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 PDF

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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
composition
composition according
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RU2740080C2 (ru
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Орон ЯКОБИ-ЦЕЕВИ
Мара НЕМАС
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Нейродерм Лтд
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/12Ketones
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    • A61K31/12Ketones
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    • AHUMAN NECESSITIES
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    • A61K31/13Amines
    • A61K31/133Amines having hydroxy groups, e.g. sphingosine
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
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    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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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    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
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    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
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    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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    • A61K47/26Carbohydrates, 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 (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.
RU2016147575A 2010-11-15 2011-11-15 Непрерывное введение l-допа, ингибиторов допа-декарбоксилазы, ингибиторов катехол-о-метилтрансферазы и предназначенные для этого композиции RU2740080C2 (ru)

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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

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