Preparation method of griseofulvin microcrystals

A technology of griseofulvin and microcrystals, which is applied in the field of preparation of griseofulvin microcrystals, can solve the problems of large particle size of griseofulvin microcrystals, achieve low production cost, simple production process, The effect of easy operation

Active Publication Date: 2017-06-13
ZHEJIANG FORESTRY UNIVERSITY
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0005] In order to solve the problem that the griseofulvin microcrystal particle size prepared by conventional methods is relatively large, the present invention proposes a preparation method of griseofulvin microcrystal, and the griseofulvin microcrystal particle diameter prepared by the present invention is Smaller than 1 micron, the production process is simple, the operation is convenient, the product has high bioavailability, and it is suitable for large-scale industrial production

Method used

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  • Preparation method of griseofulvin microcrystals

Examples

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Embodiment 1

[0024] Put 10 kg of griseofulvin raw material drug into 100 liters of acetone and heat to reflux at 45°C to dissolve. After completely dissolving, pass cooling water down to room temperature for later use. Mix 0.5 kg of sodium lauryl sulfate with 1 kg of hydroxypropyl Methylcellulose was dissolved at room temperature with 1000 liters of water, and the two solutions were mixed with a jet mixer, separated by a centrifuge and washed with 100 liters of purified water, dried under reduced pressure to obtain 9.82 kg of griseofulvin microcrystals, with an average particle size of 800 ±60nm.

Embodiment 2

[0026] Put 10 kilograms of griseofulvin bulk drug into 80 liters of dimethylformamide and heat to reflux at 100°C to dissolve. After complete dissolution, pass cooling water down to 5°C for later use. Mix 1 kilogram of tetrabutylammonium bromide with Dissolve 1 kg of methylcellulose with 1000 liters of water and cool down to 5°C, add griseofulvin dimethyl polyamide solution in a stainless steel reaction kettle under rapid stirring, separate by centrifuge and wash with 100 liters of purified water, and depressurize Dried to obtain 9.76 kg of griseofulvin microcrystals with an average particle size of 900±30nm.

Embodiment 3

[0028] Put 10 kg of griseofulvin raw material drug into 100 liters of formamide, heat and reflux at 150°C to dissolve, pass cooling water to -5°C after complete dissolution, and use 0.2 kg of dodecyl trimethyl bromide Dissolve ammonium and 0.8 kg of hydroxyethyl cellulose in 1000 liters of water and lower the temperature to -5°C. Add the formamide solution of griseofulvin into the glass-lined glass under rapid stirring, separate by centrifuge and wash with 100 liters of purified water, and depressurize Dried to obtain 9.87 kg of griseofulvin microcrystals with an average particle size of 860±50nm.

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Abstract

The invention relates to the field of medicines and provides a preparation method of griseofulvin microcrystals, aiming at solving the problem that the grain diameter of griseofulvin microcrystals prepared by a conventional method is relatively large. The preparation method comprises the following steps: firstly, preparing a griseofulvin organic solution, and a water solution of a surfactant and thickener mixture; secondly, adding the griseofulvin organic solution into the water solution of the surfactant and thickener mixture; and after mixing, filtering and drying to obtain the griseofulvin microcrystals. According to the preparation method, the grain diameter of the griseofulvin microcrystals prepared by the preparation method is less than 1 micron; and meanwhile, a production flow is simple, the operation is convenient and the bioavailability of a product is high, so that the preparation method is suitable for industrialized large-scale production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method of griseofulvin microcrystals. Background technique [0002] The molecular structure of griseofulvin is as follows: [0003] [0004] It is a non-polyene antifungal antibiotic, clinically used to treat infections caused by dermatophytes, and used to control rice blast in rice cultivation. The solubility of griseofulvin in water is extremely small. If the crystal particles are too large, it will cause problems such as low bioavailability and excessive dosage in clinical use or when used to prevent and control rice blast. In order to improve its bioavailability, it is necessary to It is prepared as microcrystals. At present, the methods for preparing water-phase insoluble chemical drug microcrystals mainly include airflow ultrafine pulverization, solvent transfer method, supercritical solution rapid expansion method, and the like. Most of the equipment used in the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/94A61P31/10A61P17/00A01P3/00
CPCC07B2200/13C07D307/94
Inventor 郭明格日乐图李茜云
Owner ZHEJIANG FORESTRY UNIVERSITY
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