RU2010146697A - Способ получения фармацевтической композиции - Google Patents
Способ получения фармацевтической композиции Download PDFInfo
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- RU2010146697A RU2010146697A RU2010146697/15A RU2010146697A RU2010146697A RU 2010146697 A RU2010146697 A RU 2010146697A RU 2010146697/15 A RU2010146697/15 A RU 2010146697/15A RU 2010146697 A RU2010146697 A RU 2010146697A RU 2010146697 A RU2010146697 A RU 2010146697A
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- receptor agonist
- sugar alcohol
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 3
- 238000004519 manufacturing process Methods 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract 27
- 239000000203 mixture Substances 0.000 claims abstract 20
- 238000002156 mixing Methods 0.000 claims abstract 16
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims abstract 11
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims abstract 11
- 239000000018 receptor agonist Substances 0.000 claims abstract 11
- 229940044601 receptor agonist Drugs 0.000 claims abstract 11
- 150000005846 sugar alcohols Chemical class 0.000 claims abstract 11
- 239000011230 binding agent Substances 0.000 claims abstract 7
- 238000004513 sizing Methods 0.000 claims abstract 6
- 238000007580 dry-mixing Methods 0.000 claims abstract 4
- 238000000227 grinding Methods 0.000 claims abstract 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract 3
- 239000003795 chemical substances by application Substances 0.000 claims abstract 2
- 238000005469 granulation Methods 0.000 claims abstract 2
- 230000003179 granulation Effects 0.000 claims abstract 2
- 238000001035 drying Methods 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
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- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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- 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
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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Abstract
1. Способ получения фармацевтической композиции, заключающийся в том, что: ! (а) смешивают агонист рецептора S1P с сахарным спиртом; ! (б) размалывают и/или гранулируют смесь, полученную на стадии (а); и ! (в) смешивают размолотую и/или гранулированную смесь, полученную на стадии (б), с замасливателем. ! 2. Способ по п.1, в котором агонист рецептора S1P тонко измельчают и/или предварительно просеивают до стадии (а). ! 3. Способ по п.1 или 2, где стадия смешения (а) включает перемешение агониста рецептора S1P и сахарного спирта в любом пригодном смесителе или миксере в течение, например 100-400 оборотов. ! 4. Способ по п.1 или 2, в котором компоненты смешивают путем сухого смешения. ! 5. Способ по п.4, где стадия смешения (б) предусматривает пропуск полученной на стадии (а) смеси через сито. ! 6. Способ по п.1 или 2, при котором на стадии (а) осуществляют стадию смешения всего количества агониста рецептора S1P сначала с небольшим количеством сахарного спирта для приготовления премикса. ! 7. Способ по п.6, в котором премикс, получаемый на стадии (а) содержит от 5 до 25 мас.% от общей массы сахарного спирта. ! 8. Способ по п.1 или 2, при котором стадия (а) также включает стадию добавления к смеси раствора связующего вещества. ! 9. Способ по п.8, при котором связующее вещество добавляют к смеси в сухом виде и на стадии грануляции добавляют воду. ! 10. Способ по п.1 или 2, в котором размолотую смесь, полученную на стадии (б), перемешивают перед смешением с замасливателем. ! 11. Способ по п.1 или 2, при котором перед смешением замасливатель просеивают. ! 12. Способ по п.10, при котором на стадии (в) к смеси, полученной на стадии (б), добавляют дополнительное количество связующего вещес
Claims (15)
1. Способ получения фармацевтической композиции, заключающийся в том, что:
(а) смешивают агонист рецептора S1P с сахарным спиртом;
(б) размалывают и/или гранулируют смесь, полученную на стадии (а); и
(в) смешивают размолотую и/или гранулированную смесь, полученную на стадии (б), с замасливателем.
2. Способ по п.1, в котором агонист рецептора S1P тонко измельчают и/или предварительно просеивают до стадии (а).
3. Способ по п.1 или 2, где стадия смешения (а) включает перемешение агониста рецептора S1P и сахарного спирта в любом пригодном смесителе или миксере в течение, например 100-400 оборотов.
4. Способ по п.1 или 2, в котором компоненты смешивают путем сухого смешения.
5. Способ по п.4, где стадия смешения (б) предусматривает пропуск полученной на стадии (а) смеси через сито.
6. Способ по п.1 или 2, при котором на стадии (а) осуществляют стадию смешения всего количества агониста рецептора S1P сначала с небольшим количеством сахарного спирта для приготовления премикса.
7. Способ по п.6, в котором премикс, получаемый на стадии (а) содержит от 5 до 25 мас.% от общей массы сахарного спирта.
8. Способ по п.1 или 2, при котором стадия (а) также включает стадию добавления к смеси раствора связующего вещества.
9. Способ по п.8, при котором связующее вещество добавляют к смеси в сухом виде и на стадии грануляции добавляют воду.
10. Способ по п.1 или 2, в котором размолотую смесь, полученную на стадии (б), перемешивают перед смешением с замасливателем.
