RU2016147575A - Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции - Google Patents
Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции Download PDFInfo
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- RU2016147575A RU2016147575A RU2016147575A RU2016147575A RU2016147575A RU 2016147575 A RU2016147575 A RU 2016147575A RU 2016147575 A RU2016147575 A RU 2016147575A RU 2016147575 A RU2016147575 A RU 2016147575A RU 2016147575 A RU2016147575 A RU 2016147575A
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- pharmaceutically acceptable
- acceptable composition
- dopa
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- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 title claims 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 title claims 2
- 239000000534 dopa decarboxylase inhibitor Substances 0.000 title 1
- 239000003697 methyltransferase inhibitor Substances 0.000 title 1
- 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
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims 4
- 208000019430 Motor disease Diseases 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 3
- 235000010323 ascorbic acid Nutrition 0.000 claims 3
- 239000011668 ascorbic acid Substances 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- 239000004475 Arginine Substances 0.000 claims 2
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 229960004308 acetylcysteine Drugs 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- 229960005070 ascorbic acid Drugs 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229960003180 glutathione Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- IVTMXOXVAHXCHI-YXLMWLKOSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid;(2s)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 IVTMXOXVAHXCHI-YXLMWLKOSA-N 0.000 claims 1
- PWKSKIMOESPYIA-UHFFFAOYSA-N 2-acetamido-3-sulfanylpropanoic acid Chemical group CC(=O)NC(CS)C(O)=O PWKSKIMOESPYIA-UHFFFAOYSA-N 0.000 claims 1
- LITUBCVUXPBCGA-WMZHIEFXSA-N Ascorbyl stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O LITUBCVUXPBCGA-WMZHIEFXSA-N 0.000 claims 1
- 239000004261 Ascorbyl stearate Substances 0.000 claims 1
- 108010024636 Glutathione Proteins 0.000 claims 1
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims 1
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims 1
- 239000004260 Potassium ascorbate Substances 0.000 claims 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims 1
- 229940072107 ascorbate Drugs 0.000 claims 1
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims 1
- 235000019276 ascorbyl stearate Nutrition 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 235000010376 calcium ascorbate Nutrition 0.000 claims 1
- 229940047036 calcium ascorbate Drugs 0.000 claims 1
- 239000011692 calcium ascorbate Substances 0.000 claims 1
- BLORRZQTHNGFTI-ZZMNMWMASA-L calcium-L-ascorbate Chemical compound [Ca+2].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] BLORRZQTHNGFTI-ZZMNMWMASA-L 0.000 claims 1
- 229960004205 carbidopa Drugs 0.000 claims 1
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical compound NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 235000019275 potassium ascorbate Nutrition 0.000 claims 1
- 229940017794 potassium ascorbate Drugs 0.000 claims 1
- CONVKSGEGAVTMB-RXSVEWSESA-M potassium-L-ascorbate Chemical compound [K+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] CONVKSGEGAVTMB-RXSVEWSESA-M 0.000 claims 1
- 235000010378 sodium ascorbate Nutrition 0.000 claims 1
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 claims 1
- 229960005055 sodium ascorbate Drugs 0.000 claims 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 claims 1
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
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- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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Claims (10)
1. Фармацевтически приемлемая композиция для лечения неврологического или двигательного расстройства, содержащая от 2,5% до 7% по массе леводопы, от 0% до 2% по массе карбидопы, от 5% до 18% по массе аргинина и от 0,25% до 3% по массе аскорбиновой кислоты или ее фармацевтически приемлемой соли.
2. Фармацевтически приемлемая композиция по п. 1, отличающаяся тем, что рН указанной композиции составляет от 9,1 до 9,8 при 25°С.
3. Фармацевтически приемлемая композиция по п. 1, отличающаяся тем, что молярное отношение леводопы и карбидопы, если она присутствует, к аргинину составляет от 1:1,8 до 1:3,5.
4. Фармацевтически приемлемая композиция по п. 1, отличающаяся тем, что указанная соль аскорбиновой кислоты выбрана из аскорбата, аскорбата натрия, аскорбата кальция, аскорбата калия, аскорбилпальмитата или аскорбилстеарата.
5. Фармацевтически приемлемая композиция по п. 1, дополнительно содержащая агент, который ингибирует образование продуктов окисления.
6. Фармацевтически приемлемая композиция по п. 5, отличающаяся тем, что указанный агент выбран из L-цистеина, N-ацетилцистеина (NAC), глутатиона (GSH), Na2-EDTA, Na2-EDTA-Ca, бисульфита натрия или их комбинаций.
7. Фармацевтически приемлемая композиция по п. 1, приготовленная для непрерывного подкожного, трансдермального, интрадуоденального или внутривенного введения.
8. Фармацевтически приемлемая композиция по п. 1, отличающаяся тем, что указанное неврологическое или двигательное расстройство представляет собой болезнь Паркинсона.
9. Способ лечения неврологического или двигательного расстройства, такого как болезнь Паркинсона, у пациента, который в этом нуждается, включающий введение указанному пациенту фармацевтически приемлемой композиции по любому из пп. 1-7.
10. Способ по п. 9, отличающийся тем, что указанную композицию вводят подкожно, трансдермально, интрадуоденально или внутривенно, при этом предпочтительно композицию вводят непрерывно.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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US41363710P | 2010-11-15 | 2010-11-15 | |
US61/413,637 | 2010-11-15 | ||
US201161524064P | 2011-08-16 | 2011-08-16 | |
US61/524,064 | 2011-08-16 |
Related Parent Applications (1)
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RU2013123457A Division RU2607497C2 (ru) | 2010-11-15 | 2011-11-15 | Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции |
Publications (3)
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RU2016147575A true RU2016147575A (ru) | 2018-10-23 |
RU2016147575A3 RU2016147575A3 (ru) | 2020-03-04 |
RU2740080C2 RU2740080C2 (ru) | 2021-01-11 |
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RU2016147575A RU2740080C2 (ru) | 2010-11-15 | 2011-11-15 | Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции |
RU2013123457A RU2607497C2 (ru) | 2010-11-15 | 2011-11-15 | Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции |
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Country Status (26)
Country | Link |
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US (6) | US9421267B2 (ru) |
EP (3) | EP3326615B1 (ru) |
JP (3) | JP5902705B2 (ru) |
KR (1) | KR101859242B1 (ru) |
CN (2) | CN103442693A (ru) |
AU (1) | AU2011330757B2 (ru) |
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BR112016021034A8 (pt) | 2014-03-13 | 2021-06-29 | Neuroderm Ltd | composição farmacêutica, uso da mesma e kit |
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