RU2012148593A - Предназначенная для перорального применения фармацевтическая композиция - Google Patents
Предназначенная для перорального применения фармацевтическая композиция Download PDFInfo
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- RU2012148593A RU2012148593A RU2012148593/15A RU2012148593A RU2012148593A RU 2012148593 A RU2012148593 A RU 2012148593A RU 2012148593/15 A RU2012148593/15 A RU 2012148593/15A RU 2012148593 A RU2012148593 A RU 2012148593A RU 2012148593 A RU2012148593 A RU 2012148593A
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- mannitol
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 3
- 239000000203 mixture Substances 0.000 claims abstract 34
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims abstract 16
- 229930195725 Mannitol Natural products 0.000 claims abstract 16
- 239000000594 mannitol Substances 0.000 claims abstract 16
- 235000010355 mannitol Nutrition 0.000 claims abstract 16
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims abstract 12
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims abstract 12
- 239000000018 receptor agonist Substances 0.000 claims abstract 12
- 229940044601 receptor agonist Drugs 0.000 claims abstract 12
- 229960001855 mannitol Drugs 0.000 claims abstract 9
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims abstract 4
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical group CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims abstract 4
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims abstract 4
- 239000002245 particle Substances 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 239000000811 xylitol Substances 0.000 claims abstract 4
- 235000010447 xylitol Nutrition 0.000 claims abstract 4
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract 4
- 229960002675 xylitol Drugs 0.000 claims abstract 4
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910019142 PO4 Inorganic materials 0.000 claims abstract 2
- 239000002552 dosage form Substances 0.000 claims abstract 2
- SWZTYAVBMYWFGS-UHFFFAOYSA-N fingolimod hydrochloride Chemical group Cl.CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 SWZTYAVBMYWFGS-UHFFFAOYSA-N 0.000 claims abstract 2
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 claims abstract 2
- 229960000367 inositol Drugs 0.000 claims abstract 2
- 239000000832 lactitol Substances 0.000 claims abstract 2
- 235000010448 lactitol Nutrition 0.000 claims abstract 2
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims abstract 2
- 229960003451 lactitol Drugs 0.000 claims abstract 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims abstract 2
- 239000010452 phosphate Substances 0.000 claims abstract 2
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 claims abstract 2
- 238000004513 sizing Methods 0.000 claims abstract 2
- 239000007909 solid dosage form Substances 0.000 claims abstract 2
- 239000007921 spray Substances 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 206010047470 viral myocarditis Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
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Abstract
1. Фармацевтическая композиция, пригодная для перорального введения, которая содержит:(а) агонист рецептора S1P; и(б) маннит,причем эта композиция представляет собой твердую дозированную форму, маннит обладает большой площадью специфической поверхности, а агонист рецептора S1P выбирают из 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диола 10 (FTY720), его фармацевтически приемлемой соли и FTY20-фосфата.2. Композиция по п.1, в которой агонист рецептора S1P представляет собой 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диол или его фармацевтически приемлемые соли.3. Композиция по п.1, в которой агонист рецептора S1P представляет собой гидрохлорид 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диола.4. Композиция по любому из предшествующих пунктов, в которой маннит приготавливают из высушенной распылением композиции.5. Композиция по п.1 или 2, в которой маннит имеет средний размер частиц от 100 до 300 мкм или от 150 до 250 мкм.6. Композиция по п.1 или 2, в которой маннит имеет насыпную плотность от 0,4 до 0,6 г/мл или от 0,45 до 0,55 г/мл.7. Композиция по п.1 или 2, в которой маннит имеет удельную площадь поверхности одной частицы от 1 до 7 м/г.8. Композиция по п.1 или 2, в которой композиция дополнительно включает маннит, инозит, ксилит или лактит, например дополнительно включает ксилит.9. Композиция по п.1 или 2, в которой агонист рецептора S1P является измельченным и/или является предварительно просеянным.10. Композиция по п.1 или 2, дополнительно содержащая замасливатель.11. Композиция по п.10, содержащая от 0,01 до 20 мас.% агониста рецептора S1P.12. Композиция по п.1 или 2, содержащая от 90 до 99,5 мас.% маннита.13. Композиция по п.1 или 2, где композиция представляет собой единичную дозированную форму и с
Claims (15)
1. Фармацевтическая композиция, пригодная для перорального введения, которая содержит:
(а) агонист рецептора S1P; и
(б) маннит,
причем эта композиция представляет собой твердую дозированную форму, маннит обладает большой площадью специфической поверхности, а агонист рецептора S1P выбирают из 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диола 10 (FTY720), его фармацевтически приемлемой соли и FTY20-фосфата.
2. Композиция по п.1, в которой агонист рецептора S1P представляет собой 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диол или его фармацевтически приемлемые соли.
3. Композиция по п.1, в которой агонист рецептора S1P представляет собой гидрохлорид 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диола.
4. Композиция по любому из предшествующих пунктов, в которой маннит приготавливают из высушенной распылением композиции.
5. Композиция по п.1 или 2, в которой маннит имеет средний размер частиц от 100 до 300 мкм или от 150 до 250 мкм.
6. Композиция по п.1 или 2, в которой маннит имеет насыпную плотность от 0,4 до 0,6 г/мл или от 0,45 до 0,55 г/мл.
7. Композиция по п.1 или 2, в которой маннит имеет удельную площадь поверхности одной частицы от 1 до 7 м2/г.
8. Композиция по п.1 или 2, в которой композиция дополнительно включает маннит, инозит, ксилит или лактит, например дополнительно включает ксилит.
9. Композиция по п.1 или 2, в которой агонист рецептора S1P является измельченным и/или является предварительно просеянным.
10. Композиция по п.1 или 2, дополнительно содержащая замасливатель.
11. Композиция по п.10, содержащая от 0,01 до 20 мас.% агониста рецептора S1P.
12. Композиция по п.1 или 2, содержащая от 90 до 99,5 мас.% маннита.
13. Композиция по п.1 или 2, где композиция представляет собой единичную дозированную форму и содержит 0,5 до 10 мг агониста рецептора S1P.
14. Композиция по п.1 или 2, используемая в способе лечения и предупреждения отторжения трансплантата органа или ткани, или лечения аутоиммунного заболевания или воспалительных состояний, вирусного миокардита или вирусных заболеваний, связанных с вирусным миокардитом, или рассеянного склероза.
15. Композиция по п.14, используемая в способе лечения рассеянного склероза.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46121503P | 2003-04-08 | 2003-04-08 | |
| US60/461,215 | 2003-04-08 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2010147000/15A Division RU2475237C2 (ru) | 2003-04-08 | 2010-11-18 | Предназначенная для перорального применения фармацевтическая композиция |
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| Publication Number | Publication Date |
|---|---|
| RU2012148593A true RU2012148593A (ru) | 2014-05-20 |
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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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| 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 |
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