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Cefadroxil tablet and preparation method thereof

A technology of cefadroxil tablet and padroxil tablet, which is applied in the field of medicine, can solve the problems of easy hygroscopic degradation, unfavorable long-term storage, safety and effectiveness hidden dangers, etc., and achieve the goal of improving bioavailability and stability Effect

Active Publication Date: 2016-05-04
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the existing cefadroxil raw materials are unstable under conditions such as high temperature and high humidity, and are easily degraded by moisture absorption, the quality stability of the preparation product is poor, which is not conducive to long-term storage, which affects the safety and effectiveness in clinical use. bring hidden danger

Method used

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  • Cefadroxil tablet and preparation method thereof
  • Cefadroxil tablet and preparation method thereof
  • Cefadroxil tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of embodiment 1 cefadroxil of the present invention

[0044] (1) 100 g of cefadroxil crude product is dissolved in 800 ml of mixed solvent A of tetrahydrofuran and water with a volume ratio of 1:2, and ammonia water is added dropwise to adjust the pH value to 8.0;

[0045] (2) Filter, add dropwise acetic acid to the filtrate to adjust the pH value to 6.8, then slowly add 320ml dropwise of a mixed solvent B of 2-butanone and chloroform with a volume ratio of 1:0.3, stir while adding, and the stirring speed is 20 rpm / Minute;

[0046] (3) Cool down to 5°C, crystallize, and grow crystals for 4 hours;

[0047] (4) Filtrate to obtain a solid, and dry it under reduced pressure at 35° C. for 3 hours to obtain 97.92 g of cefadroxil.

[0048] The cefadroxil prepared in this example has an X-ray powder diffraction pattern measured by Cu-Kα rays at 2θ of 4.27±0.2°, 8.52±0.2°, 17.13±0.2°, 19.92±0.2°, 20.52±0.2° , 21.44±0.2°, 23.87±0.2°, 25.09±0.2°, 25.85±0.2°, 29...

Embodiment 2

[0049] The preparation of embodiment 2 cefadroxil of the present invention

[0050] (1) Dissolve 100 g of cefadroxil crude product in 600 mL of mixed solvent A of tetrahydrofuran and water with a volume ratio of 1:2, and add ammonia water dropwise to adjust the pH value to 8.2;

[0051] (2) Filter, add dropwise acetic acid to the filtrate to adjust the pH value to 7.0, then slowly add 240ml dropwise of a mixed solvent B of 2-butanone and chloroform with a volume ratio of 1:0.3, stir while adding, and the stirring speed is 15 rpm / Minute;

[0052] (3) Cool down to -10°C, crystallize, and grow crystals for 2 hours;

[0053](4) Filtrate to obtain a solid, and dry it under reduced pressure at 30° C. for 2 hours to obtain 97.31 mg of cefadroxil.

[0054] The X-ray powder diffraction pattern and differential scanning calorimetry pattern of the cefadroxil prepared in this embodiment are the same as those in Example 1, and its purity as determined by high performance liquid chromato...

Embodiment 3

[0055] The preparation of embodiment 3 cefadroxil of the present invention

[0056] (1) Dissolve 100 g of cefadroxil crude product in 1000 mL of mixed solvent A of tetrahydrofuran and water at a volume ratio of 1:2, and add ammonia water dropwise to adjust the pH value to 7.6;

[0057] (2) Filter, add dropwise acetic acid to the filtrate to adjust the pH value to 6.5, then slowly add 400ml dropwise of a mixed solvent B of 2-butanone and chloroform with a volume ratio of 1:0.3, stir while adding, and the stirring speed is 25 rpm / Minute;

[0058] (3) Cool down to 0°C, crystallize, and grow crystals for 6 hours;

[0059] (4) Filtrate to obtain a solid, and dry under reduced pressure at 40°C for 4 hours to obtain 96.27 mg of cefadroxil.

[0060] The X-ray powder diffraction pattern and differential scanning calorimetry pattern of the cefadroxil prepared in this embodiment are the same as those in Example 1, and its purity as determined by high performance liquid chromatography ...

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Abstract

The invention relates to a cefadroxil tablet and a preparation method thereof, and belongs to the technical field of medicines. The cefadroxil tablet comprises the following components in parts by weight: 125-500 parts of cefadroxil, 35-60 parts of starch, 40-120 parts of 10% starch paste, 2-6 parts of magnesium stearate, and 3-12 parts of sodium carboxymethyl starch, wherein X-ray powder diffraction pattern of cefadroxil has characteristic peaks at 2theta of 4.27+ / -0.2 degree, 8.52+ / -0.2 degree and the like; and the differential scanning calorimetry pattern of cefadroxil has characteristic peaks at 189-190 DEG C. Compared with the prior art, the impurity content is not significantly changed under the conditions of high temperature, high humidity and strong light, and the stability is greatly improved; pharmacokinetic experiment results show that the bioavailability of the cefadroxil tablet is significantly improved compared with that of commercially available cefadroxil tablets.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to an anti-infection drug preparation and a preparation method thereof, in particular to a cefadroxil tablet and a preparation method thereof. Background technique [0002] Cefadroxil, chemical name (6R,7R)-3-methyl-7-[(R)-2-amino-2-(4-hydroxyphenyl)acetamido]-8-oxo-5-sulfur Hetero-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate has the structure shown in the following formula: [0003] [0004] Cefadroxil is a semi-synthetic first-generation oral cephalosporin, which has strong anti-gram-positive and certain anti-gram-negative effects, is relatively stable to penicillinase, and has fewer allergic reactions. It has the characteristics of good oral absorption, strong antibacterial power, enzyme resistance, high curative effect, long maintenance time of blood drug concentration, low toxicity, long half-life, unaffected by food, and few side effects. Clinically, it is w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/545A61K47/36A61P31/04C07D501/22C07D501/12
CPCA61K9/2059A61K9/28A61K31/545C07D501/12C07D501/22
Inventor 郑雪清高志峰王唤雨马园园张威
Owner CSPC OUYI PHARM CO LTD
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