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Method of using embelia laeta to prepare bisexual antifertility material embelin

A technology of sour vine fruit and fimbesu, which is applied in the fields of diseases, drug combinations, organic chemistry, etc., can solve the problems of difficult industrial promotion of microwave technology, high cost, unfavorable environment and human health, etc., and achieves good industrialization prospects, Liver damage protection, effect of improving arterial clogged state

Inactive Publication Date: 2012-08-15
GUANGXI INST OF CHINESE MEDICINE & PHARMA SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The traditional extraction of benzoquinone components mostly uses organic solvents such as ether, which is costly and harmful to the environment and human health
Latha uses microwave technology to extract and separate (Biotechnol Lett.2007; 29(2): 319-22.) to obtain embesin, and microwave technology is difficult to promote industrialization

Method used

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  • Method of using embelia laeta to prepare bisexual antifertility material embelin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dry the ripe fruit, crush it into a powder with a particle size of 20-50 μm, put 50 g into an extraction tank, add a hydrotrope sodium cumene sulfonate solution (222 g / L) to 1272 g, and set the temperature at 30 ° C with a stirring speed of 800-1200 rpm Under extraction for 30 minutes, filter. Add 1000 ml of hydrotropic solvent solution to the dregs, stir and extract for 30 minutes, and filter. The dregs were repeatedly extracted 5 times, and the combined filtrate was about 5000ml. The filtrate was diluted by adding more than 50,000 ml of acid water with pH 4.0, and left for 30 minutes. Orange crystals precipitated. The crystals were separated by centrifugation at 5,000 rpm for 15 minutes. The crystals were washed with water and dried in vacuo to obtain embesin crystals. Adsorption and decolorization with activated carbon yielded high-purity fimbesin (mp142-143°C).

Embodiment 2

[0023] Dry the ripe fruit, crush it into a powder with a particle size of 60-80 μm, put 50 g into the extraction tank, add a hydrotrope sodium cumene sulfonate solution (444 g / L) to 1494 g, at a temperature of 30 ° C, and a stirring speed of 800-1200 rpm Under extraction for 30 minutes, filter. Add 1000 ml of hydrotropic solvent solution to the dregs, stir and extract for 30 minutes, and filter. The dregs were repeatedly extracted 5 times, and the combined filtrate was about 5000ml. The filtrate was diluted by adding more than 50,000 ml of acid water with pH 4.0, and left for 30 minutes. Orange crystals precipitated. The crystals were separated by centrifugation at 5,000 rpm for 15 minutes. The crystals were washed with water and dried in vacuo to obtain embesin crystals. Adsorption and decolorization with activated carbon yielded high-purity fimbesin (mp142-143°C).

Embodiment 3

[0025] Dry the ripe fruit, crush it into a powder with a particle size of 80-100 μm, put 50 g into an extraction tank, add a water-soluble solvent cumene sulfonate sodium solution (666 g / L) to 1716 g, at a temperature of 30 ° C, and a stirring speed of 800-1200 rpm Under extraction for 30 minutes, filter. Add 1000 ml of hydrotropic solvent solution to the dregs, stir and extract for 30 minutes, and filter. The dregs were repeatedly extracted 5 times, and the combined filtrate was about 5000ml. Add more than 50000ml of pH4.0 acidic water to the filtrate to dilute, leave it for 30 minutes, orange-yellow crystals separate out, centrifuge at 5000rpm for 15 minutes to separate the crystals, wash the crystals with water, and dry them in a vacuum to obtain the embesin crystals (extraction rate 95%, purity 92%) , yield 2.8%). Adsorption and decolorization with activated carbon yielded high-purity fimbesin (mp142-143°C).

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Abstract

The invention discloses a method of using embelia laeta to prepare bisexual antifertility material embelin, which mainly includes the steps: drying ripe embelia laeta, crushing into powder, adding water soluble cosolvent, stirring, extracting, filtering, extracting dregs for five to ten times, combining filtrate, diluting the filtrate for standing by to enable orange-yellow crystal to seed out, centrifugally separating, washing with water and vacuum drying to obtain an embelin crystal product. The embelin has various pharmacological activities such as blood sugar reduction, islet cell protection, liver injury prevention, oxygenated free radical resistance, osteoproliferation prevention, convulsion proofing, middle cerebral artery occlusion improvement, cerebral anoxia protection, myocardial infarction prevention, wound healing promotion, oncogene inhibition, liver cancer prevention, cholinesterase inhibition, amylase activity inhibition, abirritation, ulcerative colitis prevention and the like except for the antifertility function. The method has the advantages that 1, the embelin obtained by the method is higher than 90% in purity, higher than 95% in extraction rate and 2.4-3.0% in yield; 2, the preparation conditions are simple, no organic solvent but only the water soluble cosolvent (reusable), a stirrer and a centrifuge are needed, and environment pollution is avoided; and 3, the method is technically mature, high in competitiveness, free of 'waste gas, waste water and industrial residue', and bright in industrial prospect.

Description

technical field [0001] The invention relates to the preparation of medicines, more specifically to the preparation method of the amphoteric anti-fertility substance nembesin. Background technique [0002] The disorderly expansion of the population leads to poverty and famine, especially in less developed countries and regions. Therefore, family planning has become a basic national policy for improving population quality and quality of life in underdeveloped countries and regions; in developed countries, people's requirements for quality of life are getting higher and higher, and population development is also spontaneously restricted. In order to effectively reduce the consequences of unwanted pregnancy and reduce the harm caused by abortion to women's bodies, the use of contraceptives is becoming more and more popular, and the market for high-efficiency, low-toxicity, and easy-to-use contraceptives is broad. [0003] Emergency contraception is currently the most used in th...

Claims

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Application Information

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IPC IPC(8): C07C50/28C07C46/10A61P15/16A61P15/18
Inventor 韦宝伟曾宪彪韦桂宁
Owner GUANGXI INST OF CHINESE MEDICINE & PHARMA SCI
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