A kind of cefadroxil granule preparation and preparation method thereof

A technology of cefadroxil granules and fadroxil granules, applied in the field of medicine, can solve problems such as easy hygroscopic degradation, hidden safety hazards, unfavorable long-term storage, etc., and achieve the effects of improved bioavailability and improved stability

Active Publication Date: 2019-03-01
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the cefadroxil preparations listed in the domestic market have dosage forms such as granules, dispersible tablets, tablets, capsules, etc., but because the existing cefadroxil raw materials are unstable under conditions such as high temperature and high humidity, they are easy to absorb moisture and degrade, resulting in the failure of the preparation products. The quality stability is poor, which is not conducive to long-term storage, and brings hidden dangers to the safety in clinical use

Method used

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  • A kind of cefadroxil granule preparation and preparation method thereof
  • A kind of cefadroxil granule preparation and preparation method thereof
  • A kind of cefadroxil granule preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The preparation of embodiment 1 cefadroxil of the present invention

[0032] (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;

[0033] (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;

[0034] (3) Cool down to 5°C, crystallize, and grow crystals for 4 hours;

[0035] (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.

[0036] 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

[0037] The preparation of embodiment 2 cefadroxil of the present invention

[0038] (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;

[0039] (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;

[0040] (3) Cool down to -10°C, crystallize, and grow crystals for 2 hours;

[0041] (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.

[0042] 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 chromat...

Embodiment 3

[0043] The preparation of embodiment 3 cefadroxil of the present invention

[0044] (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;

[0045] (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;

[0046] (3) Cool down to 0°C, crystallize, and grow crystals for 6 hours;

[0047] (4) Filtrate to obtain a solid, and dry under reduced pressure at 40°C for 4 hours to obtain 96.27 mg of cefadroxil.

[0048] 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 granular preparation and a preparation method thereof, and belongs to the technical field of medicines. The granular preparation is prepared from, by weight, 100 parts of cefadroxil, 780-820 parts of cane sugar, 1-3 parts of beta-cyclic dextrin, 0.5-1.5 parts of sucrose stearate and the like, wherein the positions, where 2 theta equals to 4.27+ / -0.2 degrees, 8.52+ / -0.2 degrees and the like, of an X-ray powder diffraction pattern of cefadroxil have characteristic peaks; the positions, within the range of 189-190 DEG C, of a differential scanning heat analysis graph, of cefadroxil have the maximum absorption peaks. Due to the fact that cefadroxil has excellent pharmaceutical properties, the impurity content of the prepared granular preparation is free of obvious changes under high temperature, high humidity and strong light, and the stability of the preparation is greatly improved; it is shown through pharmacokinetics experiment results that compared with cefadroxil granular preparations sold on the market, the bioavailability of the cefadroxil granular preparation is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an anti-infection drug preparation and a preparation method thereof, in particular to a cefadroxil granule preparation 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. Clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/545A61K47/40A61P31/04C07D501/22C07D501/12
CPCA61K9/1652A61K31/545C07B2200/13C07D501/12C07D501/22
Inventor 周杰韩彩霞张上上刘磊甘丽倩
Owner CSPC OUYI PHARM CO LTD
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