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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 there is no recommendation to make anetthio polylactic acid into liposomes and proliposomes

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Preparation of anetis trisulfide liposomes by ethanol injection method: take soybean phospholipids, cholesterol, VE and add absolute ethanol to dissolve them, inject them into an aqueous solution of anetis trisulfide, stir at constant temperature and high speed, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane for sizing, that is The encapsulation efficiency of the liposome of anetellitthioate can reach 64.8%.

Embodiment 2

[0012] Preparation of anetis trisulfide liposomes by film dispersion method: take soybean lecithin, cholesterol, and VE and dissolve them in 150 ml eggplant-shaped bottle with 15 ml of chloroform, form a film under reduced pressure on a rotary thin film evaporator and remove all organic solvents, add 10 ml of anetis trisulfide The aqueous solution is hydrated, and the particle is sized by passing through a microporous membrane to obtain the liposome of anetellitate, and the encapsulation efficiency can reach 62.1%.

Embodiment 3

[0014] Prepare anetthio liposomes by reverse-phase evaporation method: Weigh soybean lecithin, cholesterol, VE and add 5ml chloroform to dissolve, then add 10ml ether, then add 15ml anetthio phosphate buffer, bath ultrasonic to make uniform For single-phase system, remove chloroform ether by vacuum evaporation until gel is formed, continue to evaporate under reduced pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposome, is formed. Encapsulation efficiency 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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