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Preparation method of Albendazole liposome preparation

A technology of albendazole lipid and albendazole, which is applied in the field of preparation of albendazole liposome preparations, can solve problems such as limiting the absorption of albendazole, achieve reduction of toxic and side effects, long retention time, The effect of simple preparation method

Inactive Publication Date: 2018-06-29
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Since albendazole is insoluble in water, slightly soluble in acetone, ether or chloroform, and practically insoluble in ethanol, the absorption of the existing dosage forms of albendazole is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] A preparation method for albendazole liposome preparation, comprising the following steps:

[0019] (1) Preparation of ether solution: in parts by weight, weigh 10 to 90 parts of soybean lecithin and 5 to 40 parts of cholesterol and dissolve them in 50 to 120 parts of anhydrous ether in turn, and place them at a temperature of 50 to 65°C and stir to dissolve Obtain ether solution completely, standby;

[0020] (2) Preparation of albendazole solution: Weigh 1~2 parts of albendazole and dissolve it in a phosphate buffer solution with a concentration of 100~200mmol / L, place it at a temperature of 60~70°C and stir to dissolve completely to obtain albendazole Dazole solution, heat preservation, standby; the mass ratio of albendazole to 100-200mmol / L phosphate buffer solution is 1; (10-100);

[0021] (3) Mix the albendazole solution obtained in step (2) with the ether solution obtained in step (1), shake, ultrasonically treat for 5 to 10 minutes, and distill under reduced pre...

Embodiment 2

[0023] A preparation method for albendazole liposome preparation, comprising the following steps:

[0024] (1) Preparation of ether solution: In parts by weight, weigh 75 parts of soybean lecithin and 25 parts of cholesterol and dissolve them in 80 parts of anhydrous ether in turn, and stir and dissolve at a temperature of 50~65°C to completely obtain ether solution, which is set aside ;

[0025] (2) Preparation of albendazole solution: weigh 1 part of albendazole and dissolve it in a phosphate buffer solution with a concentration of 100mmol / L, place it at a temperature of 65°C and stir to dissolve completely to obtain an albendazole solution, keep it warm, Standby; the mass ratio of the albendazole to the 100mmol / L phosphate buffer solution is 1; 50;

[0026] (3) Mix the albendazole solution obtained in step (2) with the ether solution obtained in step (1), shake, ultrasonically treat for 10 minutes, distill off the organic solvent under reduced pressure, and then hydrate wi...

Embodiment 3

[0028] A preparation method for albendazole liposome preparation, comprising the following steps:

[0029] (1) Preparation of ether solution: In parts by weight, 80 parts of soybean lecithin and 30 parts of cholesterol were weighed and dissolved in 110 parts of anhydrous ether in turn, placed at a temperature of 60°C and stirred to dissolve completely to obtain an ether solution, which was set aside;

[0030] (2) Preparation of albendazole solution: Weigh 1.5 parts of albendazole and dissolve it in a phosphate buffer solution with a concentration of 150mmol / L, place it at a temperature of 65°C and stir to dissolve completely to obtain an albendazole solution, keep it warm, Standby; The mass ratio of described albendazole and 150mmol / L phosphate buffer solution is 1; 80;

[0031] (3) Mix the albendazole solution obtained in step (2) with the ether solution obtained in step (1), shake, ultrasonically treat for 8 minutes, distill under reduced pressure to remove the organic solve...

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Abstract

The invention relates to a preparation method of an Albendazole liposome preparation. The preparation method comprises the following steps: (1) preparation of an ether liquid: measured in parts by weight, weighing soybean lecithin and cholesterol, sequentially dissolving in anhydrous ether, stirring and completely dissolving to obtain the ether liquid for later use; (2) preparation of an Albendazole liquid: weighing Albendazole, dissolving in a phosphate buffer liquid, placing at a temperature of 60-70 DEG C, stirring and completely dissolving to obtain the Albendazole liquid and performing heat preservation for later use; (3) mixing the Albendazole liquid and the ether liquid, shaking, performing ultrasonic treatment, performing reduced pressure distillation, removing an organic solvent,stirring and hydrating in a water bath and finally stirring and uniformly mixing at a room temperature to obtain the product. The liposome preparation prepared by the preparation method provided by the invention has the benefits that the medical effect of the Albendazole on the treatment of cysticercosis and other parasites such as strongyloides stercoralis can be greatly improved, the medicine toxicity is reduced, and the medicine stability is improved.

Description

technical field [0001] The invention belongs to the technical field of albendazole liposome preparations, in particular to a preparation method of albendazole liposome preparations. 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, nontoxic and nonimmunogenic. Now 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 versatile carrier for a wide variety of 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 swal...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4184A61P33/02A61P33/10
CPCA61K9/127A61K9/1277A61K31/4184A61K47/24A61K47/28
Inventor 李建正李亚娥王凯马沛然
Owner ZHENGZHOU HOUYI PHARMA
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