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Sulfonation technique for isoliensinine, arrhythmia resistant function of products produced thereby

A technology of isoliensinine sulfone and isoliensinine, which is applied in the directions of medical preparations containing active ingredients, organic chemistry, cardiovascular system diseases, etc., and can solve the problems of poor water solubility, inability to make conventional preparations, light and heat sensitivity, etc.

Inactive Publication Date: 2008-09-24
潘阳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Pharmacological experiments have proved that isoliensinine has a broad-spectrum anti-arrhythmia effect, and its curative effect is better than that of quinidine. Since isoliensinine is a phenolic alkaloid, it is sensitive to light and heat, has unstable chemical properties, and has poor water solubility. The bioavailability is low, and conventional preparations cannot be made. The sodium isoliensinine sulfonate obtained after sulfonation not only improves the stability of isoliensinine, but also increases water solubility, which improves the bioavailability of isoliensinine. It can be prepared into preparations for clinical application. There has been no relevant report on this invention so far, and the research results will be in a leading position at home and abroad.

Method used

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  • Sulfonation technique for isoliensinine, arrhythmia resistant function of products produced thereby
  • Sulfonation technique for isoliensinine, arrhythmia resistant function of products produced thereby
  • Sulfonation technique for isoliensinine, arrhythmia resistant function of products produced thereby

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation method of sodium isoliensinine sulfonate

[0052] (1) Take the lotus seed heart and crush it into coarse powder, moisten it with 70% ethanol and put it into the percolation cylinder, add 70% ethanol until the lotus seed heart is completely submerged, soak for 24 hours, start to percolate, collect the percolation liquid until the percolation liquid is completely submerged Turn yellowish brown into dark green, stop percolation, combine percolation liquid, filter, recover ethanol, dissolve residual liquid with 10% sulfuric acid solution, filter, adjust pH to 9-10 with concentrated ammonia water, extract with chloroform, recover chloroform to obtain fat-soluble total alkali.

[0053] (2) Take the fat-soluble total alkali, dissolve it with 10% sulfuric acid solution, absorb it on a macroporous resin column, wash it with water to neutrality, continue to elute with 30% ethanol, and discard the eluent; elute with 70% ethanol to no The alkaloids of lotu...

Embodiment 2

[0057] Example 2 Preparation of lyophilized injection

[0058] Weigh 10g of isoliensinine sodium sulfonate, add 1000ml of water for injection, keep stirring at 80°C to 90°C, after it is completely dissolved, add 100g of mannitol, stir to dissolve; adjust the pH value to 6-7, filter aseptically, Quantitatively divided into control glass bottles, freeze-dried, that is.

Embodiment 3

[0059] Example 3 Preparation of Injections

[0060] Weigh 10g of isoliensinine sodium sulfonate, add it to 1000ml of water for injection, adjust the pH value to 6-7 with 0.1mol / l hydrochloric acid, stir for 30 minutes, add a certain amount of activated carbon, continue stirring for half an hour, filter, pass through 0.22μm After the membrane is filtered, it can be filled.

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Abstract

The present invention relates to di-benzyl isoquinoline monoether-key alkaloid, isoliensinine, which is extracted from lotus seeds. The present invention also discloses a preparation process of sulfonation. Isoliensinine sodium sulfonate that is prepared through the sulfonation, which not only improves the stability of the phenol alkaloid of isoliensinine, but also improves the water solubility and bioavailability of the isoliensinine. The content of the isoliensinine sodium sulfonate prepared in the method is above 97 percent. Based on the pharmacodynamic results, the method further discloses the anti-arrhythmic security and effectiveness of the isoliensinine sodium sulfonate and preparations thereof.

Description

technical field [0001] The invention relates to a sulfonation technology of isoliensinine, a bisbenzylisoquinoline monoether bond type alkaloid extracted from lotus seeds with antiarrhythmic effect, and belongs to the field of chemical medicines. Background technique [0002] With the improvement of living standards, people drink alcohol and excessive intake of high-fat and high-sugar foods, as well as work and life pressure continue to increase, the incidence of cardiovascular disease is increasing year by year, and almost all cardiovascular diseases can induce arrhythmia , such as coronary heart disease, myocarditis, rheumatic heart disease, etc. Modern medicine has proved that the most common cause of sudden death is malignant arrhythmia. Due to the many factors causing arrhythmia and the need for personalized treatment, although there are more than 10 kinds of antiarrhythmic injections in clinical use, due to the common side effects Therefore, there is still a great dem...

Claims

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Application Information

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IPC IPC(8): C07D217/20A61K31/4725A61P9/06A61K36/62
Inventor 潘阳徐斌雷均涛陈龙
Owner 潘阳
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