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Spherical particles of cefazolin sodium monohydrate and preparation method thereof

A technology for water cefazolin sodium and cefazolin sodium is applied in the field of cefazolin sodium spherical particles and crystallization preparation, which can solve the problems of low bulk density, rough surface, uneven particle size distribution, etc. The effect of uniform particle size distribution

Active Publication Date: 2017-03-08
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most of the cefazolin sodium monohydrate products are fine needle-like crystals, and there are problems such as small average particle size, uneven particle size distribution, rough surface, low bulk density, and poor fluidity of the product.
These factors have seriously restricted the post-processing of the drug product

Method used

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  • Spherical particles of cefazolin sodium monohydrate and preparation method thereof
  • Spherical particles of cefazolin sodium monohydrate and preparation method thereof
  • Spherical particles of cefazolin sodium monohydrate and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Under the condition of 40 DEG C, cefazolin sodium solid 1g is joined in the solvent system of 100g water-ethanol, wherein the mass ratio of ethanol and water is 1:1, is cooled to 5 DEG C with the cooling rate of 0.1 DEG C / min, set The stirring speed was set at 100 rpm, and 0.1% chloroform was added as a bridging agent. At this time, crystals began to precipitate. Under constant temperature and stirring conditions, the crystals grew for 5 hours. Finally, the crystal paddle was transferred to the filtration system, and the filter cake was dried at 20° C. under a vacuum of 0.1 Mpa for 10 hours to obtain spherical crystals of cefazolin sodium monohydrate, and the process yield was 95%. Product X-ray powder diffraction such as figure 1 As shown, the product TG curve is as follows figure 2 As shown, the product particle size distribution is as image 3 As shown, the appearance of the product is as follows Figure 4 and Figure 5 shown. The obtained spherical particles h...

Embodiment 2

[0032] Under the condition of 40 DEG C, cefazolin sodium solid 4g is joined in the solvent system of 100g DMAC-methanol, wherein the mass ratio of methanol and DMAC is 10:1, is cooled to 25 DEG C with the cooling rate of 5 DEG C / min, set The stirring speed was set at 250 rpm, and 0.1% toluene was added as a bridging agent. At this time, crystals began to precipitate. Under constant temperature and stirring conditions, the crystals grew for 10 hours. Finally, the crystal paddle was transferred to the filtration system, and the filter cake was dried at 35° C. for 2 hours under a vacuum of 0.1 Mpa to obtain spherical crystals of cefazolin sodium monohydrate, and the process yield was 92%. The obtained spherical particles have uniform particle size distribution, coefficient of variation C.V. = 0.28, average particle diameter equal to 302 μm, and bulk density of 0.411 g / ml. They have high sphericity, good fluidity, fast product separation speed, and pharmaceutical products have bett...

Embodiment 3

[0034]Under the condition of 40°C, cefazolin sodium solid 8g was added to the solvent system of 100g water-DMSO-n-propanol, wherein the mass ratio of n-propanol: water: DMSO was 5:0.5:0.5, and 2°C / The cooling rate of min is to cool down to 15°C, set the stirring speed to 350rpm, and add 0.3% isobutyl acetate as a bridging agent. At this time, crystals begin to precipitate. Under constant temperature and stirring conditions, the crystals grow for 8 hours. Finally, the crystal paddle was transferred to the filtration system, and the filter cake was dried at 35° C. and a vacuum of 0.1 Mpa for 6 hours to obtain spherical crystals of cefazolin sodium monohydrate, and the process yield was 94%. The obtained spherical particles have uniform particle size distribution, coefficient of variation C.V. = 0.29, average particle diameter equal to 314 μm, and bulk density of 0.42 g / ml. They have high sphericity, good fluidity, fast product separation speed, and the drug product has better fi...

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Abstract

The invention relates to monohydrate cefazolin sodium special particles and a crystallization preparation method thereof. The average particle size of the monohydrate cefazolin sodium special particles is greater than 300mu m, the variable coefficient C.V. of the monohydrate cefazolin sodium special particles is smaller than 0.3, and the bulk density of the monohydrate cefazolin sodium special particles is greater than 0.4g / ml. The crystallization preparation method comprises the following steps: adding cefazolin sodium solid into a solvent system, preparing a solution of which the mass concentration is 0.01-0.12 at 40 DEG C, cooling to be 5-35 DEG C, adding a bridging agent, and stirring at the speed of 100-500rpm so as to separate out crystal; transferring the crystal mush into a filtering system, and drying the filter cakes till constant weight, thereby obtaining the monohydrate cefazolin sodium special crystal. The invention further discloses application of the special particles as an effective medicine component for treating, preventing or delaying various infection diseases caused by sensitive bacteria. The monohydrate cefazolin sodium special particles are simple in process, easy to operate and low in equipment requirement, the process yield is higher than 90.0%, and a spherical medicinal product is relatively excellent in filling property and compression formation property, and is relatively easy in commercial industrial scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine separation, and in particular relates to a spherical particle of cefazolin sodium monohydrate and a crystallization preparation method thereof. Background technique [0002] Cefazolin sodium (cefazolin sodium), its chemical name is (6R,7R)-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)sulfur]methyl]-7 -[(1H-tetrazol-1-yl)acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt. Molecular formula: C 14 h 13 N 8 NaO 4 S 3 , the molecular weight is 476.50. The structural formula is as follows: [0003] [0004] Cefazolin sodium is a semi-synthetic cephalosporin antibiotic widely used clinically at present, and it is a broad-spectrum antibiotic. The antibacterial effect of cefazolin sodium on Gram-negative bacilli is the strongest among the common first-generation cephalosporins, and its effect on Gram-positive bacteria is stronger than that of most second- and third-genera...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36C07D501/12A61K31/546A61P31/04
CPCC07B2200/13C07D501/12C07D501/36
Inventor 郝红勋张娇尹秋响王永莉侯宝红谢闯张美景龚俊波王召鲍颖
Owner TIANJIN UNIV
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