Preparation method and pharmaceutical application of nux vomica total alkaloids

A technology of total alkaloids and strychnids, which is applied to the preparation of total alkaloids of Chinese medicinal materials strychnids, and the field of treating rheumatism, can solve the problems of difficulty in realizing large-scale industrial production, large loss of alkaloid components, low product yield and the like , to achieve the effect of improving bioavailability, enhancing inhibitory effect and improving product yield

Inactive Publication Date: 2014-07-09
ZHEJIANG UNIV OF TECH +2
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Problems solved by technology

[0004] Cai Baochang and others from Nanjing University of Traditional Chinese Medicine have fine-tuned the general knowledge of the current academic circles, and believe that although it is possible to completely remove strychnine, the cost is high and the loss of other alkaloid components is also large, so it is difficult to achieve large-scale industrial production; and they Through further experimental research, it is found that if part of the strychnine in the total alkaloids can be removed, its toxicity can be reduced, and its original pharmacological activity can be basically retained, which has more feasibility and application prospects
For example, in its authorized Chinese invention patent (patent number ZL201010107295.4, application date is 2010.02.08, and the name of the invention is a method for extracting and purifying total alkaloids of Nuxebra chinensis and its application in pharmaceuticals), which discloses A method for purifying the total alkaloids of Strychnium by removing part of the strychnine in the total alkaloids of Strychnium, the technical scheme adopts different concentrations of ethanol to extract and purify, so as to obtain Strychnine with a low strychnine content Purified product of total alkaloids of Qianzi, however, the defect of this technical scheme is: ① using alcohol extraction method, the extraction efficiency is low, and the product yield is low
②The existing mode of treating rheumatic arthralgia is still not deviated from the current academic general knowledge, that is, strychnine is still treated as a toxic component, and it is still simply removed in whole or in part in the preparation of purified total alkaloids of Nuxebra chinensis The idea of ​​strychnine to extract and purify

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  • Preparation method and pharmaceutical application of nux vomica total alkaloids
  • Preparation method and pharmaceutical application of nux vomica total alkaloids
  • Preparation method and pharmaceutical application of nux vomica total alkaloids

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Embodiment 1

[0028] Embodiment 1: the preparation method of strychnine total alkaloids, wherein the mass ratio of strychnine and strychnine is 1:0.1:

[0029] (1) Weigh strychnine, pulverize, sieve (10 mesh) to obtain coarse powder, weigh 150g of coarse powder, and the mass ratio of strychnine and strychnine in the coarse powder is 1:2;

[0030] (2) Heating and refluxing extraction with 40% ethanol with a pH of 3.0 for 3 hours, a total of 2 times, adding 1500 mL of liquid each time, centrifuging, removing the precipitate, combining the 2 filtrates, and recovering ethanol under reduced pressure to obtain 1000 mL of concentrated solution ;

[0031](3) Add sodium hydroxide, adjust the pH to 14.0, extract 7 times with 4000 mL of dichloromethane, recover the solvent under reduced pressure, vacuum dry, and accurately weigh to obtain the total alkaloid powder of strychnids, which is determined by HPLC. The mass ratio of strychnine and strychnine is 1:2;

[0032] (4) Dissolve total strychnine al...

Embodiment 2

[0034] Embodiment 2: the preparation of strychnine total alkaloids, wherein the mass ratio of strychnine and strychnine is 1:0.4:

[0035] (1) Weigh strychnine, pulverize, sieve (20 mesh) to obtain coarse powder, weigh 150 g of coarse powder, and the mass ratio of strychnine and strychnine in the coarse powder is 1:2.1;

[0036] (2) Heating and refluxing extraction with 50% ethanol with a pH of 6.0 for 1 h, a total of 3 times, adding 2000 mL of liquid each time, centrifuging, removing the precipitate, combining the 3 filtrates, and recovering ethanol under reduced pressure to obtain a concentrated solution 1000mL;

[0037] (3) Add sodium hydroxide, adjust the pH to 12.0, extract 6 times with 4000 mL of dichloromethane, recover the solvent under reduced pressure, vacuum dry, and accurately weigh to obtain the total alkaloid powder of strychnids, which is determined by HPLC. The mass ratio of strychnine and strychnine is 1:2.1;

[0038] (4) Dissolve the total alkaloid powder o...

