Processing method of aconitine hydroxyl reduction structure converted aconitine traditional Chinese medicine decoction pieces

A technology of aconitine hydroxyl group and Chinese herbal decoction pieces, which is applied in medical formulas, medical preparations containing active ingredients, organic chemistry, etc., and can solve problems such as harsh reduction reaction conditions, complex reaction products, and weak selectivity. Simple, single reaction product, and easy-to-control conditions

Inactive Publication Date: 2021-07-02
NANJING TUOZHU PHARMA & TECH
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The structure of head alkaloids is multiple hydroxyl compounds. Hydroxyl acetylation reduces its hydrophilicity and toxicity, and hydroxyl reduction can reduce hydrophilicity more effectively. However, due to the harsh conditions of the reduction reaction of hydroxyl groups, the selectivity is weak and the reaction products are complex. Therefore, the structural modification of aconitine for the purpose of reducing its hydrophilicity has not been reported yet.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Processing method of aconitine hydroxyl reduction structure converted aconitine traditional Chinese medicine decoction pieces
  • Processing method of aconitine hydroxyl reduction structure converted aconitine traditional Chinese medicine decoction pieces
  • Processing method of aconitine hydroxyl reduction structure converted aconitine traditional Chinese medicine decoction pieces

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Take 8kg of sodium carbonate, put it in a bucket, add 40L of deionized water, stir to dissolve, and get lye; take 10kg of raw aconitum slices, put them in the above-mentioned 20% sodium carbonate solution, soak for 12hr, take out the moistened decoction pieces, and drain them. Let it moisten for 3 hours, put it in a steamer, steam for 60 minutes under normal pressure, steam through the heart, take it out, and dry it under reduced pressure at 60°C to obtain concentrated alkali-made Aconitum slices. Benzoyl aconitine, aconitine reference substance, and the methanol solution of aconine and 15-hydroxyecgonine prepared separately were used as controls, and the methanol ultrasonic extract of alkali-made aconitum tablets was analyzed by HPLC. Chromatographic conditions: C18 filler, 250mm*4.5mm column, flow rate 1ml / min, ELSD detector (gas flow rate 2.8mL / min, drift tube temperature 110°C), chromatographic gradient is shown in Table 1, and the chromatogram is as follows figure ...

Embodiment 2

[0038] Take 7kg of sodium carbonate and 1kg of sodium hydroxide in a bucket, add 40L of deionized water, stir and dissolve to obtain lye; take 10kg of Aconitum aconitum slices, put them in the above-mentioned 20% alkali solution, soak for 12hr, take out the moistened The decoction pieces were moistened for 3 hours, placed in a steamer, steamed at normal pressure for 60 minutes, steamed through the heart, taken out, and dried at 60°C under reduced pressure to obtain Aconitum aconitum tablets made with concentrated alkali. The methanol solution of benzoyl aconitine and aconitine reference substance was used as the control, and the methanol ultrasonic extract of Aconitum aconitum prepared by alkali was injected and analyzed by HPLC. The chromatographic conditions are as in Example 1, and the results are as follows figure 2 .

[0039] The results showed that aconitine and benzoylaconitine were not detected in Concentrated Alkali-Prepared Aconitum Tablets by HPLC-ELSD method.

Embodiment 3

[0041] Take 5 kg of Aconitum slices made from medium-concentrated alkali, put them in a frying pot, add 50 L of water, heat and decoct for 60 minutes, and filter out the medicinal liquid; add 35 L of water to the dregs of the medicine in the pot, heat and decoct for 30 minutes, and filter out the medicinal liquid , combine the filtrates, let stand for 6 hours, filter the supernatant, cool to 40-50°C, and filter; take 2.5L pretreated AB-8 large-pore resin, put it into a chromatography column, wash with water to remove air bubbles, and put the filtrate on the resin column , the flow rate of the liquid medicine is 250ml / min. After the liquid medicine is exhausted, use 25L of deionized water to elute to remove inorganic substances, and then use 10L of 15% ethanol to elute; 10L of 15% ethanol solution was used for elution, the eluate was collected, the solvent was recovered, and dried under reduced pressure to obtain total aconitine of aconitum.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a processing method of aconitine hydroxyl reduction structure converted aconitine traditional Chinese medicine decoction pieces. According to a novel hydroxyl reduction reaction method in an aconitine structure, the reduction reaction of aconitine in processing is that 1-methoxyl hydrolysis and 3, 13, 15-hydroxyl reduction are carried out while ester bond alkali hydrolysis is carried out; under the condition, benzyl aconitine, aconitine and other aconitine compounds without ester bonds are not reduced. According to the invention, the toxic component aconitine in aconite, kusnezoff monkshood root and aconitum brachypodum can be converted, and the effective components such as sonchin in the kusnezoff monkshood root and aconitum brachypodum A in the aconitum brachypodum can be retained, so that the purposes of toxicity reduction and synergism can be achieved. The invention accidentally finds that the reaction occurs in decoction piece processing, the conditions are easy to control, the selectivity is strong, the product yield is high, the method is simple, the cost is low, the method is suitable for large-scale production, the reaction product is single, and the method can be used for preparing the aconitum traditional Chinese medicine low-toxicity decoction pieces.

Description

technical field [0001] The invention belongs to the technical fields of chemistry and pharmacy, and in particular relates to a method for processing Chinese herbal decoction pieces of the genus Aconitum obtained by transforming the hydroxyl group reduction structure of aconitine. Background technique [0002] Chemically, the reaction in which the oxidation number of a substance is reduced (gaining electrons) is called a reduction reaction. The essence of the reaction is that the oxidation number changes, that is, the electrons are transferred, and the actual effect is that the total oxidation state of the carbon atoms in the organic molecule is reduced. There are mainly catalytic hydrogenation reactions, chemical reduction reactions, and biological reduction reactions. Bioreduction generally utilizes biological or enzymatic reactions, which are difficult to apply to chemical structure modification. Catalytic hydrogenation requires a reduction reaction between an organic com...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/714C07D221/22A61K125/00
CPCA61K36/714A61K2236/10C07D221/22
Inventor 徐浩坤
Owner NANJING TUOZHU PHARMA & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap