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Method for preparing amorphous crystalline albendazole

A technology of albendazole and crystal form, applied in the field of preparation of amorphous crystal form albendazole, can solve problems such as being unsuitable for industrialized production, difficult to collect amorphous crystal form albendazole, and many residues, etc. Improve bioavailability, simple method, and the effect of improving dissolution

Inactive Publication Date: 2012-05-16
GUILIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the prepared amorphous albendazole is difficult to collect and has many residues, which is not suitable for industrial production

Method used

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  • Method for preparing amorphous crystalline albendazole
  • Method for preparing amorphous crystalline albendazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Put 10g of albendazole in 30ml of 98% formic acid (w / w), heat to 35°C to dissolve it, raise the temperature to 80°C and keep it for 1h, then add 0.01g of activated carbon for decolorization, filter while it is hot, add 10% hydroxide to the filtrate Sodium aqueous solution (w / w) adjusted the pH to 6, filtered with suction, washed with 200g of purified water, sucked dry, and dried to obtain 8.5g of amorphous albendazole with a yield of 85%.

[0023] The resulting product was tested for dissolution under the entry of CP2010 albendazole tablets, and the dissolution amount was 82% of the labeled amount.

Embodiment 2

[0025] Put 10g of albendazole in 50ml of 80% acetic acid (w / w), heat to 40°C to dissolve it, raise the temperature to 85°C and keep it for 1h, then add 0.02g of activated carbon for decolorization, filter while it is hot, and add 20% hydroxide to the filtrate Adjust the pH to 7 with sodium aqueous solution (w / w), filter with suction, wash with 1000 g of purified water, drain and dry to obtain 8.8 g of amorphous albendazole with a yield of 88%.

[0026] The resulting product was tested for dissolution under the entry of CP2010 albendazole tablets, and the dissolution amount was 85% of the labeled amount.

Embodiment 3

[0028] Put 10g of albendazole in 100ml of water, then add 15ml of concentrated hydrochloric acid, heat to 40°C to dissolve it, continue to heat up to 95°C for 1 hour, then add 0.015g of activated carbon for decolorization, filter while it is hot, add 20% hydrogen to the filtrate Adjust the pH to 7 with sodium aqueous solution (w / w), filter with suction, wash with 500 g of purified water, drain and dry to obtain 9.0 g of amorphous albendazole with a yield of 90%.

[0029] The resulting product was tested for dissolution under the entry of CP2010 albendazole tablets, and the dissolution amount was 92% of the labeled amount.

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PUM

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Abstract

The invention discloses a method for preparing amorphous crystalline albendazole, comprising the following steps: dissolving albendazole in methanoic acid, acetic acid or hydrochloric acid, and raising the temperature to 80-100 degrees centigrade and preserving the temperature for 0.5-1 h; adding active carbon into them for decoloration and filtering them, and regulating the pH value of the filter liquid to 6-7 with alkaline, and pump filtering the filter liquid; washing the filter cake to remove off inorganic salt and drying the cake to obtain amorphous crystalline albendazole. In comparison with the prior art, the method disclosed by the invention transfers the original A crystal form into an amorphous crystal form so as to largely raise the dissolution of the albendazole and further raise the bioavailability. The method is simple and is convenient to operate. The prepared finished product has a stable quality. The method is suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of amorphous crystal form albendazole. Background technique [0002] Existing studies have found that many drug molecules have multiple crystal forms, and different crystal forms have different solubility in water and human gastric juice, resulting in different bioavailability. The higher the dissolution rate of a drug in the human body, the higher its bioavailability. [0003] The free energy of different crystal forms of drugs is different, resulting in different solubility. Generally speaking, the greater the free energy, the more unstable the crystal form and the greater the solubility; vice versa. The existing crystal form of albendazole is generally A crystal form. According to the dissolution test under the entry of albendazole tablets in the 2010 edition of "Chinese Pharmacopoeia" (hereinafter referred to as CP2010), the dissolution amount is 65% o...

Claims

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Application Information

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IPC IPC(8): C07D235/32
Inventor 梁永坚
Owner GUILIN PHARMA
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