Embodiment 3

[0040] Embodiment 3: the preparation of strychnine total alkaloids, wherein the mass ratio of strychnine and strychnine is 1:1.0:

[0041] (1) Weigh strychnine, pulverize, sieve (40 mesh) to obtain coarse powder, weigh 100g of coarse powder, and the mass ratio of strychnine and strychnine in the coarse powder is 1:2.2;

[0042] (2) Extraction with 30% ethanol with a pH of 5.0 by heating and refluxing for 1 h for a total of 3 times, adding 1200 mL of liquid each time, centrifuging to remove the precipitate, combining the 3 filtrates, and recovering ethanol under reduced pressure to obtain a concentrated solution 1000mL;

[0043] (3) Add sodium hydroxide, adjust the pH to 12.0, extract 5 times with 4000 mL of dichloromethane, recover the solvent under reduced pressure, vacuum dry, and accurately weigh to obtain the total alkaloid powder of strychnids. The mass ratio of strychnine and strychnine is 1:2.2;

[0044] (4) Dissolve the total alkaloid powder of strychnids with a mixe...

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Abstract

The invention discloses a preparation method and a pharmaceutical application of nux vomica total alkaloids. The preparation method of the invention comprises the following steps: (1) crushing nux vomica, sieving with a sieve of 10-40 meshes to prepare coarse powder; (2) weighing 100g-200g of the coarse powder, performing heating reflux extraction with 1000mL-2000mL of alcohol acid solution, performing centrifugation, removing precipitates, recovering the alcohol acid solution at a reduced pressure to obtain a concentrate; (3) adding a pH adjusting agent, adjusting the pH value of the concentrate to 9-14, extracting with 3000mL-4000mL of an extraction solvent, recovering the solvent at a reduced pressure, drying at a reduced pressure to obtain nux vomica total alkaloids powder; (4) dissolving the nux vomica total alkaloids powder in a mixed acid solution, performing centrifugation to obtain the supernatant; (5) adding the pH adjusting agent, adjusting the pH value of the supernatant to 10-13, extracting with dichloromethane or ethyl acetate, recovering the solvent at a reduced pressure, and drying at a reduced pressure to obtain nux vomica total alkaloids. The purified product of nux vomica total alkaloids prepared in the invention can increase the transdermal rate of main drug components rapidly, improve the bioavailability, is low in toxicity, and has significant effect on treating rheumatic arthralgia.

Description

technical field [0001] The invention belongs to the technical field of extraction of traditional Chinese medicine ingredients, and in particular relates to a preparation method of total alkaloids of Chinese medicinal material strychnine and its pharmaceutical use, and the pharmaceutical use is mainly used in the treatment of rheumatic arthralgia. Background technique [0002] Strychnos nux-vomica L. or Strychnos Pierriana A.W.Hill is the dried and mature seed of Strychnos nux-vomica L. or Yunnan long-seed Strychnos Pierriana A.W.Hill. Compendium of Materia Medica, which are recorded in the previous editions of the Chinese Pharmacopoeia. Ma Qianzi has the functions of dredging collaterals and relieving pain, dispersing knots and reducing swelling. Traditional Chinese medicine treats rheumatism stubborn arthralgia, numbness and paralysis, falls and flutter injuries, carbuncle swelling and pain, etc.; It is used in Chinese patent medicines such as Yanggan Pills, Shangke Qiwei ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/56A61P29/00A61P19/02
Inventor 马凤森陈海波方多凤方剑乔梁宜
Owner ZHEJIANG UNIV OF TECH
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