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Preparation method and application of albendazole

A technology of albendazole and a synthesis method is applied in the field of preparation of albendazole colon target microcapsules, and achieves the effects of good solubility, accelerated release and high purity

Inactive Publication Date: 2015-09-16
CHANGZHOU JIALING MEDICINE IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it takes 1-6 hours for the above-mentioned oral colon-targeted microcapsules to reach a higher drug release rate in simulated intestinal fluid (release medium of pH=7.4), so the drug release rate of the oral colon-targeted microcapsules needs to be further improved. improve

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028]Dissolve 13.8g of o-nitroaniline and 15g of dipropyl disulfide in 100mL of methanol, stir evenly, feed chlorine gas into the reaction system, react for 1 hour, and generate a solid product, filter, wash, and dry to obtain 4-propane Sulfuryl-2-nitroaniline; the above-mentioned 4-propylthio-2-nitroaniline was dissolved in aqueous ethanol (ethanol / water=2:1 (v / v)), then added 12g sodium hydrosulfide, 60 Stir and reduce for 4 hours at ℃ to generate 4-propylthio-1,2-o-phenylenediamine, extract with 120mL of toluene; add 12g of methyl cyanocarbamate to the above extract, raise the temperature to 80℃, stir the reaction and drop Add mixed acid (a mixed acid solution of hydrochloric acid and glacial acetic acid, the molar ratio of hydrochloric acid and glacial acetic acid is 2:1), keep the pH value of the reaction system at about 4, and keep it warm at 80°C for 1 hour to form a white solid, which is centrifuged and washed with water to obtain aben Crude dazole. Add 60mL of absol...

Embodiment 2

[0030] Dissolve 13.8g of o-nitroaniline and 15g of dipropyl disulfide in 100mL of methanol, stir evenly, feed chlorine gas into the reaction system, react for 2 hours, and generate a solid product, filter, wash, and dry to obtain 4-propane Sulfuryl-2-nitroaniline; the above-mentioned 4-propylthio-2-nitroaniline was dissolved in aqueous ethanol (ethanol / water=2:1 (v / v)), then added 12g sodium hydrosulfide, 70 Stir and reduce for 3 hours at ℃ to generate 4-propylthio-1,2-o-phenylenediamine, extract with 120mL toluene; add 12g methyl cyanocarbamate to the above extract, raise the temperature to 70℃, stir the reaction and drop Add mixed acid (a mixed acid solution of hydrochloric acid and glacial acetic acid, the molar ratio of hydrochloric acid and glacial acetic acid is 2:1), keep the pH value of the reaction system at about 4, and keep it warm at 80°C for 2 hours to form a white solid, which is centrifuged and washed with water to obtain aben Crude dazole. Add 60mL of absolute...

Embodiment 3

[0032] Dissolve 13.8g of o-nitroaniline and 15g of dipropyl disulfide in 100mL of methanol, stir evenly, feed chlorine gas into the reaction system, react for 3 hours, and generate a solid product, filter, wash, and dry to obtain 4-propane Sulfuryl-2-nitroaniline; the above-mentioned 4-propylthio-2-nitroaniline was dissolved in aqueous ethanol (ethanol / water=2:1 (v / v)), then added 12g sodium hydrosulfide, 60 Stir and reduce for 5 hours at ℃ to generate 4-propylthio-1,2-o-phenylenediamine, extract with 120mL toluene; add 12g methyl cyanocarbamate to the above extract, raise the temperature to 80℃, stir the reaction and drop Add mixed acid (a mixed acid solution of hydrochloric acid and glacial acetic acid, the molar ratio of hydrochloric acid and glacial acetic acid is 2:1), keep the pH value of the reaction system at about 4, and keep it warm at 80°C for 3 hours to form a white solid, which is centrifuged and washed with water to obtain aben Crude dazole. Add 60mL of absolute...

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Abstract

The invention relates to synthesis, refinement and application of albendazole. The invention firstly provides a synthesis method of albendazole, which adopts a mixed solvent (water and ethanol)-mixed acid (formic acid and acetic acid) refinement system; and the refined albendazole has higher purity and solubility. The invention further provides a preparation method of a colon targeted microcapsule, which comprises the following steps: coating albendazole with amido polylactic acid-hydroxyacetic acid copolymer (PLGA-NH2) to prepare drug-carried nanoparticles, and simultaneously coating the drug-carried nanoparticles and a disintegrant with a pH-sensitive enteric material to obtain the albendazole colon targeted microcapsule. The colon targeted microcapsule has the triple effects of colon targeting, quick disintegration and slow drug release, prolongs the in-vivo circulation time of the oral albendazole, and enhances the absorption efficiency of albendazole.

Description

technical field [0001] The present invention relates to the synthesis and application method of albendazole, in particular to a synthesis and refining method of albendazole with high solubility, and a preparation of albendazole colonic target microcapsules with high dissolution rate method. Background technique [0002] Albendazole (Albendazole, ABZ) has another name called prothioimazole, and its chemical name is methyl 5-propylthio-2-benzoimidazole carbamate. ABZ is mainly used to treat intestinal parasitic diseases, and has a certain effect on echinococcosis. ABZ is insoluble in water and slightly soluble in organic solvents. Due to the low solubility of ABZ, it is poorly absorbed in the intestinal tract and has low bioavailability. The absorption efficiency of a drug is significantly affected by the properties of the drug itself, among which the three most important factors are the permeability, solubility and dissolution rate of the drug. The drug absorption fractio...

Claims

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Application Information

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IPC IPC(8): C07D235/32A61K9/50A61K47/48A61K31/4184A61P33/00
CPCA61K9/5031A61K31/4184A61K47/61C07D235/32
Inventor 张月亮徐立新
Owner CHANGZHOU JIALING MEDICINE IND
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