RU2005105301A - Парентеральные композиции, содержащие гидроксиэфиры рапамицина - Google Patents
Парентеральные композиции, содержащие гидроксиэфиры рапамицина Download PDFInfo
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- RU2005105301A RU2005105301A RU2005105301/15A RU2005105301A RU2005105301A RU 2005105301 A RU2005105301 A RU 2005105301A RU 2005105301/15 A RU2005105301/15 A RU 2005105301/15A RU 2005105301 A RU2005105301 A RU 2005105301A RU 2005105301 A RU2005105301 A RU 2005105301A
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- solvent
- polyethylene glycol
- cci
- composition
- polysorbate
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- 239000000203 mixture Substances 0.000 title claims 16
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 title 1
- 229960002930 sirolimus Drugs 0.000 title 1
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 24
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 21
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 21
- 239000002904 solvent Substances 0.000 claims 20
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 14
- 229960000235 temsirolimus Drugs 0.000 claims 14
- 239000012141 concentrate Substances 0.000 claims 13
- 239000006184 cosolvent Substances 0.000 claims 13
- 239000003963 antioxidant agent Substances 0.000 claims 12
- 230000003078 antioxidant effect Effects 0.000 claims 12
- 235000006708 antioxidants Nutrition 0.000 claims 12
- 238000000034 method Methods 0.000 claims 9
- 229940068918 polyethylene glycol 400 Drugs 0.000 claims 9
- 239000004094 surface-active agent Substances 0.000 claims 9
- 229960004063 propylene glycol Drugs 0.000 claims 8
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 6
- 229920001213 Polysorbate 20 Polymers 0.000 claims 6
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 6
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 6
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 6
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 6
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 6
- 229940068977 polysorbate 20 Drugs 0.000 claims 6
- 229920000053 polysorbate 80 Polymers 0.000 claims 6
- 229940068968 polysorbate 80 Drugs 0.000 claims 6
- 229940087168 alpha tocopherol Drugs 0.000 claims 5
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 5
- 229960004756 ethanol Drugs 0.000 claims 5
- 229940113116 polyethylene glycol 1000 Drugs 0.000 claims 5
- 229940068886 polyethylene glycol 300 Drugs 0.000 claims 5
- 229940057847 polyethylene glycol 600 Drugs 0.000 claims 5
- 229960000984 tocofersolan Drugs 0.000 claims 5
- 239000002076 α-tocopherol Substances 0.000 claims 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims 3
- 235000010323 ascorbic acid Nutrition 0.000 claims 3
- 239000011668 ascorbic acid Substances 0.000 claims 3
- 229960005070 ascorbic acid Drugs 0.000 claims 3
- 238000007865 diluting Methods 0.000 claims 3
- PJUIMOJAAPLTRJ-UHFFFAOYSA-N monothioglycerol Chemical compound OCC(O)CS PJUIMOJAAPLTRJ-UHFFFAOYSA-N 0.000 claims 3
- 239000000473 propyl gallate Substances 0.000 claims 3
- 235000010388 propyl gallate Nutrition 0.000 claims 3
- 229940075579 propyl gallate Drugs 0.000 claims 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims 2
- 239000004471 Glycine Substances 0.000 claims 2
- 229930003427 Vitamin E Natural products 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- 229920001400 block copolymer Polymers 0.000 claims 2
- POODVSCQKVCWCE-UHFFFAOYSA-N butanedioic acid;propane-1,2-diol Chemical compound CC(O)CO.OC(=O)CCC(O)=O POODVSCQKVCWCE-UHFFFAOYSA-N 0.000 claims 2
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 2
- 239000000787 lecithin Substances 0.000 claims 2
- 235000010445 lecithin Nutrition 0.000 claims 2
- 229940067606 lecithin Drugs 0.000 claims 2
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims 2
- 235000015112 vegetable and seed oil Nutrition 0.000 claims 2
- 239000008158 vegetable oil Substances 0.000 claims 2
- 239000011709 vitamin E Substances 0.000 claims 2
- 229940046009 vitamin E Drugs 0.000 claims 2
- 235000019165 vitamin E Nutrition 0.000 claims 2
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical group CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 1
- 239000012895 dilution Substances 0.000 claims 1
- 238000010790 dilution Methods 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000011732 tocopherol Substances 0.000 claims 1
- 229930003799 tocopherol Natural products 0.000 claims 1
- 235000010384 tocopherol Nutrition 0.000 claims 1
- 229960001295 tocopherol Drugs 0.000 claims 1
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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- 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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Claims (30)
1. Концентрат сорастворителя и CCI-779, который включает CCI-779, растворитель, приемлемый для парентерального применения, и антиоксидантный компонент.
2. Концентрат сорастворителя по п. 1, где растворителем, приемлемым для парентерального применения, является диметилацетамид.
