenoprofenoprofenoprofenofenoprofenoprofenoprofenoprofenoprofenoprofenoprofenoprofen fenrofenoprofen fenrofenoprofen. , alminoprofen, thiaprofenic acid, fluprofen and bucloxic acid. 3. The method of claim 1, wherein said wax is glyceryl behenate. A method of manufacturing a dosage form, comprising: mixing particles of a derivative of propionic acid according to claim 1 with excipients of the dosage form; pressing the mixture into a dosage form. 5. Particles of the propionic acid derivative prepared by the method of claim 1.6. The dosage form prepared by the method according to p. 2.7. A method of treatment comprising administering a dosage form according to claim 6.8. A rapid release pharmaceutical composition comprising particles of a propionic acid derivative according to claim 5.9. The pharmaceutical composition with rapid release according to claim 8, wherein said composition is a chewable tablet.

Claims (12)

1. Способ производства частиц производного пропионовой кислоты, включающий:1. A method of manufacturing particles of a derivative of propionic acid, including: плавление производного пропионовой кислоты и воска при перемешивании;melting the propionic acid derivative and the wax with stirring; диспергирование расплавленной смеси производного пропионовой кислоты/воска в горячей воде;dispersing a molten propionic acid / wax derivative mixture in hot water; перенос горячей дисперсии производного пропионовой кислоты/воска/горячей воды в другой контейнер, содержащий холодную воду, где диспергированные капли смеси производного пропионовой кислоты/воска застывают и образуют мелкодисперсные/сферические частицы; иtransferring the hot dispersion of the propionic acid derivative / wax / hot water to another container containing cold water, where the dispersed drops of the propionic acid / wax derivative mixture solidify and form finely divided / spherical particles; and фильтрование и сушку мелкодисперсных/сферических частиц.filtering and drying fine / spherical particles. 2. Способ по п. 1, в котором указанное производное пропионовой кислоты выбрано из группы, состоящей из ибупрофена, напроксена, беноксапрофена, напроксена натрия, флурбипрофена, фенопрофена, фенбупрофена, кетопрофена, индопрофена, пирпрофена, карпофена, оксапрофена, пранопрофена, микропрофена, тиоксапрофена, супропрофена, алминопрофена, тиапрофеновой кислоты, флупрофена и буклоксовой кислоты.2. A method according to Claim. 1, wherein said propionic acid derivative is selected from the group consisting of ibuprofen, naproxen, benoxaprofen, naproxen sodium, flurbiprofen, fenoprofen, fenbuprofena, ketoprofen, indoprofen, pirprofen, karpofena, oksaprofena, pranoprofen, microprofiles, tioxaprofen suproprofen, alminoprofen, thiaprofenic acid, fluprofen and bucloxic acid. 3. Способ по п. 1, в котором указанный воск представляет собой глицерилбегенат.3. The method of claim 1, wherein said wax is glyceryl behenate. 4. Способ производства дозированной формы, включающий:4. A method of manufacturing a dosage form, including: смешивание частиц производного пропионовой кислоты по п. 1 с эксципиентами дозированной формы; иmixing particles of a propionic acid derivative according to claim 1 with dosage form excipients; and прессование смеси в дозированную форму.pressing the mixture into a dosage form. 5. Частицы производного пропионовой кислоты, приготовленные способом по п. 1.5. Particles of a derivative of propionic acid prepared by the method of claim 1. 6. Дозированная форма, приготовленная способом по п. 2.6. The dosage form prepared by the method according to p. 2. 7. Способ лечения, включающий введение дозированной формы по п. 6.7. A method of treatment comprising administering a dosage form according to claim 6. 8. Фармацевтический состав с быстрым высвобождением, содержащий частицы производного пропионовой кислоты по п. 5.8. The pharmaceutical composition with a quick release containing particles of a derivative of propionic acid according to claim 5. 9. Фармацевтический состав с быстрым высвобождением по п. 8, причем указанный состав представляет собой жевательную таблетку.9. The pharmaceutical composition with a quick release according to claim 8, wherein said composition is a chewable tablet. 10. Фармацевтический состав с быстрым высвобождением по п. 8, причем указанный состав представляет собой таблетку для рассасывания в полости рта.10. The pharmaceutical composition with a quick release according to claim 8, wherein said composition is a tablet for absorption in the oral cavity. 11. Фармацевтический состав с быстрым высвобождением по п. 8, в котором указанные частицы производного пропионовой кислоты содержат от приблизительно 80 частей производного пропионовой кислоты/приблизительно 20 частей воска до приблизительно 95 частей производного пропионовой кислоты/приблизительно 5 частей воска.11. The rapid release pharmaceutical composition of claim 8, wherein said particles of a propionic acid derivative comprise from about 80 parts of a propionic acid derivative / about 20 parts of a wax to about 95 parts of a propionic acid derivative / about 5 parts of a wax. 12. Фармацевтический состав с быстрым высвобождением по п. 9, в котором указанные частицы производного пропионовой кислоты содержат приблизительно 85 частей производного пропионовой кислоты/приблизительно 15 частей воска. 12. The rapid release pharmaceutical composition of claim 9, wherein said particles of the propionic acid derivative comprise about 85 parts of the propionic acid derivative / about 15 parts of the wax.
RU2015114540A 2012-09-18 2013-09-16 PARTICLES OF LEFG-FUSION DERIVATIVE PROPIONIC ACID FOR USE IN ORAL DOSED FORMS RU2015114540A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261702392P 2012-09-18 2012-09-18
US61/702,392 2012-09-18
US13/789,797 US20140256810A1 (en) 2013-03-08 2013-03-08 Low melting propionic acid derivative particles for use in oral dosage forms
US13/789,797 2013-03-08
PCT/US2013/059918 WO2014047001A1 (en) 2012-09-18 2013-09-16 Low melting propionic acid derivative particles for use in oral dosage forms

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RU2015114540A true RU2015114540A (en) 2016-11-10

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EP (1) EP2897584A1 (en)
CN (1) CN104640537A (en)
AU (1) AU2013318356A1 (en)
BR (1) BR112015005876A2 (en)
CA (1) CA2884119A1 (en)
HK (2) HK1209372A1 (en)
RU (1) RU2015114540A (en)
WO (1) WO2014047001A1 (en)

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CN109956860B (en) * 2019-03-08 2022-03-01 天津大学 A kind of preparation method of ibuprofen spherical crystal
CN116211807B (en) * 2019-11-25 2025-08-08 上海博志研新药物研究有限公司 Ibuprofen pharmaceutical composition, preparation method and application

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CN104640537A (en) 2015-05-20
EP2897584A1 (en) 2015-07-29
AU2013318356A1 (en) 2015-03-19
HK1212886A1 (en) 2016-06-24
BR112015005876A2 (en) 2017-07-04
WO2014047001A1 (en) 2014-03-27
CA2884119A1 (en) 2014-03-27
HK1209372A1 (en) 2016-04-01

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