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Nanoscale albendazole micropowder and preparation method thereof

A kind of albendazole micropowder, the technology of albendazole, which is applied in the field of nano-scale albendazole micropowder and its preparation, can solve the problems such as the insolubility of albendazole, and achieves simple and easy method, improved solubility and dissolution. Speed, simple process effect

Active Publication Date: 2011-03-16
THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] The present invention provides a kind of nanoscale albendazole micropowder and its preparation method, which overcomes the deficiencies in the prior art and solves the problem of insoluble albendazole The problem is that the process is stable, the preparation forms are diverse, and the operation is simple. The obtained nano-scale albendazole powder has a small and controllable particle size and good solubility.

Method used

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  • Nanoscale albendazole micropowder and preparation method thereof
  • Nanoscale albendazole micropowder and preparation method thereof
  • Nanoscale albendazole micropowder and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0053] In the first step, 290 mg of albendazole raw material was weighed, and 2 ml of formic acid was added to completely dissolve it to obtain the first solution. In the second step, 100 milliliters of ethanol solutions containing 2.75 grams of Tween 80, 0.74 grams of sodium hydroxide and 0.10 grams of polyacrylic acid were prepared as the second solution. The third step is to fully mix the first solution and the second solution under the conditions of a temperature of 40° C., a stirring speed of 3000 rpm, and a stirring time of 10 minutes to obtain an albendazole slurry with a pH of 4.50. In the fourth step, the albendazole slurry obtained in the third step is first centrifuged to obtain a centrifugal precipitate, and then the centrifugal precipitate is freeze-dried to obtain a nano-scale albendazole micropowder, and the particle size detection shows that its The particle size is 270 nm.

Embodiment 2

[0055] In the first step, 290 mg of albendazole raw material was weighed, and 2 ml of formic acid was added to completely dissolve it to obtain the first solution. In the second step, 100 milliliters of aqueous solutions containing 0.10 gram of poloxamer-188, 1.60 gram of sodium hydroxide and 0.10 gram of sodium metaphosphate were prepared simultaneously, which was the second solution. The third step is to fully mix the first solution and the second solution under the conditions of a temperature of 0°C, a stirring speed of 500 rpm, and a stirring time of 30 minutes to prepare an albendazole slurry with a pH of 10.98. In the fourth step, the albendazole slurry obtained in the third step is first centrifuged to obtain a centrifugal precipitate, and then the centrifugal precipitate is freeze-dried to obtain a nano-scale albendazole micropowder, and the particle size detection shows that its The particle size is 300 nm.

Embodiment 3

[0057] In the first step, 290 mg of albendazole raw material was weighed, and 2 ml of formic acid was added to completely dissolve it to obtain the first solution. In the second step, 100 milliliters of ethanol solutions containing 0.20 gram of poloxamer-188, 0.78 gram of sodium hydroxide and 40.0 gram of polyvinylpyrrolidone were prepared simultaneously as the second solution. The third step is to fully mix the first solution and the second solution under the conditions of a temperature of 25° C., a stirring speed of 1000 rpm, and a stirring time of 20 minutes to prepare an albendazole slurry with a pH of 4.60. In the fourth step, the albendazole slurry obtained in the third step is first centrifuged to obtain a centrifugal precipitate, and then the centrifugal precipitate is freeze-dried to obtain a nano-scale albendazole micropowder, and the particle size detection shows that its The particle size is 280 nm.

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Abstract

The invention relates to the technical field of medicinal materials, in particular to nanoscale albendazole micropowder and a preparation method thereof. The method comprises the following steps: 1. dissolving albendazole into a good solvent to obtain a first solution; 2. adding a surfactant, a polymeric substance and sodium hydroxide to a poor solvent to obtain a second solution; 3. fully mixing the first solution with the second solution to obtain an albendazole slurry; and 4. carrying out centrifugal separation on the albendazole slurry obtained in step 3 to obtain a centrifugal precipitate, and then freeze-drying the centrifugal precipitate to obtain the nanoscale albendazole micropowder. The invention has the advantages that the particle size of the albendazole raw material is obviously reduced and the solubility and dissolving-out speed of a drug are effectively improved, thus improving the absorption and bioavailability of the albendazole well, overcoming a series of defects of low bioavailability, poor absorption and the like of the traditional albendazole non-nanometer raw material or preparation, and effectively giving play to therapeutic effect of the albendazole in resisting parasites in tissues and organs.

Description

technical field [0001] The invention relates to the technical field of medicinal raw materials, and relates to a nanoscale albendazole micropowder and a preparation method thereof. Background technique [0002] Internal parasites are a group of organisms that parasitize in the host or host (host) to obtain the nutrients or shelter needed to maintain their survival, development or reproduction. Such organisms not only parasitize the human digestive tract, lungs, liver, blood In the pipeline, it even parasitizes all tissues and organs that can be parasitic, such as brain tissue and eyeballs. [0003] Albendazole (ABZ), also known as albendazole, is a benzimidazole derivative and is a broad-spectrum antiparasitic drug used in clinical practice. The chemical composition is methyl [(5-propylthio)-1H-benzimidazol-2-yl]carbamate. Since its launch in 1977, it has been widely used in the clinical treatment of parasitic diseases such as hookworm disease, ascariasis, whipworm disease...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4184A61P33/00
Inventor 温浩陈迹王建华马运芳赵军陈蓓袁圆单志桂
Owner THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY
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