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Water-soluble silymarin and preparation method thereof

A silymarin and water-soluble technology, which is applied in the direction of pharmaceutical formulations, organic active ingredients, and medical preparations containing active ingredients, can solve the problem of fat-soluble silymarin solvent residues, low solubility and bioavailability of active ingredients, and difficulty in making Intravenous injections and other issues, to achieve the effect of improving bioavailability, improving production efficiency, and improving resource utilization

Inactive Publication Date: 2011-06-08
江苏健佳药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many deficiencies in the application of this fat-soluble silymarin: first, fat-soluble silymarin has the defect of high residual solvent, and the residual amount of acetone, ethyl acetate or n-hexane is all above 20000PPm, far exceeding the national standard of acetone or Ethyl acetate does not exceed 5000ppm, and n-hexane does not exceed 290ppm; moreover, acetone or ethyl acetate are harmful and dangerous chemicals that can paralyze the human nervous system, and inhalation of acetone vapor can cause headaches and vertigo , vomiting and other symptoms, high-concentration ethyl acetate vapor can cause liver and kidney congestion, and then cause acute pulmonary edema; n-hexane also has strong anesthetic properties; therefore, the existing preparation solvents of silybum are extremely harmful to the human body. great danger
Second, fat-soluble silymarin is insoluble in water, and the active ingredients are not suitable for absorption by the human body. After being made into preparations, there are defects of low solubility and bioavailability of active ingredients and poor drug stability.
Third, since fat-soluble silymarin is insoluble in water, it is mainly used to make capsules or tablets, which is difficult to make into intravenous injections and difficult to use in food and health products
Although the milk thistle meglumine salt obtained by the above method can enhance its water solubility and solubility, thereby improving its bioavailability, this method not only does not solve the solvent residue problem of fat-soluble silymarin, but also brings new problems. Residual problems of organic solvents such as methanol
Moreover, although the effect of milk thistle meglumine salt is very close to that of silymarin, its main components and effects still need to be further studied, and the stability and effectiveness of its drug action still need to be further improved.
Therefore, there is no directly prepared water-soluble silymarin product of substantial significance on the market

Method used

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  • Water-soluble silymarin and preparation method thereof
  • Water-soluble silymarin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The milk thistle seeds are first screened to remove impurities, and then the oil is squeezed out with a screw oil press to form milk thistle cakes. The milk thistle oil is for sale; the milk thistle cakes are in the shape of round cakes, and the outer diameter of the round cakes is 110mm, and the thickness is controlled Between 1.5mm±0.2mm; milk thistle cake for later use.

[0025] Put 500 kg of silymarin cake after oil removal into the extraction tank, and put into the extraction tank 4000 kg of lye ethanol with a weight ratio of 1:8; the lye ethanol is thrown into the ethanol solution with solid NaOH and mixed Forming, the weight percent concentration of ethanol solution is 30%, promptly contains the NaOH of 30% ethanol solution 97kg and 3kg in every 100kg alkali water ethanol. The pH of the alkaline water ethanol is 8.3. Heat the mixture of alkaline water ethanol and milk thistle cake in the extraction tank to 80° C., keep the temperature at a constant temperature f...

Embodiment 2

[0030] After the milk thistle seeds are screened to remove impurities, the oil is squeezed out with a mechanical oil press, and the milk thistle oil is sold; the squeezed milk thistle cake is preliminarily crushed for later use.

[0031] Put the milk thistle cake after the oil is squeezed into the extraction tank, and fill the extraction tank with the alkali water ethanol in the ratio of the milk thistle cake to the alkali water ethanol weight ratio of 1:7. Alkaline ethanol is mixed by ethanol solution and solid NaOH, and the weight percentage of its ethanol solution is 25%, contains 25% ethanol solution 96kg, NaOH4kg in every 100kg alkali ethanol, alkali water ethanol PH=8.5. Heat the mixture of alkaline water ethanol and milk thistle cake in the extraction tank to 85° C., keep the temperature at a constant temperature for 1.5 hours, and then extract twice continuously to obtain milk thistle extract.

[0032] The milk thistle extract is transported to the clathrate tank, and th...

Embodiment 3

[0036] After the milk thistle seeds are screened to remove impurities, the oil is squeezed out with a mechanical oil press, and the milk thistle oil is sold; the squeezed milk thistle cake is preliminarily crushed for later use.

[0037] Put the milk thistle cake after the oil is squeezed into the extraction tank, and fill the extraction tank with the alkali water ethanol in the ratio of the milk thistle cake to the alkali water ethanol weight ratio of 1:9. Alkaline ethanol is mixed by ethanol solution and solid NaOH, and the weight percent of its ethanol solution is 35%, contains 35% ethanol solution 98kg, NaOH 2kg in every 100kg alkali ethanol, alkali water ethanol PH=8. Heat the mixture of alkaline water ethanol and milk thistle cake in the extraction tank to 75° C., keep the temperature at a constant temperature for 2.5 hours, and extract continuously for 4 times to obtain milk thistle extract.

[0038] The milk thistle extract is transported to the clathrate tank, and the...

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Abstract

The invention discloses water-soluble silymarin, which is an inclusion compound that takes cyclodextrin as main molecules and silymarin as guest molecules; and the inclusion compound contains 12 to 20wt % of silybinin. The preparation method thereof comprises the following steps: silybum marianum seeds are squeezed into silybum marianum cakes; the silybum marianum cakes are added into alkali water ethanol solution and are heated to 75DEG C to 85DEG C, the constant temperature is kept for 1.5-2.5 hours, and silybum marianum extracting solution is prepared after 2-4 times of continuous extraction; the silybum marianum extracting solution is added with the cyclodextrin for inclusion, thus obtaining inclusion compound solution; flocculant is added, standing after being well stirred; after flocculate is filtered out, membrane separation process is carried out, thus obtaining water-soluble silymarin solution; and after the membrane separation process, the water-soluble silymarin solution isconcentrated and dried, thus obtaining the dried product of the water-soluble silymarin. The water-soluble silymarin prepared by the method has the advantages of high solubility, good quality, good drug stability and high bioavailability.

Description

technical field [0001] The invention relates to the extraction of silymarin, an active ingredient in the medicinal plant milk thistle of Compositae, in particular to water-soluble silymarin and its extraction and preparation method. Background technique [0002] Milk thistle is an excellent liver-protecting plant, and its seeds contain flavonoids - silymarin. Silymarin contains flavonoids such as silybin, iso-silibinin, silybinin and silybin, and its main component, silybin, has anti-oxidant free radicals, anti-lipid peroxidation, and protection of liver cell membranes , anti-hepatic fibrosis, etc., thereby improving the detoxification ability of the liver and protecting the liver; at the same time, silymarin also has a significant effect on some diseases of the cardiovascular system such as hyperlipidemia; preparation. [0003] At present, the preparation of silymarin all uses acetone, ethyl acetate or n-hexane as a solvent to extract fat-soluble silymarin. There are man...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P9/00A61P3/06A61K47/40A61P1/16A61K131/00A61K36/28A61K31/357
Inventor 周勇徐柏衡
Owner 江苏健佳药业有限公司
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