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New hydroxysafflor yellow pharmaceutical salt

A technology of hydroxysafflower and yellow pigment, which is applied in freeze-dried powder injection, medicinal salt of hydroxysafflower yellow pigment, medicinal salt of hydroxysafflower yellow A and its preparation field, which can solve the problem of low product purity and influence on product , structural properties can not be qualitative and other issues

Active Publication Date: 2014-08-13
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 problem. Controllability, and affect the stability and safety of products, especially injectable drugs

Method used

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  • New hydroxysafflor yellow pharmaceutical salt
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  • New hydroxysafflor yellow pharmaceutical salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Embodiment 1: Hydroxy safflower yellow A potassium (in general formula I, R is potassium)

[0112] 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 strongly acidic 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. Adjust the pH to 4-7, then slowly add to the macroporous adsorption resin separation column, the ratio of column diameter to height is 1:12, and the sample loading flow rate is 10ml per minute. After loading the sample, it was eluted with deionized wate...

Embodiment 2

[0133] Embodiment 2: Hydroxy safflower yellow A potassium (in formula I, R is potassium)

[0134]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 KOH to adjust the pH to 4-7, 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 wa...

Embodiment 3

[0135] Embodiment 3: the hydroxyl safflower yellow A ammonium of formula III (in formula I, R is NH 4 )

[0136] 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 001*7 strong acidic H-type cation exchange resin that has been treated and balanced. The column diameter-height ratio is 1:10, the column volume is 500ml, and the flow rate is 3ml / min. Adjust the pH to 4-7, then slowly add to the macroporous adsorption resin separation column, the ratio of column diameter to height is 1:12, and the sample loading flow rate is 10ml per minute. After loading the sample, it was elute...

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Abstract

The invention provides a new hydroxysafflor yellow A pharmaceutical salt compound shown as formula I, particularly provides a new monomeric compound of potassium hydroxysafflor yellow A and ammonium hydroxysafflor yellow A, and provides a production method and medicinal use of the compound. The hydroxysafflor yellow A pharmaceutical salt monomeric compound is prepared from a medicinal material safflower as a raw material, by use of a strongly acidic H cation exchange resin, hydroxysafflor yellow A is transformed into an acid form, and then by pH adjustment, the hydroxysafflor yellow A pharmaceutical salt monomeric compound is generated from the hydroxysafflor yellow A. The purity higher than 98% can be guaranteed, and compared with the hydroxysafflor yellow A, the new hydroxysafflor yellow A pharmaceutical salt compound is a controllable monomeric compound which is safer, more effective and more stable in application in resisting platelet aggregation, coronary heart disease, angor pectoris, acute cerebral ischemia and other various blood circulation disorders. R is as defined by the specification.

Description

technical field [0001] The invention provides a new medicinal salt of hydroxysafflower yellow, in particular, a medicinal salt of hydroxysafflower yellow A and its preparation method, freeze-dried powder injection and 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. It is the most effective water-soluble part of safflower pharmacological effects. It can inhibit platelet aggregation and release induced by platelet activating factor, and can compete with It can effectively inhibit the combination o...

Claims

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Application Information

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IPC IPC(8): C07D309/10A61K31/351A61P9/10A61P7/02
CPCC07D309/10
Inventor 叶凤起蔡犇陈勇灵卢敏
Owner ZHEJIANG YONGNING PHARMA
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