11. Способ по п.1 или 2, при котором перед смешением замасливатель просеивают.
12. Способ по п.10, при котором на стадии (в) к смеси, полученной на стадии (б), добавляют дополнительное количество связующего вещества.
13. Способ по п.1 или 2, включающий стадии
(а) сухое перемешивание агониста рецептора S1P с сахарным спиртом;
(б) сухое перемешивание полученной смеси агониста рецептора S1P с сахарным спиртом со связующим веществом;
(в) добавление воды;
(б) гранулирование смеси; и
(в) сушки и перемалывания гранулята.
14. Способ по п.1 или 2, при котором композиция содержит от 0,01 до 20% мас.% агониста рецептора S1P в пересчете на общую массу композиции.
15. Способ по п.1 или 2, при котором композиция содержит 75-99,99 мас.% сахарного спирта в перечете на общую массу композиции.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46121503P | 2003-04-08 | 2003-04-08 | |
| US60/461,215 | 2003-04-08 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009105403/15A Division RU2009105403A (ru) | 2003-04-08 | 2009-02-17 | Твердая фармацевтическая композиция для перорального введения (варианты) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2010146697A true RU2010146697A (ru) | 2012-05-27 |
| RU2475236C2 RU2475236C2 (ru) | 2013-02-20 |
Family
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Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005134173/15A RU2358716C2 (ru) | 2003-04-08 | 2004-04-06 | Органические соединения |
| RU2009105403/15A RU2009105403A (ru) | 2003-04-08 | 2009-02-17 | Твердая фармацевтическая композиция для перорального введения (варианты) |
| RU2010146697/15A RU2475236C2 (ru) | 2003-04-08 | 2010-11-17 | Способ получения фармацевтической композиции |
| RU2010147000/15A RU2475237C2 (ru) | 2003-04-08 | 2010-11-18 | Предназначенная для перорального применения фармацевтическая композиция |
| RU2012148593/15A RU2012148593A (ru) | 2003-04-08 | 2012-11-15 | Предназначенная для перорального применения фармацевтическая композиция |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005134173/15A RU2358716C2 (ru) | 2003-04-08 | 2004-04-06 | Органические соединения |
| RU2009105403/15A RU2009105403A (ru) | 2003-04-08 | 2009-02-17 | Твердая фармацевтическая композиция для перорального введения (варианты) |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2010147000/15A RU2475237C2 (ru) | 2003-04-08 | 2010-11-18 | Предназначенная для перорального применения фармацевтическая композиция |
| RU2012148593/15A RU2012148593A (ru) | 2003-04-08 | 2012-11-15 | Предназначенная для перорального применения фармацевтическая композиция |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1773307T3 (pl) * | 2004-07-30 | 2015-03-31 | Novartis Ag | Preparaty 2-amino-1,3-propanodioli i ich analogów |
| CN1891212B (zh) * | 2005-07-07 | 2010-10-13 | 马启明 | 一种口服制剂及其制备方法 |
| NZ566137A (en) * | 2005-09-09 | 2011-05-27 | Novartis Ag | The use of diphenyl thioether derivatives to treat autoimmune diseases |
| EP2623113B1 (en) | 2005-11-09 | 2017-05-31 | Onyx Therapeutics, Inc. | Compound for enzyme inhibition |
| TWI389683B (zh) | 2006-02-06 | 2013-03-21 | Kyorin Seiyaku Kk | A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient |
| NZ597545A (en) | 2006-06-19 | 2013-07-26 | Proteolix Inc | Peptide epoxyketones for proteasome inhibition |
| GB0612721D0 (en) | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
| RU2487703C2 (ru) * | 2006-09-26 | 2013-07-20 | Новартис Аг | Фармацевтические композиции, включающие модулятор s1р |
| EP1905434A1 (en) * | 2006-09-26 | 2008-04-02 | Novartis AG | Organic compounds comprising an S1P receptor agonist and their therapeutic use |
| EP1923054A1 (en) * | 2006-09-26 | 2008-05-21 | Novartis AG | Fast disintegrating pharmaceutical composition comprising an S1P agonist or modulator |
| EP1923055A1 (en) * | 2006-09-26 | 2008-05-21 | Novartis AG | Freeze-dried pharmaceutical composition comprising an S1P agonist or modulator |
| AU2011235934A1 (en) * | 2006-09-26 | 2011-11-03 | Novartis Ag | Pharmaceutical compositions comprising an S1P modulator |
| EP1923058A1 (en) * | 2006-09-26 | 2008-05-21 | Novartis AG | Coated pharmaceutical composition comprising an S1P agonist or modulator |
| WO2008124210A1 (en) * | 2007-02-14 | 2008-10-16 | Emory University | Methods and compositions for treating or preventing infection using leukocyte sequestration agents |
| FI2140867T4 (fi) | 2007-03-29 | 2023-09-14 | Farmaseuttinen koostumus | |
| CA2701778C (en) | 2007-10-04 | 2018-09-11 | Onyx Therapeutics, Inc. | Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides |
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