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Ginsenoside Rg3 hydroxypropyl-beta-cyclodextrin inclusion compound and preparation and preparation method

A technology of cyclodextrin inclusion compound and ginsenoside, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problems of high incidence of allergic reactions, achieve low toxicity, improve stability and biological The effect of utilization

Inactive Publication Date: 2014-06-04
QINGDAO BAICAOHUI INST OF CHINESE HERBAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Since ginsenoside Rg3 is fat-soluble, it is necessary to use a large amount of solubilizers with toxic side effects when preparing preparations, especially injections, such as the use of polyoxyethylene castor oil (Cremophor-EL) and other surfactants, which have carcinogenic properties. Sensitivity, higher incidence of allergic reactions after heavy use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0018] Preparation Example 1 Preparation of hydroxypropyl-β-cyclodextrin inclusion compound of ginsenoside Rg3

[0019] Take 10000mg of hydroxypropyl-β-cyclodextrin and dissolve it in 100ml of water, stir vigorously, take 100mg of ginsenoside Rg3 and dissolve it in a solvent of chloroform:methanol:water 6:4:1, and add hydroxypropyl-β-cyclodextrin Add dropwise to the aqueous solution of dextrin, then stir for 4 hours, filter with a 0.45 μm microporous membrane, concentrate the filtrate under reduced pressure to 1 / 3 of the original volume to remove the organic solvent, add water for injection to double the original volume, and use Sterilize by 0.22μm filtration, and then freeze-dry aseptically to obtain white loose powder, which is the hydroxypropyl-β-cyclodextrin inclusion compound of ginsenoside Rg3. According to HPLC detection, the inclusion compound contains 85 mg of ginsenoside Rg3 , The inclusion rate is 85%.

preparation example 2

[0020] Preparation Example 2 Preparation of Hydroxypropyl-β-cyclodextrin Inclusion Complex of Ginsenoside Rg3

[0021] Take 800mg of hydroxypropyl-β-cyclodextrin and dissolve it in 30ml of water, stir vigorously, take 200mg of ginsenoside Rg3 and dissolve it in a solvent of chloroform:methanol:water of 6:4:1, and add hydroxypropyl-β-cyclodextrin to the solvent containing hydroxypropyl-β-cyclodextrin Add dropwise to the aqueous solution of dextrin, then stir for 4 hours, filter with a 0.45 μm microporous membrane, concentrate the filtrate under reduced pressure to 1 / 3 of the original volume to remove the organic solvent, add water for injection to double the original volume, and use Sterilize by 0.22μm filtration, and then aseptically freeze-dry to obtain white loose powder, which is the hydroxypropyl-β-cyclodextrin inclusion compound of ginsenoside Rg3. According to HPLC detection, the inclusion compound contains 20 mg of ginsenoside Rg3 , The inclusion rate is 10%.

preparation example 3

[0022] Preparation Example 3 Preparation of Hydroxypropyl-β-cyclodextrin Inclusion Compound of Ginsenoside Rg3

[0023] Add 150 mg of ginsenoside Rg3 to 1500 mg of uniformly ground hydroxypropyl-β-cyclodextrin, grind for 3 hours, and dry under reduced pressure to obtain clathrate.

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PUM

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Abstract

The invention provides a ginsenoside Rg3 hydroxypropyl-beta-cyclodextrin inclusion compound, wherein the ratio of ginsenoside Rg3 to hydroxypropyl-beta-cyclodextrin is 1:(1-300). The invention also provides a preparation method of the inclusion compound and a preparation prepared from the inclusion compound.

Description

[0001] Summary [0002] The invention provides a hydroxypropyl-β-cyclodextrin inclusion compound of ginsenoside Rg3, wherein ginsenoside Rg3:hydroxypropyl-β-cyclodextrin=1:1-300, and the invention also provides the inclusion compound The preparation method of the clathrate and the preparation made from the clathrate. technical field [0003] The invention relates to a preparation and a preparation method of ginsenoside Rg3, in particular to a hydroxypropyl-β-cyclodextrin inclusion compound of ginsenoside Rg3, a preparation and a preparation method. Background technique [0004] Ginsenoside Rg3 is a single-component compound extracted from ginseng, which can inhibit the proliferation and growth of tumor cells by inducing differentiation or apoptosis, but has very low toxicity to normal tissues. [0005] Since ginsenoside Rg3 is fat-soluble, it is necessary to use a large amount of solubilizers with toxic side effects when preparing preparations, especially injections, such a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00
Inventor 毕玉轩
Owner QINGDAO BAICAOHUI INST OF CHINESE HERBAL MEDICINE
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