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Process for extracting dioscin, preparation thereof and use

A technology of diosgenin and extract, which is applied in the field of preparation of drugs for the prevention and treatment of cardiovascular diseases, can solve the problems of uneven coating dispersion, slow drug effect, and affecting drug properties, and achieves low one-time investment cost and easy industrialization The effect of mass production and improvement of clarity

Active Publication Date: 2011-07-27
江苏黄河药业股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there are many methods for extracting diosgenin from Dioscorea scutellaria, most of which adopt the traditional method of water extraction and alcohol precipitation, or as in CN02146284.4, the method of ethanol reflux extraction, but most of them There is the problem of too many impurities in the method: because the natural plant extract contains starch, protein, pectin, gum, resin, mucus, etc. in addition to the extract components, the existence of these components often makes the extract be in a suspended state, And affect the filtration rate of the extract, for this reason to implement impurity removal, the commonly used methods have centrifugation, clarifying agent method, alcohol precipitation method, macroporous resin adsorption method, ion exchange method, micro-pore filter membrane filtration method and ultrafiltration, etc.
At present, most of them are produced by macroporous resin with strong polarity, so the adsorption capacity is small.
[0006] And the deficiencies that the coated tablet of prior art diosgenin exists in practical application are, (1) tablet core medicine stripping speed is slow, and medicine effective effect is slow; ) The color of the coating is unstable, and it is easily oxidized to affect the properties of the drug; (4) The dispersion of the coating is not uniform, and the poor coverage leads to the loss of the smell of the drug, which affects the therapeutic effect of the drug

Method used

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  • Process for extracting dioscin, preparation thereof and use
  • Process for extracting dioscin, preparation thereof and use
  • Process for extracting dioscin, preparation thereof and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Comparative experiment on the preparation of dioscin by multifunctional scouring enzyme DMA enzymatic hydrolysis and weak polar macroporous resin extraction method (referred to as compound extraction method) and enzymatic hydrolysis method

[0045] Experiment 1: Take 25g of dried Dioscorea scutellaria powder, add quantitative water to a three-necked flask, stir evenly, add 0.1% cellulase and pectinase compound enzyme preparation at a temperature of 50°C for 12 hours, and then add a certain amount of Concentrated H 2 SO 4 Prepare 2 mol / L hydrolyzate at 100°C for 4 hours, filter, wash the filter residue with 10% NaOH solution until neutral, dry, and grind to obtain a powder extract. After the extract was reflux extracted for 8 hours with a Soxhlet extractor, the extract was concentrated with a rotary evaporator and the product was crystallized, and finally dried in a vacuum oven at 80-100°C to obtain dioscin, and the yield and melting point of the obtained product were d...

Embodiment 2

[0051] Take 2kg of dry Dioscorea scutellaria powder, add a certain amount of water, stir evenly, add 30g / L of multifunctional scouring enzyme DMA dissolved in 30°C water, then add cold water to adjust the water amount, add the required 8g / L hydrogen peroxide and wash agent, stir evenly, heat up to 70°C and keep warm for 50min to obtain the extract;

[0052] Add 6 times the amount of water to the obtained extract, heat and reflux to extract twice, each time for 1 hour, filter, combine the extracts, and concentrate to 0.25g crude drug / ml; after filtering, pass through AB-8 macroporous resin, and extract the extract according to dioscin The ratio of the content meter to the dry resin is 1:5, the column flow rate is 1BV / h, and the diameter of the resin is 1:3; the resin is washed with water for 3BV, and the elution flow rate is 2BV / h, and the water eluent is discarded; % water-containing ethanol to elute 8BV, the flow rate is 2BV / h, and the ethanol eluate is collected; the ethanol...

Embodiment 3

[0054] Take 1kg of dry Dioscorea baicalensis powder, add a certain amount of water, stir evenly, add multifunctional scouring enzyme DMA15g / L dissolved in 60°C water, then add cold water to adjust the water amount, add the required 10g / L hydrogen peroxide and wash agent, stir evenly, and heat up to 80°C for 60 minutes to obtain the extract;

[0055] Add 15 times the amount of 30% ethanol to the obtained extract, heat and reflux to extract 4 times, each time for 3 hours, filter, combine the extracts, and concentrate to 2.0g crude drug / ml; The ratio of the diosgenin content meter to the dry resin is 1:10, the upper column flow rate is 4BV / h, and the diameter of the resin is 1:9; the resin is washed with water for 8BV, and the elution flow rate is 4BV / h, and the water eluent is discarded; Contain 95% aqueous ethanol for elution, flow rate is 4BV / h, collect ethanol eluate; ethanol eluate is concentrated under reduced pressure to a relative density of 1.25, and dried under reduced ...

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Abstract

The invention relates to a method for extracting dioscorea zingiberensis diosgenin in traditional Chinese medicine peltate yam, a preparation agent, and the application of the dioscorea zingiberensis diosgenin in preparing drugs in prevention and treatment of cardiovascular diseases. The dioscorea zingiberensis diosgenin extraction method of the invention adopts enzyme to remove coarse impurities, and then uses weak-polar macroporous resin to extract the dioscorea zingiberensis diosgenin. The method of the invention can significantly improve the purity and extraction rate of dioscorea zingiberensis diosgenin to reduce the production cost. The dioscorea zingiberensis diosgenin of the invention can also prepare coated tablets, syrup, oral solution, drops or capsules; compared with the priorart, the dioscorea zingiberensis diosgenin prepared through the method of the invention has better efficacy and is conducive to the transport and storage. Clinical trials prove that the dioscorea zingiberensis diosgenin extracted in the invention has a significant effect on coronary heart disease, hyperlipidemia and other cardiovascular diseases.

Description

technical field [0001] The invention relates to a process for extracting diosgenin from the traditional Chinese medicine Dioscorea punctatus, a pharmaceutical preparation and a preparation method thereof, and its application in the preparation of drugs for preventing and treating cardiovascular diseases, belonging to the field of traditional Chinese medicines. Background technique [0002] Rhizoma Dioscoreae Zingiberensis is the rhizome of Dioscorea Zingiberensis (Latin name Dioscorea Zingiberensis C.H.Wright), a plant of the Dioscorea family. Rhizoma Dioscoreae Zingiberensis has the functions of promoting blood circulation and relaxing tendons, digestion and diuresis, and is rich in steroidal saponins. [0003] Dioscorea saponin is extracted from medicinal Dioscorea scutellaria and pangolin, etc. It has the characteristics of clear chemical structure and high oral absorption and availability. In the prior art, there are many methods for extracting diosgenin from Dioscorea s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/7048A61K36/8945A61K9/36A61P9/00
Inventor 葛海涛张杰
Owner 江苏黄河药业股份有限公司
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