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Complex salt or composition medicine of breviscapine and basic amino acid for treating cardiac and cerebral vascular diseases

A cardiovascular and cerebrovascular disease, breviscapine technology, applied in the field of breviscapine basic amino acid double salt or composition medicine for the treatment of cardiovascular and cerebrovascular diseases, can solve the problem of affecting the absorption and metabolism of breviscapine, affecting solubility and stability Improve pharmacokinetic parameters, increase bioavailability, and improve molecular polarity

Inactive Publication Date: 2006-11-08
SICHUAN GUOKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, because its molecule belongs to the multi-substituted flavonoid structure, its molecular rigidity is strong, and its solubility in water is poor, which not only affects its solubility and stability in various preparations, such as the clarity of injections, but also affects the breviscapine. Absorption and metabolism in the body, thus limiting its route of administration, reducing its bioavailability, allergic reactions, urticaria, weakness of limbs, dry mouth, fatigue, cardiovascular reactions, high fever, chills, infusion Adverse effects such as reactions have greatly affected the clinical promotion and use of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1, the preparation of breviscapine arginine double salt

[0015] Weigh 230 mg of breviscapine, completely dissolve it in 60 ml of absolute ethanol at a slight temperature, feed in portions under stirring, and add 116.0 mg of L-arginine. Let it cool down slightly, add sodium carbonate solution dropwise under stirring, and monitor the pH change until the pH is about 7-9. Continue to stir and reflux for 3 to 4 hours. After the reaction is completed, the reaction solvent is removed by rotary evaporation. After the residue is vacuum-dried for 2 hours, add 60ml to 100ml of ethanol, shake fully, filter under reduced pressure, and recover ethanol from the filtrate under reduced pressure. Place, filter with suction, and combine the filtrates. The filtrate was ultrasonically treated for 15-30 minutes, and then filtered with a 0.22 μm microporous membrane, and the filtrate was distilled to volume to obtain the final product. Or freeze-dry the filtrate to obtain white...

Embodiment 2

[0016] Example 2, Preparation of Breviscapine Lysine Double Saline Injection

[0017] Weigh 150 g of breviscapine lysine double salt, add 20,000 ml of purified water for injection, dissolve, filter, prepare 2 ml / bottle, and sterilize to obtain 10,000 water injections. Each bottle contains breviscapine lysine double salt 15mg.

Embodiment 3

[0018] Embodiment 3, preparation of breviscapine lysine powder injection

[0019] Weigh 200g of breviscapine lysine double salt, dextran S 40 160g, add 25000ml of water for injection to dissolve, filter through a 0.22μm microporous membrane, measure the content, and pack into 2.5ml each. Freeze-dry to obtain 10,000 breviscapine lysine double salt powder injections, each containing 20 mg breviscapine lysine double salt.

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PUM

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Abstract

The present invention relates to complex salt or composition medicine of breviscapine and basic amino acid for treating cardiac and cerebral vascular diseases. The composition medicine consists of breviscapine 1 weight portions, and basic amino acid 0.01-100 weight portions, and proper amount of supplementary material. It may be prepared into powder for injection, injection, oral liquid, capsule and other suitable clinical preparation forms. The composition medicine of the present invention has obviously raised dissolubility and bioavailability of breviscapine, high medicine effect, obvious synergistic effect and wide clinical application foreground.

Description

technical field [0001] The invention relates to a scutellarin basic amino acid double salt or composition drug used for treating cardiovascular and cerebrovascular diseases in the technical field of medicine, specifically comprising 1 part of breviscapine (weight percentage), basic amino acid namely arginine, composition A double salt or composition drug formed by compatibility of 0.01 to 100 parts of amino acids of one of amino acid, tryptophan and lysine, or any combination of any of them in any proportion. Background technique [0002] Cardiovascular and cerebrovascular disease is the disease with the highest mortality rate in the world today, killing more than 120 million people every year, accounting for more than 25% of the global death total, and disabling thousands of patients. Moreover, the age tends to be younger and middle-aged, especially the rapid development of society, the change of diet structure, environmental pollution, and the incidence of various psycholo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/16A61K9/20A61K9/48A61K9/70A61K31/198A61K31/4172A61P9/00A61P9/10
Inventor 周旋邹小利江雪邓敏
Owner SICHUAN GUOKANG PHARMA
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