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Water soluble silymarin and its prepn

A silymarin and water-soluble technology, which is applied in the field of drug synthesis, can solve the problems such as the absence of water-soluble silymarin, and achieve the effect of enhancing water-solubility, avoiding difficult absorption, and low toxicity

Inactive Publication Date: 2007-08-22
李宝
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the silybin meglumine salt given in the above technical scheme can improve the bioavailability of the silybin meglumine inclusion compound, it still needs to be further improved in water solubility and stability, and no water-soluble salt has been found in the market. Relevant reports on silymarin as medicine

Method used

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  • Water soluble silymarin and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045]First put 3 kg of silymarin into the synthesis tank, dissolve it completely with ethanol and filter it, then dissolve 1.5 kg of meglumine, 0.7 kg of polyvinylpyrrolidone (PVP), and 0.3 kg of poloxamer 188 with ethanol, then filter it and add it while it is hot Mix and stir in the silymarin solution for 30 minutes, the temperature of the solution in the tank is 78°C, and reflux for 30 minutes after stirring, the temperature of reflux is 78°C, after the reaction, the solvent in the synthesis tank is concentrated in vacuum to obtain 7.3 kg of fluid extract, the temperature 60°C, vacuum degree -0.05Mpa, then put the liquid extract into the drying tank, preheat at 70-75°C for 30 minutes, start vacuuming, when the vacuum degree reaches -0.09Mpa, the temperature in the tank is 60-65 5.5 kilograms of water-soluble silymarin dry extracts were obtained after starting to dry for 3 hours at ℃, and the obtained water-soluble silymarin dry extracts were put back into the synthesis tank...

Embodiment 2

[0048] First put 5 kg of silymarin into the synthesis tank, dissolve it completely with ethanol and filter it, dissolve 2 kg of meglumine, 1 kg of polyvinylpyrrolidone (PVP), and 0.5 kg of poloxamer 188 with ethanol, then filter it and add it while it is hot Mix and stir in the silymarin solution for 30 minutes. The temperature of the solution in the tank is 78°C. After stirring, it is refluxed for 30 minutes. The temperature of reflux is 78°C. After the reaction, the solvent in the synthesis tank is vacuum concentrated to obtain 11.6 kg of liquid extract. 60°C, vacuum degree -0.05Mpa, then put the liquid extract into the drying tank, preheat at 70-75°C for 30 minutes, start vacuuming, when the vacuum degree reaches -0.09Mpa, the temperature in the tank is 60-65 8.6 kilograms of water-soluble silymarin dry extracts were obtained after starting to dry for 3 hours at ℃, and the obtained water-soluble silymarin dry extracts were put back into the synthesis tank, and ethanol was ad...

Embodiment 3

[0051] First put 7 kg of silymarin into the synthesis tank, dissolve it completely with ethanol and filter it, then dissolve 3 kg of meglumine, 1.5 kg of polyvinylpyrrolidone (PVP), and 0.8 kg of poloxamer 188 with ethanol, then filter it and add it while it is hot Mix and stir in the silymarin solution for 30 minutes, the temperature of the solution in the tank is 78°C, and reflux for 30 minutes after stirring, the temperature of reflux is 78°C, after the reaction, the solvent in the synthesis tank is concentrated in vacuum to obtain 16.5 kg of fluid extract, the temperature 60°C, vacuum degree -0.05Mpa, then put the liquid extract into the drying tank, preheat at 70-75°C for 30 minutes, start vacuuming, when the vacuum degree reaches -0.09Mpa, the temperature in the tank is 60-65 12.5 kilograms of water-soluble silymarin dry extracts were obtained after drying for 3 hours at ℃, and the obtained water-soluble silymarin dry extracts were re-dropped into the synthesis tank, and ...

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Abstract

The water soluble silymarin preparation consists of silymarin, meglumine, PVP and poloxamer. It is prepared through dissolving silymarin and cosolvent in ethanol, filtering, reflux reaction and concentrating to obtain extractum; drying to obtain dry paste; redissolving, vacuum concentrating to crystallize, suction filtering to obtain crystal; ethanol washing, suction filtering, re-crystallizing and drying to obtain crystal; crushing, mixing and packing to obtain the water soluble silymarin preparation. The present invention features high water solubility, high stability and high bioavailability.

Description

technical field [0001] The invention relates to a medicinal derivative and a preparation method thereof, in particular to a water-soluble silymarin and a preparation method thereof, belonging to the technical field of drug synthesis. Background technique [0002] Silymarin is a lignin flavonoid compound extracted and isolated from the fruit of Silybum marianum, a plant of the genus Milk thistle in the family Asteraceae. It has obvious functions of protecting and stabilizing liver cell membranes, and can promote liver cell regeneration. The damage has protective and therapeutic effects in different degrees, and the Yiganling tablet sold on the market is a single preparation of silymarin. Since silymarin itself is a flavonoid compound that is insoluble in water, there are problems affecting the dissolution rate and bioavailability of the drug after it is made into a preparation, which seriously affects the efficacy of the drug. There is also a silybin meglumine tablet on the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61K47/18A61K47/34A61P1/16A61K47/10A61K47/32
Inventor 李宝
Owner 李宝
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