阅读说明：本技术 一种双阶马钱子炮制品提取物及其制备方法 (Double-order nux vomica processed product extract and preparation method thereof ) 是由 秦伟瀚 阳勇 李卿 王云红 郭延垒 于 2019-10-25 设计创作，主要内容包括：本发明提供了一种双阶马钱子炮制品提取物,其双阶马钱子炮制品提取物的活性成分为士的宁和马钱子碱与生姜中酚性或弱酸性成分发生反应生成的生物碱。本发明提供的双阶马钱子炮制品提取物克服了马钱子提取物留存少量士的宁和马钱子碱的缺陷；减少了体积,为马钱子炮制品的剂型开发创造了条件。(The invention provides a double-order nux vomica processed product extract, wherein the active ingredients of the double-order nux vomica processed product extract are strychnine and alkaloid generated by the reaction of strychnine and phenolic or weakly acidic ingredients in ginger. The double-stage processed nux vomica product extract provided by the invention overcomes the defect that a small amount of strychnine and strychnine is remained in the nux vomica extract; the volume is reduced, and conditions are created for the formulation development of the processed products of nux vomica.)

1. A preparation method of a processed product extract of nux vomica is characterized by comprising the following steps: the method comprises the following steps:

1) weighing semen Strychni, rhizoma Zingiberis recens and semen Phaseoli Radiati according to weight ratio, adding water, and boiling with strong fire for 60 min;

2) taking out semen Strychni, oven drying at 80 deg.C, and scalding with sand to obtain processed semen Strychni;

3) processing semen Strychni, pulverizing, extracting with ethanol solution of pH5 under reflux to obtain extractive solution;

4) recovering ethanol from the extracting solution, adjusting the pH value to 2-3 by using hydrochloric acid, filtering, adjusting the pH value of the filtrate to 9-10 by using ammonia water, evaporating by using a water bath, and drying to constant weight to obtain the double-order nux vomica processed product extract.

2. The method for preparing the processed product extract of nux vomica as claimed in claim 1, wherein: in the step 1), the mass ratio of the nux vomica to the ginger to the mung bean to the water is 10:20:1: 150.

3. The method for preparing the processed product extract of nux vomica as claimed in claim 1, wherein: and 3) adding 50% ethanol solution with the pH of 5, which is 6 times of the amount of the nux vomica seeds, heating and refluxing for 3 times, extracting for 1 hour each time, and combining ethanol extracting solutions to obtain an extracting solution.

4. The processed product extract of nux vomica is characterized in that: an extract of the processed product of nux vomica prepared by the method of any one of claims 1 and 3.

5. The processed double-rank nux vomica extract according to claim 4, wherein: the active ingredients of the processed product extract of nux vomica are strychnine and alkaloid generated by the reaction of strychnine and phenolic or weakly acidic ingredients in ginger.

Technical Field

The invention relates to a traditional Chinese medicine extract, in particular to a nux vomica concocted product extract.

Technical Field

Semen Strychni is dried mature seed of Strychni Pulveratum (S t r y h o n S nux-vomica L.) and semen Strychni (S.Wallichiana Steudex D.C.: S.p ieriana.). Contains alkaloid 2-5%, mainly strychnine and strychnine. Strychnos nux-vomica is bitter in taste, cold in nature and toxic. It enters liver and spleen meridians. Has effects in dispersing pathogen accumulation, relieving swelling, dredging meridians, and relieving pain; is used for treating rheumatism, numbness, paralysis, carbuncle, swelling and pain, and traumatic injury. In the records of Yi Xue Zhong Can xi Lu, nux vomica is superior to other herbs in that it can open meridians and collaterals and reach joints thoroughly. The clinical application of nux vomica is not declined for nearly a thousand years, which shows that the nux vomica has obvious curative effect and can be called 'Duyaqiang agent good for Jiechu'. But at the same time, because it is a toxic drug, the clinical application of the medicine is greatly limited.

The therapeutic dose of raw nux vomica is very close to the toxic dose, so the nux vomica needs to be processed firstly. The processing of Chinese herbs has been done by sand-scalding, frying, processing with licorice, soaking in vinegar, and burst-pressing, and the common purpose is to reduce toxicity. Modern multiple toxicological experimental studies prove that the various processing methods have exact attenuation function. Studies by chenchenchenille et al show that: the processing has certain influence on strychnine and strychnine content. The toxicity can be reduced by processing with vinegar, frying and processing with liquorice; the content of strychnine and strychnine in vinegar-soaked products is greatly reduced, the toxicity is reduced, but the titer can also be reduced. The sand scald product contains higher amount of strychnine and strychnine than the raw product. Ding's and the like process the raw nux vomica by using a popcorn machine, which proves that the content of strychnine is lower by a bursting method compared with a sand ironing method, thereby improving the clinical medication safety and curative effect of the processed nux vomica product. Chen Shi et al used 4 different herba Ephedrae preparata methods to process semen Strychni, determined the contents of strychnine and strychnine in different processed semen Strychni products, and conducted acute toxicity, analgesic effect and antiinflammatory effect research. The results show that: 4 kinds of Chinese ephedra processed nux vomica processed by different methods have lower toxicity than the unprocessed nux vomica and the sand-heated product prepared by the pharmacopeia method, and a large number of researches show that the toxicity of the processed nux vomica is reduced, compared with the unprocessed product, the safety of the processed nux vomica is improved, and the clinical application of the nux vomica is expanded. The research results show that the processing purposes of the nux vomica are to reduce toxicity and increase curative effect and application range, and the traditional processing method is low in cost, but the attenuation effect is not ideal, and the operation is complex and time-consuming, so that a novel processing method which has exact curative effect and can greatly reduce the toxicity is needed.