3. Концентрат сорастворителя по п. 1, где растворителем, приемлемым для парентерального применения, является спиртовой растворитель.
4. Концентрат сорастворителя по п. 3, где спиртовой растворитель включает этанол, пропиленгликоль, полиэтиленгликоль 300, полиэтиленгликоль 400, полиэтиленгликоль 600 или полиэтиленгликоль 1000.
5. Концентрат сорастворителя по любому из пп. 1-4, где антиоксидантный компонент включает лимонную кислоту, глицин, d,1--токоферол, BHA, BHT, монотиоглицерин, аскорбиновую кислоту или пропилгаллат.
6. Концентрат сорастворителя и CCI-779 по п.1, который включает CCI-779, лимонную кислоту и дегидратированный этанол.
7. Концентрат сорастворителя и CCI-779 по п.1, который включает CCI-779, дегидратированный этанол, d,1-α-токоферол и пропиленгликоль.
8. Концентрат сорастворителя по п. 7, который дополнительно включает лимонную кислоту.
9. Концентрат сорастворителя по п.1, где CCI-779 составляет от около 0,05 мг/мл до около 50 мг/мл.
10. Концентрат сорастворителя по п.1, где CCI-779 составляет от около 25 мг/мл.
11. Концентрат сорастворителя по п.1, где антиоксидант составляет от около 0,001% до 1,0% мас./об.
12. Парентеральная композиция, которая включает CCI-779, спиртовой растворитель, антиоксидант, разбавляющий растворитель и поверхностно-активное вещество.
13. Композиция по п.12, где спиртовым растворителем является этанол, пропиленгликоль, полиэтиленгликоль 300, полиэтиленгликоль 400, полиэтиленгликоль 600 или полиэтиленгликоль 1000.
14. Композиция по п.12 или 13, где антиоксидантом является лимонная кислота, глицин, d,1-α-токоферол, BHA, BHT, монотиоглицерин, аскорбиновая кислота или пропилгаллат.
15. Композиция по п.12, где разбавляющим растворителем является вода, этанол, полиэтиленгликоль 300, полиэтиленгликоль 400, полиэтиленгликоль 600, полиэтиленгликоль 1000 или пропиленгликоль.
16. Композиция по по п.12, где поверхностно-активным веществом является полисорбат 20, полисорбат 80, желчная кислота, лецитин, этоксилированное растительное масло, пропиленгликольсукцинат токоферола витамина Е или блоксополимеры полиоксиэтилена-полиоксипропилена.
17. Композиция по по п.12, где CCI-779 составляет от около 1 мг/мл до около 25 мг/мл.
18. Композиция по по п.12, где CCI-779 составляет от около 2,5 мг/мл до около 10 мг/мл.
19. Композиция по п.12, где антиоксидант составляет от около 0,0005% мас./об. до около 0,5% мас./об. композиции.
20. Композиция по п.12, где поверхностно-активное вещество составляет от около 0,5% мас./об. до около 10% мас./об. композиции.
21. Композиция по по п.12, где растворитель составляет от около 10% мас./об. до около 90% мас./об. композиции.
22. Способ получения парентеральной композиции CCI-779, который включает:
(а) смешивание CCI-779 с растворителем, приемлемым для парентерального применения, и антиоксидантным компонентом для получения концентрата сорастворителя;
(b) смешивание разбавляющего раствора и поверхностно-активного вещества для получения разбавителя; и
(с) смешивание концентрата сорастворителя с разбавителем для получения парентеральной композиции CCI-779.
23. Способ по п.22, где растворителем является спиртовой растворитель, включающий этанол, пропиленгликоль, полиэтиленгликоль 300, полиэтиленгликоль 400, полиэтиленгликоль 600 или полиэтиленгликоль 1000.
24. Способ по п.22 или 23, где антиоксидантный компонент включает лимонную кислоту, d,1-α-токоферол, BHA, BHT, монотиоглицерин, аскорбиновую кислоту или пропилгаллат.
25. Способ по п.22, где разбавляющим растворителем является вода, этанол, полиэтиленгликоль 300, полиэтиленгликоль 400, полиэтиленгликоль 600, полиэтиленгликоль 1000 или пропиленгликоль.
26. Способ по п.22, где поверхностно-активным веществом является полисорбат 20, полисорбат 80, желчная кислота, лецитин, этоксилированное растительное масло, пропиленгликольсукцинат токоферола витамина Е или блок-сополимеры полиоксиэтилена-полиоксипропилена.
27. Способ по п.22, где растворителем является дегидратированный этанол, антиоксидантом является лимонная кислота, разбавляющими растворителями являются вода и полиэтиленгликоль 400 и поверхностно-активным веществом является полисорбат 20 или полисорбат 80.
