RU2017139767A - Концентрированные терапевтические фосфолипидные композиции - Google Patents
Концентрированные терапевтические фосфолипидные композиции Download PDFInfo
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- RU2017139767A RU2017139767A RU2017139767A RU2017139767A RU2017139767A RU 2017139767 A RU2017139767 A RU 2017139767A RU 2017139767 A RU2017139767 A RU 2017139767A RU 2017139767 A RU2017139767 A RU 2017139767A RU 2017139767 A RU2017139767 A RU 2017139767A
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- 239000000203 mixture Substances 0.000 title claims 52
- 150000003904 phospholipids Chemical class 0.000 title claims 25
- 230000001225 therapeutic effect Effects 0.000 title claims 5
- -1 phospholipid compounds Chemical class 0.000 claims 13
- JAZBEHYOTPTENJ-JLNKQSITSA-N all-cis-5,8,11,14,17-icosapentaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 claims 12
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims 12
- 235000020673 eicosapentaenoic acid Nutrition 0.000 claims 12
- 229960005135 eicosapentaenoic acid Drugs 0.000 claims 12
- JAZBEHYOTPTENJ-UHFFFAOYSA-N eicosapentaenoic acid Natural products CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O JAZBEHYOTPTENJ-UHFFFAOYSA-N 0.000 claims 12
- 235000020669 docosahexaenoic acid Nutrition 0.000 claims 9
- 150000003626 triacylglycerols Chemical class 0.000 claims 9
- 239000002775 capsule Substances 0.000 claims 6
- 229940090949 docosahexaenoic acid Drugs 0.000 claims 6
- DVSZKTAMJJTWFG-SKCDLICFSA-N (2e,4e,6e,8e,10e,12e)-docosa-2,4,6,8,10,12-hexaenoic acid Chemical compound CCCCCCCCC\C=C\C=C\C=C\C=C\C=C\C=C\C(O)=O DVSZKTAMJJTWFG-SKCDLICFSA-N 0.000 claims 3
- GZJLLYHBALOKEX-UHFFFAOYSA-N 6-Ketone, O18-Me-Ussuriedine Natural products CC=CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O GZJLLYHBALOKEX-UHFFFAOYSA-N 0.000 claims 3
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims 3
- 239000003963 antioxidant agent Substances 0.000 claims 3
- 230000003078 antioxidant effect Effects 0.000 claims 3
- 235000006708 antioxidants Nutrition 0.000 claims 3
- 235000021466 carotenoid Nutrition 0.000 claims 3
- KAUVQQXNCKESLC-UHFFFAOYSA-N docosahexaenoic acid (DHA) Natural products COC(=O)C(C)NOCC1=CC=CC=C1 KAUVQQXNCKESLC-UHFFFAOYSA-N 0.000 claims 3
- 229940106134 krill oil Drugs 0.000 claims 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 2
- 150000001747 carotenoids Chemical class 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- RYCNUMLMNKHWPZ-SNVBAGLBSA-N 1-acetyl-sn-glycero-3-phosphocholine Chemical compound CC(=O)OC[C@@H](O)COP([O-])(=O)OCC[N+](C)(C)C RYCNUMLMNKHWPZ-SNVBAGLBSA-N 0.000 claims 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 claims 1
- JEBFVOLFMLUKLF-IFPLVEIFSA-N Astaxanthin Natural products CC(=C/C=C/C(=C/C=C/C1=C(C)C(=O)C(O)CC1(C)C)/C)C=CC=C(/C)C=CC=C(/C)C=CC2=C(C)C(=O)C(O)CC2(C)C JEBFVOLFMLUKLF-IFPLVEIFSA-N 0.000 claims 1
- 241000239366 Euphausiacea Species 0.000 claims 1
- 238000008214 LDL Cholesterol Methods 0.000 claims 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 claims 1
- 229930003427 Vitamin E Natural products 0.000 claims 1
- CWRILEGKIAOYKP-SSDOTTSWSA-M [(2r)-3-acetyloxy-2-hydroxypropyl] 2-aminoethyl phosphate Chemical compound CC(=O)OC[C@@H](O)COP([O-])(=O)OCCN CWRILEGKIAOYKP-SSDOTTSWSA-M 0.000 claims 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims 1
- 235000013793 astaxanthin Nutrition 0.000 claims 1
- MQZIGYBFDRPAKN-ZWAPEEGVSA-N astaxanthin Chemical compound C([C@H](O)C(=O)C=1C)C(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)C(=O)[C@@H](O)CC1(C)C MQZIGYBFDRPAKN-ZWAPEEGVSA-N 0.000 claims 1
- 229940022405 astaxanthin Drugs 0.000 claims 1
- 239000001168 astaxanthin Substances 0.000 claims 1
- 125000001895 carotenoid group Chemical group 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229930003935 flavonoid Natural products 0.000 claims 1
- 150000002215 flavonoids Chemical class 0.000 claims 1
- 235000017173 flavonoids Nutrition 0.000 claims 1
- 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 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 1
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 235000019155 vitamin A Nutrition 0.000 claims 1
- 239000011719 vitamin A Substances 0.000 claims 1
- 235000019165 vitamin E Nutrition 0.000 claims 1
- 229940046009 vitamin E Drugs 0.000 claims 1
- 239000011709 vitamin E Substances 0.000 claims 1
- 229940045997 vitamin a Drugs 0.000 claims 1
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Claims (54)
1. Композиция, включающаяся фосфолипидные соединения Формулы I:
где R1 и R2 каждый независимо представляют собой остаток докозагексаеноевой кислоты (DHA) или эйкозапентаеновой кислоты (EPA);
каждый X независимо выбран из -CH2CH2NH3, -CH2CH2N(CH3)3 или
общее количество фосфолипидов в композиции находится в концентрации от 50% (мас./мас. (фосфолипиды/вся композиция)) до 99% (мас./мас. (фосфолипиды/вся композиция)); композиция дополнительно содержит свободный ЕРА и свободный DHА;
где
общее количество EPA в композиции составляет от 15 мас.% до 25 мас.%; и
общее количество DHА в композиции составляет от 10 мас.% до 15 мас.%.
