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Hydroxy propyl-beta-cyclodextrin inclusion compound of anisolene and its preparation and preparation method

A technology of cyclodextrin inclusion compound and anisole, which is applied in the direction of non-active ingredients of polymer compounds, can solve the problems of affecting curative effect, poor stability of preparations, and low bioavailability, so as to improve bioavailability and stability , Ease of use

Inactive Publication Date: 2004-08-04
沈阳皓天万嘉医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Anisene is a fat-soluble component and is difficult to dissolve in water. It is usually made into soft capsules for clinical application, and its bioavailability is usually low, which affects the curative effect
Anisole milk injection is administered by intramuscular injection, which improves the bioavailability, but the preparation is poor in stability, easy to separate, and has large particles, which brings potential danger to clinical application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Take 1g of anisole, dissolve it in 5ml of ethanol, take 5g of hydroxypropyl-β-cyclodextrin, dissolve it in 200ml of water for injection, add the anisole ethanol solution dropwise into the HPCD solution, stir magnetically at room temperature for 3 hours, use 0.45 Filter and freeze with μm microporous membrane to obtain a white loose powder, which was confirmed by thin-layer chromatography to form an inclusion complex of anisole and hydroxypropyl-β-cyclodextrin. As determined by gas chromatography, the inclusion rate is 95%.

Embodiment 2

[0022] The clathrate powder obtained in Example 1 was washed with ether, and the ether was evaporated to obtain a white clathrate powder.

Embodiment 3

[0024] Others are the same as Example 1, change the magnetic stirring method to the ultrasonic oscillation method, shake at room temperature for 20 minutes, filter the inclusion solution through a 0.45 μm microporous membrane, freeze-dry the filtrate, and obtain a white loose powder, which is confirmed by thin-layer chromatography. An inclusion complex was formed, and the inclusion rate was 87% as determined by gas chromatography.

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PUM

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Abstract

An inclusion compound of anisylene and hydroxypropyl-beta-cyclo-dextrin is prepared through dissolving anisylene in organic solvent, adding it to the aqueous solution of hydroxypropyl-beta-cyclodextrin, stirring, freeze drying to obtain the water-soluble inclusion. It can be used to prepare freeze-drying powder injection and tablet.

Description

Technical field [0001] The present invention relates to hydroxypropyl-beta-cyclodextrin inclusion compound of anisene, preparation and preparation method. The inclusion compound can be used for injection and oral administration, and has the effect of increasing white blood cells. Background technique [0002] Anisene is a plant active ingredient extracted from plants such as Magnoliaceae Illicium verum Hook.f. or Umbelliferae Feniculum vulgare Mill. or Lamiaceae Ocimumbasilicum L.. Its English name is anethol, and its chemical name is 1-methoxy-4-propenylbenzene with the formula C 10 h 12 O, anisole can also be called anethole, anisole, anisole has the effect of increasing white blood cells, it is used for chemotherapy and radiotherapy of cancer patients, it can also be used as a flatulence drug and a carminative, and it is also used in spices. The prepared anisole capsules have been widely used clinically, and good curative effect has been achieved in clinical application...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40C08K5/01C08L5/16
Inventor 董英杰艾莉
Owner 沈阳皓天万嘉医药科技有限公司
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