28. Способ по п.22, где растворителем является дегидратированный этанол, антиоксидантом является лимонная кислота, разбавляющими растворителями являются дегидратированный этанол и полиэтиленгликоль 400 и поверхностно-активным веществом является полисорбат 20 или полисорбат 80.
29. Способ по п.22, где растворителями являются дегидратированный этанол и пропиленгликоль, антиоксидантом является d,1-α-токоферол, разбавляющими растворителями являются вода и полиэтиленгликоль 400 и поверхностно-активным веществом является полисорбат 20 или полисорбат 80.
30. Способ по п.22, где растворителями являются дегидратированный этанол и пропиленгликоль, антиоксидантом является d,1-α-токоферол, разбавляющими растворителями являются дегидратированный этанол и полиэтиленгликоль 400, и поверхностно-активным веществом является полисорбат 20 или полисорбат 80.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39952602P | 2002-07-30 | 2002-07-30 | |
| US60/399,526 | 2002-07-30 |
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| RU2005105301A true RU2005105301A (ru) | 2005-09-10 |
| RU2344821C2 RU2344821C2 (ru) | 2009-01-27 |
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| RU2005105301/15A RU2344821C2 (ru) | 2002-07-30 | 2003-07-25 | Парентеральные композиции, содержащие гидроксиэфиры рапамицина |
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| AT (1) | ATE385795T1 (ru) |
| AU (2) | AU2003254168A1 (ru) |
| BR (1) | BR0313024A (ru) |
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| RU (1) | RU2344821C2 (ru) |
| SI (1) | SI1553940T1 (ru) |
| TW (1) | TWI307277B (ru) |
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-
2003
- 2003-07-25 TW TW092120393A patent/TWI307277B/zh not_active IP Right Cessation
- 2003-07-25 ES ES03771828T patent/ES2300622T3/es not_active Expired - Lifetime
- 2003-07-25 CN CNB038179199A patent/CN100402031C/zh not_active Expired - Lifetime
- 2003-07-25 PT PT03771828T patent/PT1553940E/pt unknown
- 2003-07-25 DK DK03771828T patent/DK1553940T3/da active
- 2003-07-25 AR AR20030102681A patent/AR040693A1/es not_active Application Discontinuation
- 2003-07-25 WO PCT/US2003/023276 patent/WO2004011000A1/en not_active Ceased
- 2003-07-25 KR KR1020057001505A patent/KR101131794B1/ko not_active Expired - Lifetime
- 2003-07-25 CA CA2493878A patent/CA2493878C/en not_active Expired - Lifetime
- 2003-07-25 RU RU2005105301/15A patent/RU2344821C2/ru active
- 2003-07-25 MX MXPA05001013A patent/MXPA05001013A/es active IP Right Grant
- 2003-07-25 UA UAA200501758A patent/UA82328C2/ru unknown
- 2003-07-25 AT AT03771828T patent/ATE385795T1/de not_active IP Right Cessation
- 2003-07-25 BR BR0313024-0A patent/BR0313024A/pt not_active Application Discontinuation
- 2003-07-25 SI SI200331190T patent/SI1553940T1/sl unknown
- 2003-07-25 US US10/626,943 patent/US8026276B2/en not_active Expired - Lifetime
- 2003-07-25 DE DE60319118T patent/DE60319118T2/de not_active Expired - Lifetime
- 2003-07-25 EP EP03771828A patent/EP1553940B1/en not_active Revoked
- 2003-07-25 NZ NZ537829A patent/NZ537829A/en unknown
- 2003-07-25 JP JP2004524806A patent/JP2005537285A/ja not_active Withdrawn
- 2003-07-25 AU AU2003254168A patent/AU2003254168A1/en not_active Abandoned
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2004
- 2004-12-26 IL IL166003A patent/IL166003A/en active IP Right Grant
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2005
- 2005-01-11 CR CR7647A patent/CR7647A/es not_active Application Discontinuation
- 2005-01-26 NO NO20050455A patent/NO20050455L/no not_active Application Discontinuation
- 2005-01-27 ZA ZA200500831A patent/ZA200500831B/en unknown
- 2005-02-23 CO CO05017056A patent/CO5700745A2/es not_active Application Discontinuation
- 2005-02-24 EC EC2005005628A patent/ECSP055628A/es unknown
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2010
- 2010-03-01 AU AU2010200761A patent/AU2010200761B2/en not_active Expired
- 2010-05-06 JP JP2010106707A patent/JP5345105B2/ja not_active Expired - Lifetime
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2011
- 2011-08-10 US US13/206,641 patent/US8299116B2/en not_active Expired - Fee Related
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2012
- 2012-10-15 US US13/651,623 patent/US8455539B2/en not_active Expired - Fee Related
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2013
- 2013-04-04 AR ARP130101103A patent/AR090603A2/es not_active Application Discontinuation
- 2013-05-13 US US13/892,389 patent/US8722700B2/en not_active Expired - Lifetime
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