2. Композиция по п. 1, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации от 60%±5% (мас./мас. (фосфолипиды/вся композиция)) до 70%±5% (мас./мас. (фосфолипиды/вся композиция)).
3. Композиция по п. 2, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации 66% ±5% (мас./мас. (фосфолипиды/вся композиция)).
4. Композиция по п. 1, отличающаяся тем, что соединения Формулы I находятся в концентрации более 70% (мас./мас. (фосфолипиды/вся композиция)) до 90% (мас./мас. (фосфолипиды/вся композиция)) по массе фосфолипидов от общей массы композиции.
5. Композиция по п. 4, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации от 80% (мас./мас. (фосфолипиды/вся композиция)) до 90% (мас./мас. (фосфолипиды/вся композиция)).
6. Композиция по п. 5, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации 90% (мас./мас. (фосфолипиды/вся композиция)).
7. Композиция по п. 1, отличающаяся тем, что концентрированный терапевтический фосфолипидный экстракт содержит одинаковое количество эйкозапентаеновой кислоты и докозагексаеноевой кислоты.
8. Композиция по п. 1, отличающаяся тем, что композиция дополнительно содержит триглицериды и где концентрация триглицеридов составляет менее чем 5% (мас./мас. (триглицериды/вся композиция)).
9. Композиция по п. 1, отличающаяся тем, что дополнительно содержит дополнительный антиоксидант.
10. Композиция по п. 9, отличающаяся тем, что дополнительный антиоксидант выбран из астаксантина, каротиноида и флавоноида.
11. Композиция по п. 10, отличающаяся тем, что дополнительный антиоксидант является каротиноидом.
12. Композиция по п. 11, отличающаяся тем, что каротиноид является про-витамином A или витамином Е.
13. Композиция по п. 1, для снижения уровней триглицеридов, циркулирующих в плазме.
14. Композиция по п. 13, дополнительно снижает концентрации ЛПНП- холестерина в плазме и повышает концентрации ЛПВП-холестерина в плазме.
15. Композиция по п. 11, отличающаяся тем, что фосфолипидные соединения включают фосфатидилэтаноламин, фосфатидилхолин, лизофосфатидилэтаноламин, N-ацил-фосфатидилэтаноламин (APE) и лизофосфатидилхолин.
16. Капсула, содержащая концентрированный терапевтический экстракт масла криля, где концентрированный терапевтический экстракт масла криля содержит фосфолипидные соединения Формулы I:
где R1 и R2 каждый независимо представляют собой остаток докозагексаеноевой кислоты (DHA) или эйкозапентаеновой кислоты (EPA);
каждый X независимо выбран из -CH2CH2NH3, -CH2CH2N(CH3)3 или
общее количество фосфолипидов в экстракте находится в концентрации от 50% (мас./мас. (фосфолипиды/вся композиция)) до 99% (мас./мас. (фосфолипиды/вся композиция)); и композиция дополнительно содержит свободный ЕРА и свободный DHА;
где
общее количество EPA в композиции составляет от 15 мас.% до 25 мас.%; и
общее количество DHА в композиции составляет от 10 мас.% до 15 мас.%,
экстракт пригоден для потребления человеком.
17. Капсула по п. 16, отличающаяся тем, что композиция дополнительно содержит триглицериды в концентрации менее чем 5 % (мас./мас. (триглицериды/вся композиция)).
18. Капсула по п. 16, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации от 60%±5% (мас./мас. (фосфолипиды/вся композиция)) до 70%±5% (мас./мас. (фосфолипиды/вся композиция)).
19. Капсула по п. 16, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации 66% ±5% (мас./мас. (фосфолипиды/вся композиция)).
20. Капсула по п. 16, отличающаяся тем, что экстракт получен из криля.
21. Использование композиции для получения фармацевтических композиций для снижения уровня триглицеридов в сыворотке крови, где композиция содержит эффективное количество концентрированного терапевтического фосфолипидного экстракта,
где:
экстракт содержит фосфолипидные соединения Формулы I:
R1 и R2 каждый независимо представляют собой остаток докозагексаеноевой кислоты (DHA) или эйкозапентаеновой кислоты (EPA);
каждый X независимо выбран из -CH2CH2NH3, -CH2CH2N(CH3)3 или
где общее количество фосфолипидных соединений Формулы I из экстракта находится в концентрации от 50% до 90% (мас./мас. (фосфолипиды/вся композиция));
общее количество EPA в экстракте составляет от 15 мас.% до 25 мас.%;
общее количество DHА в экстракте составляет от 10 мас.% до 15 мас.%,
и
экстракт пригоден для потребления человеком.
22. Использование по п.21, отличающееся тем, что композиция содержится в капсуле.
23. Использование по п.21, отличающееся тем, что композиция является маслом криля.
24. Использование по п.21, отличающееся тем, что экстракт дополнительно содержит триглицериды в концентрации менее чем 5 % (мас./мас. (триглицериды/вся композиция)).
25. Использование по п.21, отличающееся тем, что фосфолипидные соединения Формулы I находятся в концентрации от 60%±5% (мас./мас. (фосфолипиды/вся композиция)) до 70%±5% (мас./мас. (фосфолипиды/вся композиция)).
26. Использование по п.21, отличающаяся тем, что фосфолипидные соединения Формулы I находятся в концентрации 66% ±5% (мас./мас. (фосфолипиды/вся композиция)).
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