Piperazine-cyclodextrines complex and medicinal product containing the specified complex

 

Described piperazine-cyclodextrines complex formed from 3-[2-[4-(3-chloro-2-were)-1-piperazinil] -ethyl] -5,6-dimethoxy-1-(4-imidazolidinyl)-1H-indazole and freely water-soluble cyclodextrin derivative, where the specified cyclodextrin derivative is sulfobutyl-cyclodextrin or a hydroxyl--cyclodextrin or its salt. Also described for the treatment of diseases of the circulatory system and diseases of the brain, containing as active ingredient the above complex. The complex has a high solubility in water and low local irritant effect. 2 S. and 11 C.p. f-crystals, 3 tables.

Description text in facsimile form (see graphic part)

Claims

1. Piperazine-cyclodextrines complex formed from 3-[2-[4-(3-chloro-2-were)-1-piperazinil] -ethyl] -5,6-dimethoxy-1-(4-imidazolidinyl)-1H-indazole and freely water-soluble cyclodextrin derivative, where the specified cyclodextrin derivative is sulfobutyl-cyclodextrin or hydroxypropyl--cyclodextrin or its salt.

3. Piperazine-cyclodextrines complex according to any one of p. 1 or 2, in which the water-soluble cyclodextrin derivative is sulfobutyl-cyclodextrin or its salt.

4. Piperazine-cyclodextrines complex according to any one of paragraphs. 1-3, in which the water-soluble cyclodextrin derivative is sulfobutyl-cyclodextrin, with a replacement rate of 70% or less, or its salt.

5. Piperazine-cyclodextrines complex according to any one of paragraphs. 1-4, in which the water-soluble cyclodextrin derivative is sulfobutyl-cyclodextrin, with a replacement rate of 20-50%, or its salt.

6. Piperazine-cyclodextrines complex according to any one of paragraphs. 1-5, in which the water-soluble cyclodextrin derivative is a sodium salt sulfobutyl ether-cyclodextrin, with a replacement rate of approximately 33%.

7. Piperazine-cyclodextrines complex according to any one of p. 1 or 2, in which a water-soluble derivative of cyclodextrin is a hydroxypropyl--cyclodextrin or its salt.

8. Piperazine-cyclodextrines droxidopa-cyclodextrin, with a replacement rate of 70% or less, or its salt.

9. Piperazine-cyclodextrines complex according to any one of paragraphs. 1, 2 or 8, in which a water-soluble derivative of cyclodextrin is a hydroxypropyl--cyclodextrin, with a replacement rate of 20-50%, or its salt.

10. Piperazine-cyclodextrines complex according to any one of paragraphs. 1, 2 or 9, in which a water-soluble derivative of cyclodextrin is a hydroxypropyl--cyclodextrin, with a replacement rate of approximately 23% or less, or its salt.

11. Drug for the treatment of diseases of the circulatory system and diseases of the brain, having a protective effect on the brain, containing as the active ingredient piperazine-cyclodextrines complex according to any one of paragraphs. 1-10.

12. Drug under item 11, which is a composition for injection containing piperazine-cyclodextrines complex according to any one of paragraphs. 1-10.

13. Drug under item 12, which is a composition for injection, obtained by lyophilization of an aqueous solution containing piperazine-cyclodextrines complex according to any one of paragraphs. 1-10.

 

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