Salvianolic acid A magnesium salt, preparation method and use of the salvianolic acid A magnesium salt, and salvianolic acid A magnesium salt-containing freeze-dried powder injection composition

A technology for freeze-dried powder injection and salvianolic acid, which is applied in the field of medicine, can solve the problems such as the difficulty in exerting the medicinal use of salvianolic acid A, the poor water solubility of salvianolic acid A, and the reduction of irritation, so as to improve solubility and stability. Good, not easy to be oxidized effect

Inactive Publication Date: 2012-05-02
吴谢军 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Salvianolic acid A has poor water solubility, low pH and high irritation, so its use in preparations is greatly restricted, making it difficult to bring into play the good medical use of salvianolic acid A. Therefore, various methods should be used to treat salvianolic acid A Improve the water solubility of salvianolic acid A and reduce its irritation, thereby expanding its application in the treatment of cardiovascular and cerebrovascular diseases
[0004] CN101361728A discloses the injection preparation process of salvianolic acid A, but the salvianolic acid A developed by it has poor water solubility and high irritation; CN101134726 discloses a derivative of salvianolic acid A and its application as an antioxidant, emphasizing It is the effect of the product modified on different structures of salvianolic acid A, which is obviously different from the structure of the developed magnesium salt compound of the present invention.
CN101497570A discloses the preparation of salvianolic acid A amino acid salt and the combination of powder injection. Although its irritation is reduced, it still has certain irritation. In the prior art, there is no method that can not only improve the water solubility of salvianolic acid A , and can reduce its irritation

Method used

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  • Salvianolic acid A magnesium salt, preparation method and use of the salvianolic acid A magnesium salt, and salvianolic acid A magnesium salt-containing freeze-dried powder injection composition
  • Salvianolic acid A magnesium salt, preparation method and use of the salvianolic acid A magnesium salt, and salvianolic acid A magnesium salt-containing freeze-dried powder injection composition
  • Salvianolic acid A magnesium salt, preparation method and use of the salvianolic acid A magnesium salt, and salvianolic acid A magnesium salt-containing freeze-dried powder injection composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh 0.82g of magnesium hydroxide, add 1L of water, and add CO 2 To clarify, remove CO from water by ultrasound 2 Magnesium bicarbonate was obtained; 36.0 g of salvianolic acid A was added and reacted at 30° C. for 30 min to obtain a reaction solution; the same volume of ethyl acetate as the reaction solution was added, vortexed for 5 minutes, centrifuged for 5 minutes, and vortexing and centrifugation were repeated 3 times. The magnesium salt of salvianolic acid A is obtained by freeze-drying. The molar ratio of salvianolic acid A to magnesium bicarbonate is 1:0.2.

Embodiment 2

[0036] Weigh 4.10g of magnesium hydroxide, add 1L of water, and pass in CO 2 To clarify, remove CO from water by ultrasound 2 Magnesium bicarbonate was obtained; 36.0 g of salvianolic acid A was added and reacted at 30°C for 30 min to obtain a reaction solution. The same volume of ethyl acetate as the reaction solution was added, vortexed for 5 minutes, centrifuged for 5 minutes, and the vortexing and centrifugation operations were repeated 3 times. The magnesium salt of salvianolic acid A is obtained by freeze drying. The molar ratio of salvianolic acid A to magnesium bicarbonate is 1:1.

Embodiment 3

[0038] Weigh 2.05g of magnesium hydroxide, add 1L of water, and add CO 2 To clarify, remove CO from water by ultrasound 2 Magnesium bicarbonate was obtained; 36.0 g of salvianolic acid A was added and reacted at 30°C for 30 min to obtain a reaction solution. The same volume of ethyl acetate as the reaction solution was added, vortexed for 5 minutes, centrifuged for 5 minutes, and the vortexing and centrifugation operations were repeated 3 times. The magnesium salt of salvianolic acid A is obtained by freeze-drying. The molar ratio of salvianolic acid A to magnesium bicarbonate is 1:0.5, which is the optimal ratio.

[0039] The structure of the magnesium salt of salvianolic acid A is confirmed as follows:

[0040] Proton Nuclear Magnetic Resonance Spectroscopy (CD 3 OD, 300MHz) analysis:

[0041] It can be seen from the proton nuclear magnetic resonance spectrum that the chemical shift of H-8″ changes the most, the δ(H-8″) of salvianolic acid A is 5.16, the δ(H-8″) of salvianolic aci...

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Abstract

The invention discloses a salvianolic acid A magnesium salt, specially, relates to the salvianolic acid A magnesium salt, a preparation method and a use of the salvianolic acid A magnesium salt, and a salvianolic acid A magnesium salt-containing freeze-dried powder injection composition, and belongs to the technical field of medicines. The preparation method of the salvianolic acid A magnesium salt comprises the following steps of adding magnesium hydroxide into water, feeding CO2 into the magnesium hydroxide solution until the magnesium hydroxide solution is clarified, removing the CO2 in the magnesium hydroxide solution by ultrasonic waves to obtain magnesium hydrogen carbonate, adding salvianolic acid A into the obtained magnesium hydrogen carbonate so that the salvianolic acid A and the obtained magnesium hydrogen undergo a reaction at a temperature of 20 to 40 DEG C for 20 to 40 minutes to produce a reaction product solution, adding ethyl acetate into the reaction product solution, wherein the volume of the added ethyl acetate is equal to that of the reaction product solution, carrying out vortexing, and then carrying out centrifugal separation and freeze drying to obtain the salvianolic acid A magnesium salt. The salvianolic acid A magnesium salt has strong stability in an aqueous solution, high solubility and small irritation. The preparation method of the salvianolic acid A magnesium salt adopts a good preparation technology and has the simple steps. The salvianolic acid A magnesium salt-containing freeze-dried powder injection composition has good stability and high uniformity, and satisfies medicine rehydration capability requirements. The salvianolic acid A magnesium salt can be utilized for preparation of medicines for treating ischemic stroke.

Description

Technical field [0001] The invention is a magnesium salt, especially the magnesium salt and preparation methods and applications and frozen -dried powder needle compositions of sanol acid, which belongs to the field of pharmaceutical technology. Background technique [0002] Vanphenol acid A is a phenolic acid compound that exists in the lip -shaped plant.Vanol acid A has a variety of pharmacological activity such as anti -platelet aggregation, anticoagulant, anti -thrombosis, and antioxidant, and has potential treatment value for cardiovascular and cerebrovascular diseases. [0003] Danol acid A is poor in water, and its pH is small, and the irritation is large, making it greatly restricted in the use of the preparation, making it difficult to play with good pharmaceutical uses of sodium phenolic acid A.Improve the water solution of sorcine A and reduce its irritation, thereby expanding its application in the treatment of cardiovascular and cerebrovascular diseases. [0004] CN1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/732C07C67/28A61K31/216A61K9/19A61P9/10
CPCY02P20/141
Inventor 吴谢军唐星朱靖博
Owner 吴谢军
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