Development of micro particle silybum marianum preparation

A technology of silymarin and micronization, which is applied in pill delivery, digestive system, antiviral agent, etc., can solve the problems of cost increase, low bioavailability of silymarin, environmental pollution, etc.

Inactive Publication Date: 2005-05-18
董诗文 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the problem of low bioavailability of silymarin is mainly solved from two aspects: 1. Preparation of water-soluble derivatives of silymarin. At present, the more common water-soluble derivatives of silymarin include silybin meglumine, silybin phosphate monophosphate, etc. However, the current research shows that the clinical efficacy of silymarin often decreases after making derivatives (Vladimír Kren, Jirí Kubisch. Glycosylation of silybin. J. Chem. Soc., Perkin Trans. 1, 1997: 2467-2474); in addition, the derivatization reaction involves chemical synthesis, resulting in increased cost and environmental pollution
At present, there is no report on the application of micronization technology in the production process of milk thistle preparations

Method used

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  • Development of micro particle silybum marianum preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1. Preparation of silymarin-phospholipid solid dispersion

[0045] Weigh 100g of medicinal-grade phospholipids, add 600ml of absolute ethanol, stir thoroughly to completely dissolve the phospholipids in the solvent; then add 100g of silymarin, sonicate and moderately heat to completely dissolve the silymarin; filter while hot; take the filtrate and evaporate under reduced pressure at 60°C Ethanol; vacuum drying at 60°C to remove residual solvent; pulverization to obtain a silymarin-phospholipid solid dispersion.

Embodiment 2

[0046] Example 2. Preparation of silymarin-poloxamer solid dispersion

[0047] Weigh 150g of poloxamer 188 and heat it on a 60°C water bath. After all the poloxamer is melted, weigh 10g of silymarin and add it to the molten poloxamer. Stir thoroughly. After all the poloxamers are mixed, -25 Cool quickly at ℃, place it in a desiccator for a few days to fully dry and pulverize to obtain a silymarin-poloxamer solid dispersion.

Embodiment 3

[0048] Example 3. Preparation of silymarin-PEG 6000 solid dispersion

[0049] Weigh 400g of PEG 6000, place it on a water bath, and heat and melt at 70°C. After all the PEG is melted, add 100g of silymarin, stir and mix well, freeze and rapidly cool at -20°C, place it in a desiccator, and pulverize to obtain silymarin. -PEG solid dispersion.

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PUM

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Abstract

Dispersive silybum marianum with obviously raised bioavailability is prepared by combining sold dispersing technology and particle technology and adopting dispersive tablet as carrier. Compared with available technology, the present invention has fast disintegration, fast seepage, high bioavailability and effectively raised clinical treating effect. After mixing with water, the dispersive silybum marianum tablet can disintegrate into suspension, so that it is convenient in taking, especially for aged people and children in patients.

Description

Technical field [0001] The present invention relates to the development of a new pharmaceutical product, in particular to the preparation of a silymarin micronized preparation-silybum marianum dispersible tablet. Background technique [0002] Silymarin is the general term for a series of flavonoid lignin compounds extracted and refined from the fruit of the compositae plant Silybum marianum. The main components include silybin and silybin. silidianin), silichristin and isosilybin, these compounds are all flavonoid lignin derivatives, a series of isomers, the molecular formula is C 25 H 22 O 11 , The molecular weight is about 482. The silymarin extracted and refined from the fruit of silybum marianum is currently included in the national standards as a chemical raw material. The content of silymarin is generally calculated as silybin. [0003] Preparations made of silymarin are widely used in the treatment of hepatitis and liver damage caused by various reasons all over the world....

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/357A61P1/16A61P31/12
Inventor 董诗文谷道昭
Owner 董诗文
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