Industrialized production method for efficiently extracting, separating and purifying serial cinchona alkaloid from cinchona bark

A technology of cinchona bark and cinchona, which is applied in the directions of organic chemistry, drug combination, cardiovascular system diseases, etc., can solve the problems of difficult industrialized large-scale production of alkaloids, high energy consumption, and low recovery rate of cinchona alkaloids extraction. , to achieve the effect of good extraction recovery

Inactive Publication Date: 2012-07-11
江苏斯威森生物医药工程研究中心有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] The present invention needs to solve the shortcomings of low extraction recovery rate of cinchona alkaloids in the prior art, high pollution, high energy consumption, and difficulty in industrializ

Method used

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  • Industrialized production method for efficiently extracting, separating and purifying serial cinchona alkaloid from cinchona bark
  • Industrialized production method for efficiently extracting, separating and purifying serial cinchona alkaloid from cinchona bark

Examples

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Embodiment 1

[0021] Embodiment 1 Preparation of quinine alkaloids

[0022] Get the cinchona bark with moisture content less than 3%, pulverize and cross 60 mesh sieves. Weigh 2 kg of cinchona bark powder, soak in 5 L of 5% sodium hydroxide solution, and ultrasonically break the cells for 1 h. Filter and dry to obtain cinchona bark powder, and the lye is recovered and recycled. Put the dried cinchona bark powder into a multi-functional extraction tank, and extract it twice with 16L industrial methanol, each time for 3.5h (the recovery rate of quinine alkaloid extraction detected by HPLC should be greater than 95%, otherwise, extract with 8L methanol 2h), filtered and concentrated to obtain cinchona bark methanol extract fluid extract, methanol recovery and recycling. Disperse the liquid extract above in 2L of water, adjust the pH value to 3.5 with concentrated sulfuric acid, and extract once with 1L of dichloroethane. The organic phase reclaims ethylene dichloride for recycling, the wate...

Embodiment 2

[0023] The preparation of embodiment 2 quinidine, cinchonidine and cinchonine

[0024] Continue to adjust the mother liquor from the previous step to a pH value of 12 with concentrated ammonia water, and continue to precipitate new precipitates from the mother liquor, and filter to obtain 4.6 kg of other total alkaloids. The total alkaloids were column chromatographed and eluted with a gradient of petroleum ether: ethyl acetate = 9:1 to 7:3 to obtain 1.6 kg of quinidine, 1.0 kg of cinchonidine and 1.2 kg of cinchonine respectively as main products. The contents detected by HPLC were all greater than 99.5%.

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Abstract

The invention discloses a method for preparing serial cinchona alkaloid with effects of malaria resistance, arrhythmia resistance and the like by adopting cinchona bark as a raw material. The method utilizes advanced ultrasonic cell disruption and extraction, simple extraction separation and high-purity column purification process to generate quinine sulfate, quinidine, cinchonidine and cinchonine, of which the purities are all higher than 99.5%. Compared with the traditional method, the method has higher extraction recovery and environment-friendly and low-carbon process flow, and is better applicable to industrial mass production of active ingredients at the grade of GMP (Good Manufacturing Practice and food additives).

Description

technical field [0001] The invention relates to a method for efficiently separating and purifying a series of cinchona alkaloids from cinchona bark produced in Africa and Southeast Asia. Cinchona alkaloids have a wide range of physiological and pharmacological activities such as treating malaria, arrhythmia and anti-inflammation. The extraction method uses advanced ultrasonic tissue cell crushing and extraction, simple extraction separation and high-purity column chromatography purification technology. Background technique [0002] The cinchona tree is also known as the cinchona tree, the quinine tree, and the cinchona tree. Contains about 25 species, belonging to evergreen shrubs or small trees, some of which are small shrubs, and some are large trees, with a height of about 2.5-3m. The origin comes from the Andes Mountains in South America. In the genus Cinchona, there are species such as red cinchona tree (C.succirubra), medicinal cinchona tree (C.officinalis) and west ...

Claims

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Application Information

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IPC IPC(8): C07D453/04A61P33/06A61P9/06A61P29/00
CPCY02A50/30
Inventor 彭学东王正濂龚福春张梅
Owner 江苏斯威森生物医药工程研究中心有限公司
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