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Fenbendazole liposome preparation and preparing method thereof

A technology of fenbendazole lipid and fenbendazole, which is applied in the field of new preparations of fenbendazole, can solve the problems of short elimination half-life, frequent medication, etc., to improve quality and curative effect, improve bioavailability, retain long time effect

Inactive Publication Date: 2016-01-13
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Common clinical dosage forms include oral dosage forms and injections; however, the elimination half-life of conventional dosage forms of the drug is short, frequent medication, and widely distributed in the body

Method used

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  • Fenbendazole liposome preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] A fenbendazole liposome preparation is prepared from the following raw materials in parts by weight: 1 part of fenbendazole, 10-90 parts of soybean lecithin, and 5-40 parts of cholesterol.

[0018] The preparation method of fenbendazole liposome preparation as described above, comprises the following steps:

[0019] (1) Mix soybean lecithin and cholesterol, add absolute ethanol, add 7 to 14 mL of absolute ethanol for every 100 mg of soybean lecithin and cholesterol, place in a water bath at 65 to 70 ° C, stir to dissolve, and remove the solvent under reduced pressure to obtain Phospholipid membrane;

[0020] (2) Add 100-200mmol / L phosphate buffer solution to fenbendazole, add 10-15mL phosphate buffer solution per mg of fenbendazole, stir to make fenbendazole solution, place at 65 ~70°C water bath, keep warm, and set aside;

[0021] (3) Take the preheated fenbendazole solution obtained in step (2), add the phospholipid film obtained in step (1), stir and hydrate in a w...

Embodiment 2

[0023] A fenbendazole liposome preparation is prepared from the following raw materials in parts by weight: 1 part of fenbendazole, 50 parts of soybean lecithin, and 25 parts of cholesterol.

[0024] The preparation method of fenbendazole liposome preparation as described above, comprises the following steps:

[0025] (1) Weigh 100mg of soybean lecithin and 50mg of cholesterol, mix them, add 20ml of absolute ethanol, place in a 65°C water bath, stir to dissolve, remove the solvent under reduced pressure, and obtain a phospholipid film;

[0026] (2) Weigh 2mg of fenbendazole and add 20ml of 0.1mol / L phosphate buffered saline water, stir to make a fenbendazole solution, put it in a 70°C water bath, keep warm, and set aside;

[0027] (3) Take the preheated fenbendazole solution, add it to a beaker containing phospholipids and cholesterol lipid film, stir and hydrate in a water bath at 65°C for 10 minutes; then place the beaker on a magnetic stirrer, stir at room temperature for 3...

Embodiment 3

[0029] A fenbendazole liposome preparation is prepared from the following raw materials in parts by weight: 1 part of fenbendazole, 60 parts of soybean lecithin, and 20 parts of cholesterol.

[0030] The preparation method of fenbendazole liposome preparation as described above, comprises the following steps:

[0031] (1) Mix 300mg soybean lecithin and 100mg cholesterol, add 50ml absolute ethanol, place in a 65°C water bath, stir to dissolve, and remove the solvent under reduced pressure to obtain a phospholipid film;

[0032] (2) Weigh 5mg of fenbendazole and add 60ml of 0.1mol / L phosphate buffered saline water, stir to make a fenbendazole solution, put it in a 70°C water bath, keep warm, and set aside;

[0033] (3) Take the preheated fenbendazole solution, add it to a beaker containing phospholipids and cholesterol lipid film, stir and hydrate in a water bath at 65°C for 15 minutes. Then place the beaker on a magnetic stirrer, stir at room temperature for 45 minutes, mix we...

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Abstract

The invention discloses a fenbendazole liposome preparation and a preparing method thereof. The fenbendazole liposome preparation is prepared through a phosphate method with soya bean lecithin and cholesterol as film materials. The fenbendazole liposome preparation has good preparation nature and good target performance, the treatment effect can be improved, and the fenbendazole liposome preparation has the advantages that long-time acting is achieved, medicine toxicity is reduced, and drug stability is improved.

Description

technical field [0001] The invention relates to a new preparation of fenbendazole, in particular to a fenbendazole liposome preparation and a preparation method thereof. Background technique [0002] Liposomes are continuous bilayer lipid molecules containing an aqueous space; the main components of liposomes are natural phospholipids and steroids, so they are biocompatible, biodegradable, non-toxic and non-immunogenic. There are many types of liposomes, all of which contain water and lipid spacers, so water-soluble and fat-soluble molecules and ions are easily included in liposome particles; this unique property makes liposomes a variety of Generic carrier for drugs. Liposome is a targeted drug carrier, which belongs to a new dosage form of targeted drug delivery system. It can embed drug powder or solution in particles with a diameter of nanometer scale. This particle has a cell-like structure. It enters the human or animal body and is mainly swallowed by the reticuloend...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4184A61P33/10A61P31/04A61P33/02A61P31/10A61P11/00
Inventor 李亚娥李建正
Owner ZHENGZHOU HOUYI PHARMA