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First-class new medicine cyclovirobuxine D series for treating cardiovascular and cerebrovascular disease and method for preparing the same

A technology for cardiovascular and cerebrovascular diseases, cyclovirboxicin, applied in the field of a new drug pegylated cyclovirboxicin D series for the treatment of cardiovascular and cerebrovascular diseases and its preparation field, which can solve the problem that the water solubility has not been well improved , poor water solubility, narrow safety range, etc., to achieve good blood compatibility and physiological activity

Inactive Publication Date: 2006-09-06
SICHUAN CHUANDA WEST CHINA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, pharmacological experiments and clinical application studies have shown that cyclovirboxine D has a narrow range of safety, and because it is a fat-soluble alkaloid, its water solubility is very poor, so the bioavailability of cyclovirboxine D can be improved and its biodynamics in vivo can be improved. It is very necessary to expand its safe use range and carry out structural modification and pharmacological activity research.
However, there are few studies on its structural modification, but its water solubility has not been well improved.

Method used

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  • First-class new medicine cyclovirobuxine D series for treating cardiovascular and cerebrovascular disease and method for preparing the same
  • First-class new medicine cyclovirobuxine D series for treating cardiovascular and cerebrovascular disease and method for preparing the same
  • First-class new medicine cyclovirobuxine D series for treating cardiovascular and cerebrovascular disease and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of polyethylene glycol-monoacid 5 (PEG-DA)

[0021] 60g (10mmol) PEG-6000 dissolved in 150mL anhydrous chloroform (CaH 2 Distilled off in the presence), 5g (50mmol) of succinic anhydride, 4mL of dry pyridine were added, and the reaction was refluxed under stirring for 48h. The reaction mixture was evaporated to dryness under reduced pressure, and the residue was saturated with NaHCO 3 Dissolve the aqueous solution, filter, cool the filtrate to 0~5℃, acidify with hydrochloric acid, extract three times with chloroform, wash the combined chloroform solution three times with water, anhydrous Na 2 SO 4 After drying and removing the desiccant, the filtrate is concentrated, and a large amount of dry ether is added to precipitate the product. The product was recrystallized three times with ether, and then weighed after drying. The product weighed 57 g and the yield was 90%.

[0022] According to this method, PEG-400-diacid, PEG-1000-diacid, PEG-2000-diacid, PEG-4000-diaci...

Embodiment 2

[0033]Take 150g of PEG-6000-diacid-CVB-D, add 20000ml of refined water for injection, dissolve, filter, prepare 2ml / bottle, sterilize, and get 10,000 water injections. Each bottle contains 15mg of PEG-6000-Diacid-CVB-D.

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Abstract

By organic synthesis and high molecular polymerization and other measures in this invention, graft hydrophilic polietilenglicol on the sideline of cyclovirobuxine D, and obtain a series of modified cyclovirobuxine D new drugs for cerebrovascular disease therapy. Characterize product structure with IR, 1H-NMR, GPC, MS, and so on; at the same time do its water-solubility, hemolysis test and hypoxia-resistant test on rat. The results above show: activated polietilenglicol has been successfully grafted on cyclovirobuxine D, and this turns water-insoluble cyclovirobuxine D into water-soluble polyaethylenglycolization cyclovirobuxine D; also it has good blood compatibility and physiologic activity. So the new drugs of polyaethylenglycolization cyclovirobuxine D system can be made into ampules, oral liquid, capsule, troche, and any other form feasible to clinic. The average molecular weight of the polietilenglicol is 200-60000.

Description

Technical field [0001] The present invention relates to the technical field of medicine. Hydrophilic polyethylene glycol is directly grafted onto the amino side chain of Cyclovirobuxine D through organic synthesis and polymer polymerization to obtain a series of modified PEGylation. The new drug of Cyclovirobuxine D, with IR, 1 The structure of the product was characterized by H-NMR, GPC, MS, etc. At the same time, the water solubility and hemolysis test and the hypoxia tolerance of mice were carried out. The results showed that the activated polyethylene glycol was successfully It is grafted onto Cyclovirobuxine D, so that the water-insoluble Cyclovirobuxine D becomes water-soluble pegylated Cyclovirobuxine D. And has good blood compatibility and physiological activity. Therefore, the pegylated Cyclovirobuxine D series of new drugs can be made into all clinically suitable other dosage forms including injections, oral liquids, capsules, and tablets. technical background [0002] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/765A61K31/56A61P9/00
Inventor 郭彩红窦后松范辰华郜宁杨定菊李颖尹述凡
Owner SICHUAN CHUANDA WEST CHINA PHARMA
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