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Preparation method and medical application of extract of monkshood reduced total alkali

An extract, the technology of Aconitum aconitum, applied in the field of extract preparation of Aconitum aconitum reduced total alkaloids, can solve the problems of poor druggability and small safety window of treatment, etc., and achieve the effect of low production cost, simple method and high alkaloid content

Pending Publication Date: 2021-06-11
NANJING TUOZHU PHARMA & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The aconitum extract prepared by the above method is still toxic, has a small safety window for treatment, and has poor druggability. Therefore, no Aconitum aconitum extract has been developed into a drug so far.
In the extraction process, in addition to the hydrolysis conversion of the ester bond, the use of the chemical properties of aconitine to change the number of methoxyl and hydroxyl groups in its structure through hydrolysis and reduction to produce a low-toxic Aconitum extract has not yet been reported.

Method used

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  • Preparation method and medical application of extract of monkshood reduced total alkali
  • Preparation method and medical application of extract of monkshood reduced total alkali
  • Preparation method and medical application of extract of monkshood reduced total alkali

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Cut the fresh roots of Aconiti officinalis into slices, 3 parts of fresh Aconitum aconitum slices, 0.05 parts of calcium hydroxide, add 8 parts of water to the first extraction, add to a frying pan, heat at 100°C for 60 minutes, and keep the medicinal liquid in alkaline pH9- 12. Filter out the medicinal liquid; add 7 parts of water to the second extraction, heat at 100°C for 30 minutes, filter out the medicinal liquid, combine the decoction, let stand for 6 hours, cool to 40-50°C, filter the supernatant, and flow the filtrate through the pre- The chromatographic column of the processed non-polar macroporous resin, the resin model is AB-8, the dosage is 0.5 times the amount of medicinal materials fed, and the flow rate is 0.1 times the resin volume / min. After completely flowing through the adsorption, wash with deionized water Remove the resin column, the elution volume is 8 times the volume of the resin, then elute the resin column with 15% ethanol, the elution volume of...

Embodiment 2

[0029] 1 part of aconite slices, 0.05 parts of sodium carbonate, add 10 parts of water for the first extraction, add to a frying pan, heat at 100°C for 60 minutes, keep the medicinal liquid at an alkaline pH9-10 during the extraction process, and filter out the medicinal liquid; extract the water for the second time Add 7 parts, heat at 100°C for 30min, filter out the medicinal solution, combine the decoction, let it stand for 6 hours, cool to 40-50°C, filter the supernatant, and the filtrate flows through the layer of pretreated non-polar macroporous resin Analysis column, the resin model is D101, the dosage is 0.5 times of the amount of medicinal materials fed, and the flow rate is 0.2 times of the resin volume / min. After completely flowing through the adsorption, the resin column is eluted with deionized water, and the elution volume is 4 times of the resin volume. Then elute the resin column with 15% ethanol, the eluting volume of alcohol solution is 4 times of the resin vo...

Embodiment 3

[0031] Get the total reducing bases of Aconitum in Example 1 and the total reducing bases of Aconite in Example 2, and be configured into a solution containing 7 mg / ml of total reducing bases of Aconitum and 7.5 mg / ml of total reducing bases of Aconitum respectively, and additionally prepare into a solution containing aconitine 0.01mg / ml; get 30 mice with a body weight of 20g, divide them into three groups, 10 in each group, and administer the above-mentioned aconitine total reducing bases, aconitum total reducing bases, aconitum total reducing bases, and Each 1ml of the head alkali solution / animal, observed the number of dead animals, and the experimental results are shown in Table 1. The results show that the toxicity of total reducing bases of aconitum is similar to that of total reducing bases of aconitum, and the toxicity of aconitine is more than 700 times lower than that of aconitine.

[0032] Table 1

[0033] group Number of mice administered in each group...

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Abstract

The invention discloses a preparation method and medical application of an extract of monkshood reduced total alkali, which comprises the following steps of: adding inorganic alkali in a monkshood water extraction process, and keeping the pH value of liquid medicine to be 9-12 alkalinity in a decoction reflux process, so that aconitine is converted into a new compound during extraction; a combined process of a macroporous resin refining process, impurity elution with a diluted alcohol solution, impurity elution with an acid water solution and component elution with an acidic diluted alcohol solution is adopted, diluted alcohol is an ethanol solution with the concentration of 20% or below, the process has the unexpected effects that the production safety is improved, the cost is reduced, and the prepared extract is high in alkaloid content and safer in production. The invention is composed of a process of converting an aconitine structure into a new compound through reflux extraction of a strong alkali solution and a process of macroporous resin refining and diluted alcohol elution, the prepared main components are the new compound, the ecognin and the 15-hydroxyl ecognin, the content of the ecognin and the 15-hydroxyl ecognin accounts for more than 50% of the total alkali, and the invention is low in toxicity and strong in drug effect and is used for preparing drugs for treating inflammation pain.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a method for preparing an extract of Aconitum reduced total alkaloids and its medical application. Background technique [0002] Aconitum carmichaeli Debx. is aconitum belonging to Ranunculaceae Aconitum. Its root is commonly used in traditional Chinese medicine. The processed and dried mother root is called "Aconitum carmichaeli Debx", and the processed and dried child root is called "Aconitum". The main producing area of ​​Chuanwu is Sichuan, and it has been planted in Sichuan for nearly a thousand years. The raw product of Aconitum Aconitum is highly toxic and belongs to the "very poisonous" class of traditional Chinese medicine. It has the functions of expelling wind and dampness, warming meridian and relieving pain. Generally, the steamed "Zhichuanwu" is used clinically, while the raw products are mostly for external use, such as ointment, tincture, etc., for t...

Claims

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Application Information

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IPC IPC(8): A61K36/714A61K31/439A61P29/00A61P19/02A61K125/00
CPCA61K36/714A61K31/439A61P29/00A61P19/02A61K2236/333A61K2236/331A61K2236/55A61K2236/51
Inventor 徐浩坤
Owner NANJING TUOZHU PHARMA & TECH
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