Silybin injection containing cyclo dextrin or its derivatives

A technology for silymarin and injection, which is applied in the field of silymarin injection and can solve the problems of large individual differences, low oral bioavailability, and impact on absorption, etc.

Inactive Publication Date: 2003-01-22
广州瑞济生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is reported in the literature that the oral bioavailability of silymarin is low, usually 30% to 40%, and individual differences are large. Although the water solubility of silymarin can be increased by making silymarin meglumine salt, the absorption amount can be appropriately increased, but due to water Silymarine meglumine will still be precipitated in the stomach, which will affect its absorption, so the preparation of milk thistle injection has important clinical significance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Dissolve 3 g of hydroxypropyl β-cyclodextrin in 10 ml of water for injection, add 300 mg of silymarin, adjust the pH to 10 with 1N NaOH solution, stir to dissolve the silymarin, continue stirring for 5 hours, adjust the pH to 6.5 with 1N HCl solution, and filter , Sterilization, and freeze-drying to obtain the cyclodextrin-containing silymarin injection of the present invention.

Embodiment 2

[0013] Add 300 mg of silibinin into 15 ml of water, drip into 3N NaOH solution to dissolve, add 10 g of hydroxypropyl-β-cyclodextrin, stir for 1 hour, adjust the pH to 6.5, and sterilize.

Embodiment 3

[0015] Add 100 mg of silymarin to 5 ml of water, drop 5N NaOH to dissolve, add 6 g of methyl-β-cyclodextrin, stir for 2 hours, adjust the pH to 6.3 with 10N HCl, filter, and freeze-dry.

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PUM

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Abstract

The present invention features that silybin is included by cyclodextrin or its derivative so as to dissolve in water to prepare injection. The present invention solves the problem of water insoluble silybin for being suitable for intravenous injection.

Description

Technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a silymarin injection containing cyclodextrin or its derivatives. Background technique [0002] Milk thistle is also known as milk thistle. Its extract is silymarin. It has been used to treat liver disease for many years. There are many reports on silymarin research at home and abroad. In the research on silymarin, it is found that silymarin contains multiple A mixture of components, of which silibinin and isosilibinin are the main components, in addition to silidianin and silidianin. Studies on the pharmacological effects of silymarin have found that silymarin has obvious liver protective effects, and its effects are mainly reflected in anti-oxygen free radicals, anti-lipid peroxidation, anti-lipoxygenase, and anti-GSH lingering effects. The function realizes its protection of the liver and prevents alcohol, toxins and viruses from damaging the liver. Although no antiviral effect of si...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/357A61P1/16
Inventor 关世侠
Owner 广州瑞济生物技术有限公司
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