Semen Strychni contains alkaloid, loganin, Doudouchun glycoside, chlorogenic acid, palmitic acid, fatty oil, protein, and polysaccharide. Wherein the total alkaloid accounts for 2 to 5 percent and is the main component. Mainly stryehnine (stryehnine) accounting for about 50% of the total alkali content, and Brucine (Brucine) content accounting for 30% -40%. And small amount of alkaloids such as isostrychnine, isomannine, pseudostrychnine, strychnine oxynitride, loganin, nuxvomicin, colubulin, Nofadrogen, Icaritin, strychnine oxynitride, and 2-hydroxy-3-methoxy brucine. Wherein strychnine and strychnine are the main active ingredients and toxic ingredients, and are also the ingredients which are researched more at present. Literature studies suggest that strychnine and strychnine content is reduced and isostrychnine, isomannine, strychnine oxynitride and strychnine oxynitride content are increased after raw strychnos nux-vomica is subjected to sand-ironing, and it is inferred that strychnine and strychnine are probably converted. Therefore, modern new analysis technology is necessary to deeply research the change and migration of the chemical components of the nux vomica and the processed products thereof, and the material bases of different processing methods can be more comprehensively explained.

Modern pharmacological studies show that nux vomica has the effects of exciting the central nervous system, treating cardiovascular system, resisting inflammation, treating immune system, resisting tumor, relieving pain, relieving cough, eliminating phlegm, relieving asthma, inhibiting bacteria, resisting arrhythmia and the like. The therapeutic dose of nux vomica can improve the excitation process and the inhibition process of cerebral cortex. The toxic dose can make cerebral cortex generate various time phase states, and severe poisoning can cause convulsion of whole body muscle spasticity and gradually leads to death of respiratory muscle spasm contraction asphyxia. Reports have shown that both strychnine and strychnine in extremely large doses prevent the action of cholinesterase on acetylcholine. Nux vomica can also directly damage renal tubular epithelial cells, resulting in acute renal failure and uremia. The researches prove that the nux vomica has definite curative effect but strong toxicity, and the clinical application of the nux vomica is greatly limited, so that a new processing method needs to be developed to achieve the aims of reducing toxicity and improving efficacy.

The applicant and the research team thereof carry out deep research on the attenuation and synergism mechanism of the new nux vomica processing technology, and research results show that a new nux vomica processing technology with two stages is obtained, and a Chinese patent 'a two-stage nux vomica processing method (application number: 201811157918.1)' is applied in 2018, 9, and 30 days; the research aims at improving the chemical structures of strychnine and strychnine which are main active ingredients in nux vomica by a new processing technology so as to achieve the aims of reducing toxicity and improving efficacy. However, the processed nux vomica products still contain a small amount of strychnine and strychnine, and the traditional processed nux vomica decoction pieces also limit the formulation development and clinical application of nux vomica.

Disclosure of Invention

Aiming at the problems, the invention provides a preparation method of a double-order nux vomica processed product extract, which comprises the following steps:

1) weighing semen Strychni, rhizoma Zingiberis recens and semen Phaseoli Radiati according to weight ratio, adding water, and boiling with strong fire for 60 min;

2) taking out semen Strychni, oven drying at 80 deg.C, and scalding with sand to obtain processed semen Strychni;

3) processing semen Strychni, pulverizing, extracting with ethanol solution of pH5 under reflux to obtain extractive solution;

4) recovering ethanol from the extracting solution, adjusting the pH value to 2-3 by using hydrochloric acid, filtering, adjusting the pH value of the filtrate to 9-10 by using ammonia water, evaporating by using a water bath, and drying to constant weight to obtain the double-order nux vomica processed product extract.

In the step 1), the mass ratio of the nux vomica to the ginger to the mung bean to the water is 10:20:1: 150.

And 3) adding 50% ethanol solution with the pH of 5, which is 6 times of the amount of the nux vomica seeds, heating and refluxing for 3 times, extracting for 1 hour each time, and combining ethanol extracting solutions to obtain an extracting solution.

A processed product extract of nux vomica is the processed product extract of nux vomica prepared by any one of the methods.

The active ingredients of the processed product extract of nux vomica are strychnine and alkaloid generated by the reaction of strychnine and phenolic or weakly acidic ingredients in ginger.

The beneficial technical effects of the invention are as follows: 1. the double-stage processed nux vomica product extract provided by the invention overcomes the defect that a small amount of strychnine and strychnine is remained in the nux vomica extract;

2. the volume is reduced, and conditions are created for the formulation development of the processed products of nux vomica.

Drawings

FIG. 1 is a process diagram for establishing a quality loss method;

FIG. 2 is a diagram of the filtration of strychnine and strychnine with mass loss of mother nucleus;

FIG. 3 is a score plot before and after molding;

FIG. 4 shows front and rear opls-da diagrams of molding.

Detailed Description