Anethole trithione liposome and its prepn

A technology of anisitrazine and liposome, applied in the field of medicine, can solve problems such as low bioavailability, and achieve the effect of improving curative effect

Inactive Publication Date: 2006-05-17
胡才忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Anetthio polylactic acid nanoparticle freeze-dried injection; bioavailability is low, but

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0009] Example 1:

[0010] Ethanol injection method to prepare anistrisulfide liposomes: dissolving soybean phospholipids, cholesterol, and VE in anhydrous ethanol and then injecting them into an aqueous solution of anistrisulfide, stirring at a constant temperature and high speed, evaporating under reduced pressure to remove ethanol, and granulating through a microporous membrane, namely The anisetrithio liposome was obtained, and the encapsulation efficiency was up to 64.8%.

Example Embodiment

[0011] Example 2:

[0012] Thin-film dispersion method to prepare liposomes: Dissolve soybean lecithin, cholesterol and VE in a 150ml eggplant-shaped bottle with 15ml chloroform, form a film under reduced pressure on a rotary thin-film evaporator and remove the organic solvent, add 10ml of anettrisulfide The aqueous solution is hydrated, passed through a microporous membrane for granulation, and anisitride liposomes are obtained, and the encapsulation efficiency can reach 62.1%.

Example Embodiment

[0013] Example 3:

[0014] Preparation of liposomes by reversed-phase evaporation: Weigh soybean lecithin, cholesterol, VE, add 5 ml of chloroform to dissolve, then add 10 ml of ether, then add 15 ml of phosphate buffered solution of anistrisulfide, and bathe ultrasonically to make the formation uniform In the single-phase system, the chloroform ether was removed by evaporation under reduced pressure until gel formation, continued evaporation under reduced pressure for 5 to 10 minutes, and vortexed until the aqueous suspension, ie, liposomes, was formed. The encapsulation rate can reach 28.5%.

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PUM

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Abstract

The present invention is anethole trithione liposome with high absorption, high bioavailability and high stability and its preparation. The anethole trithione liposome or anethole trithione liposome precursor is prepared with anethole trithione and phosphatide, cholesterol, supporting agent and other supplementary material. It has phosphatide/medicine weight ratio of 0.1-50, and is prepared through ethanol injecting process, film dispersion process, inverse evaporation process, extruding process or mechanical process. The supporting agent may be sorbitol, mannitol, cane sugar, etc. and has ratio to phosphatide of 0.01-500. The anethole trithione liposome can raise the GSH level of liver, raises the activity of GCS, GSSG-R and GSH-S-TX and lower the activity of GSH-PX, so as to raise the activity of liver cell and increase bile scretion. It is suitable for treating cholecystitis, gall stone and indigestion, and may be used in the assisting treatment of acute and chronic hepatosis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular it is a trithione liposome (including proliposome) and a preparation method thereof. Background technique [0002] Anethole Trithione (Anethole Trithione) molecular formula; C10H80S3 molecular weight: 240.35. Chemical name: 5-(p-methoxyphenyl)-1,2-dithiocyclopent-4-ene-3-thione [5-(p -methoxyphenyl)-1,2-dith-iacyclopent-4-ene-3-thione]. Can enhance liver glutathione (GSH) level, significantly enhance glutamyl cysteine ​​synthetase (GCS), glutathione reductase (GSSG-R) and glutathione sulfur transferase (GSH-S -TX) activity, reducing the activity of glutathione peroxidase (GSH-PX), thereby enhancing the vitality of liver cells, increasing the secretion of bile, and having a choleretic effect. After oral administration, it is rapidly absorbed, and it takes effect 15 to 30 minutes after taking it, and reaches the peak plasma level after 1 hour. This product is mainly metabolized in...

Claims

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Application Information

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IPC IPC(8): A61K31/385A61K9/08A61K9/127A61K9/16A61K9/19A61K9/20A61K9/48A61P1/16
Inventor 胡才忠
Owner 胡才忠
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