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Erianin inclusion compound

A technology of erianin and clathrates, applied in the field of series derivative products, can solve the problems of fat emulsion form limitation, high cost, poor stability of erianin fat emulsion, etc.

Inactive Publication Date: 2010-06-16
ZHEJIANG TIANHUANG MEDICINAL PLANT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The Erianin fat emulsion obtained by this method has poor stability, and the preparation process requires complex requirements, nitrogen protection is also required during the preparation process, and the cost is relatively high
At the same time, due to the limitation of the form of fat emulsion, the application method of this product is relatively simple.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0017] The preparation method of erianin clathrate in the present embodiment is as follows:

[0018] (1) Add hydroxypropyl-β-cyclodextrin into water and stir until completely dissolved, the mass ratio of hydroxypropyl-β-cyclodextrin to water is 1:3~5; Water ethanol, which is completely dissolved by ultrasonic vibration, and the mass ratio of erianin to absolute ethanol is 1:500~2000;

[0019] (2) Put the aqueous solution of hydroxypropyl-β-cyclodextrin in a water bath at 40-60°C and stir it at a speed of 800-3000r / min, then add distilled water to the aqueous solution of hydroxypropyl-β-cyclodextrin Elanin ethanol solution, the amount added is controlled so that the mass ratio of erianin to cyclodextrin is 1:8~1:11, and the dropping rate is 1.5~5ml / min; After 1 hour, continue to stir for 1 hour;

[0020] (3) The mixed solution was placed in a water bath at 55° C. and concentrated under reduced pressure to recover ethanol. When the solution was translucent and viscous, it was ...

Embodiment 1

[0023] The erianin clathrate contains the active ingredient erianin and a clathrate agent, the mass ratio of the contained erianin to the clathrate agent is 1:8, and the clathrate agent is hydroxypropyl-β-cyclodextrin.

Embodiment 2

[0025] The erianin clathrate contains the active ingredient erianin and an inclusion agent, the mass ratio of the contained erianin to the inclusion agent is 1:10, and the inclusion agent is hydroxypropyl-β-cyclodextrin.

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PUM

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Abstract

The invention relates to an erianin product and aims at providing a product produced from the inclusion to erianin by using hydroxypropyl-Beta-cyclodextrin and series derived products of an erianin inclusion compound. The erianin inclusion compound comprises active ingredients of erianin and an inclusion agent which is hydroxypropyl-Beta-cyclodextrin and the weight ratio of the erianin to the inclusion agent is 1:8-1:11. As the active ingredients of the erianin are externally wrapped with hydroxypropyl-Beta-cyclodextrin groups which have the characteristic of water solubility, the applicationmethods of the erianin which is slightly water-soluble originally are greatly expanded. The included erianin can be prepared into tablets, capsules, oral solution, granules, injecta, and the like, canbe conveniently utilized in various ways and is also easy to be absorbed by human bodies.

Description

technical field [0001] The invention relates to an erianin product, in particular to a product formed by inclusion of erianin with hydroxypropyl-β-cyclodextrin and a series of derivative products of the inclusion compound. Background technique [0002] Erianin is a bibenzyl compound, its structural formula is 3-hydroxy-4,3',4',5'-tetramethoxybibenzyl, its molecular weight is 318, and its English name is erianin or dihydrocombretastatin A-4. In organic solvents, very slightly soluble in water. In the early 90s of the 20th century, Cushman, M et al. found that Erianin had an effect on human lung adenocarcinoma cell line A-549, breast cancer cell line MCF-7, and colon cancer cell line cultured in vitro by means of in vitro cell culture. HT-29, leukemia cell line MLM, etc. all have inhibitory effect on growth, and its mechanism of action is related to inhibition of tubulin polymerization, inhibition of new blood vessel formation, contraction of blood vessels and reduction of ti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K47/48A61K47/40A61K31/09A61P43/00A61K47/61
Inventor 陈立钻吴人照杨兵勋郁曾渭张旭峰寿丹
Owner ZHEJIANG TIANHUANG MEDICINAL PLANT PHARMA