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Hydroxypropyl-beta-cyclodextrin coating material of borneol an dits preparing method

A technology of cyclodextrin inclusion compound and hydroxypropyl group, which is applied in the direction of active ingredients of hydroxyl compounds, non-active ingredients of polymer compounds, pill delivery, etc. Discovery and other issues

Inactive Publication Date: 2006-03-15
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the solubility of β-cyclodextrin is still lower than the solubility requirement of injections, it is still not possible to make injections and be used clinically.
[0005] After searching, so far, no information has been found about borneol using β-cyclodextrin derivatives, namely hydroxypropyl-β-cyclodextrin, to prepare borneol’s hydroxypropyl-β-cyclodextrin inclusion compound and patents and literature reports on preparations and preparation methods

Method used

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  • Hydroxypropyl-beta-cyclodextrin coating material of borneol an dits preparing method
  • Hydroxypropyl-beta-cyclodextrin coating material of borneol an dits preparing method
  • Hydroxypropyl-beta-cyclodextrin coating material of borneol an dits preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 0.5g of borneol, dissolve it in 1mL of absolute ethanol, take 5g of hydroxypropyl-β-cyclodextrin, dissolve it in 100mL of water for injection, and slowly dissolve the borneol solution in anhydrous ethanol in a 50°C water bath with electric rotation stirring. Add it dropwise into the aqueous solution of hydroxypropyl-β-cyclodextrin, seal the container, continue to stir for 2 hours, let it stand at room temperature for 24 hours, use a 0.45 μm microporous membrane to filter the clathrate solution, fill it, and freeze-dry it to obtain White loose powder, confirmed by thin-layer chromatography, forming an inclusion complex of borneol and hydroxypropyl-β-cyclodextrin, determined by gas chromatography, the inclusion rate is 70%.

Embodiment 2

[0037] The clathrate powder obtained in Example 1 was washed with ether, and the ether was evaporated to obtain a white clathrate powder.

Embodiment 3

[0039] Take 13g of borneol, dissolve it in 25mL of ethanol, take 250g of hydroxypropyl-β-cyclodextrin, dissolve it in 2500mL of water for injection, and slowly add the borneol solution to the hydroxyl Propyl-β-cyclodextrin aqueous solution, closed container, continue to stir for 3 hours, stand at room temperature for 12 hours, ultrafilter, take part of the filtrate, freeze-dry to obtain white loose powder, confirmed by thin-layer chromatography, formed The inclusion compound of borneol and hydroxypropyl-β-cyclodextrin is determined by gas chromatography, and the inclusion rate is 78%.

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PUM

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Abstract

A medicine in the form of inclusion compound for treating the disease in central nerve system and inflammation by injection, oral application, or exterior application is prepared from borneol and hydroxypropyl-beta-cyclodextrin through dissolving borneol in organic solvent, adding it to the aqueous solution of hydroxyproply-beta-cyclodextrin, high-speed stirring, laying aside, drying, dissolving in water, ultra-filtering, millipore filtering and freeze drying.

Description

technical field [0001] The invention relates to a traditional Chinese medicine preparation for treating cardiovascular and cerebrovascular diseases, in particular to a hydroxypropyl-beta-cyclodextrin inclusion compound of borneol and its preparation and preparation method. The clathrate can be used to prepare injections, oral preparations and external preparations. It has the functions of treating central nervous system diseases, promoting drugs to pass through the blood-brain barrier, anti-inflammatory, antibacterial, analgesic and promoting transdermal absorption. Background technique [0002] Borneol is a processed product of the resin of the arbor plant of Dipterocarpaceae, Dryobalanops arornatica Gaertn.f., or the crystallization obtained by distilling and cooling the trunk of Dipterocarpa, called "borneoborneol" or "plum slice". It is processed and chopped from the sublimation of the leaves of the perennial herbaceous plant Ainaxiang (Big AI) B1umea balsamifera DC. It...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61K47/40A61K9/20A61K9/22A61K9/48A61K9/02A61K9/06A61K9/12A61K9/19A61K9/70A61P9/00A61P25/00A61P27/02
Inventor 张铁军王靖廖茂梁许浚薛艳
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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