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Novel hydroxysafflor yellow A divalent medicinal salts, and preparing method and uses thereof

A technology of safflower yellow pigment and hydroxy safflower is applied in the field of hydroxy safflower yellow A bivalent medicinal salt and preparation thereof, freeze-dried powder injection and medicinal use, and the field of hydroxy safflower yellow medicinal salt, which can solve the problem of The product purity is not high, the quality is uncontrollable, and the structural properties cannot be qualitatively determined, etc.

Inactive Publication Date: 2014-12-24
ZHEJIANG YONGNING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the hydroxysafflower yellow A produced by the existing production process is not high in product purity, basically there are more than 10% impurities, and the structural properties of such impurities have not been qualitatively determined, and there is a certain quality that cannot be determined. Controllability, and affect the stability and safety of products, especially injectable drugs

Method used

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  • Novel hydroxysafflor yellow A divalent medicinal salts, and preparing method and uses thereof
  • Novel hydroxysafflor yellow A divalent medicinal salts, and preparing method and uses thereof
  • Novel hydroxysafflor yellow A divalent medicinal salts, and preparing method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] Embodiment 1: Hydroxysafflower yellow A calcium (in general formula I, R is calcium)

[0118] Weigh safflower, add 12.5 times the weight of the medicinal material in deionized water, extract at 100°C for 20-25 minutes, filter, add 10 times the weight of the medicinal material to the filter residue and repeat the extraction once again according to the above conditions, and filter. Combine the secondary extracts, cool to room temperature, centrifuge with a centrifuge, and take the centrifugate for later use. Slowly add the above centrifugate to the well-balanced 001*7 strong acid H-type cation exchange resin, the ratio of column diameter to height is 1:10, the column volume is 500ml, and the flow rate is 3ml / min. (OH) 2 Adjust the pH to about 5.5, and then slowly add to the macroporous adsorption resin separation column, the column diameter-to-height ratio is 1:12, and the sample loading flow rate is 10ml per minute. After loading the sample, it was eluted with deionize...

Embodiment 2

[0136] Embodiment 2: Hydroxysafflower yellow A calcium (in formula I, R is calcium)

[0137] Weigh safflower, add 12.5 times the weight of the medicinal material in deionized water, extract at 100°C for 20-25 minutes, filter, add 10 times the weight of the medicinal material to the filter residue and repeat the extraction once again according to the above conditions, and filter. Combine the secondary extracts, cool to room temperature, centrifuge with a centrifuge, and take the centrifugate for later use. Slowly add the above centrifugate to the HB-8 macroporous strongly acidic H-type cation exchange resin that has been treated and balanced. The column diameter-to-height ratio is 1:10, the column volume is 500ml, and the flow rate is 3ml / min. Use calcium hydroxide solution to adjust the pH to about 5.5, then slowly add to the macroporous adsorption resin separation column, the column diameter-to-height ratio is 1:12, and the sample loading flow rate is 10ml per minute. After ...

Embodiment 3

[0138] Example 3: Calcium Hydroxysafflor Yellow A

[0139] Weigh safflower, add 12.5 times the weight of the medicinal material in deionized water, extract at 100°C for 20-25 minutes, filter, add 10 times the weight of the medicinal material to the filter residue and repeat the extraction once again according to the above conditions, and filter. Combine the secondary extracts, cool to room temperature, centrifuge with a centrifuge, and take the centrifugate for later use. Slowly add the above-mentioned centrifugate into the macroporous adsorption resin separation column, the diameter-to-height ratio of the column is 1:12, and the sample loading flow rate is 10 ml per minute. After loading the sample, it was eluted with deionized water at room temperature at a flow rate of 20 ml per minute. The eluate was concentrated under reduced pressure at 60°C to obtain a concentrated solution of crude safflower yellow. In terms of safflower, 100ml of concentrated solution is obtained pe...

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Abstract

The invention provides novel hydroxysafflor yellow A divalent medicinal salt compounds shown as a formula (I), especially a calcium salt of hydroxysafflor yellow A and a magnesium salt of the hydroxysafflor yellow A which are single compounds, and a producing method and medicinal uses of the salt compounds. A natural medicine material safflower is adopted as a raw material. Carthamin yellow is converted into a hydroxysafflor yellow A acid form through a strong-acid H-type cation exchange resin. Then by adjusting a pH value, the hydroxysafflor yellow A is converted into the hydroxysafflor yellow A divalent medicinal salt single compounds. The purity of the compounds can be higher than 98.5%. Compared with the hydroxysafflor yellow A, the compounds are safer, more effective, more stable and more controllable for treatment of blood circulation disturbance diseases such as anti-platelet aggregation, coronary diseases, angina and acute cerebral ischemia, and have better water solubility and human body tolerance. R is defined in the specification.

Description

technical field [0001] The invention provides a new medicinal salt of hydroxysafflower yellow, in particular, a divalent medicinal salt of hydroxysafflower yellow A, its preparation method, freeze-dried powder injection and its medical application. belongs to the field of medicinal chemistry. Background technique [0002] The traditional Chinese medicine safflower is the dried flower of Carthamus tinctouius L., a plant of Compositae. It is a common traditional Chinese medicine for promoting blood circulation and removing stasis. It can be used for the treatment of many blood circulation disorders such as coronary heart disease and angina pectoris. Hydroxysafflor yellow A (hydroxysafflor yellow A) is a compound with a single chalcone glycoside structure, which is the most effective water-soluble part of safflower pharmacological effects, can inhibit platelet aggregation and release induced by platelet activating factor, and can compete with It can effectively inhibit the com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/10A61K31/351A61P9/10A61P7/02
CPCA61K36/286C07D309/10A61P7/02A61P7/04A61P9/00A61P9/10
Inventor 叶凤起蔡犇卢敏陈勇灵
Owner ZHEJIANG YONGNING PHARMA
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