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Cefadroxil compound and pharmaceutical composition comprising same

A technology of cefadroxil compound and cefadroxil hydrate, applied in the field of cefadroxil compounds and pharmaceutical compositions thereof, can solve the problems of easy moisture absorption, limited application, poor solubility of cefadroxil, etc., and achieve uniform particle size , to avoid agglomeration, the effect of uniform particle size distribution

Active Publication Date: 2015-03-25
金鸿药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, the cefadroxil of the prior art has poor solubility and is easy to absorb moisture, which limits its application to a certain extent

Method used

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  • Cefadroxil compound and pharmaceutical composition comprising same
  • Cefadroxil compound and pharmaceutical composition comprising same
  • Cefadroxil compound and pharmaceutical composition comprising same

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0045] Embodiment 1, the preparation of cefadroxil hydrate crystal

[0046] 1) Dissolving the cefadroxil bulk drug in the mixed solution A made of water, acetonitrile and tetrahydrofuran, adjusting the pH value to 2.0 with hydrochloric acid to obtain the water / acetonitrile / tetrahydrofuran solution of cefadroxil, wherein the cefadroxil bulk drug The weight to volume ratio with mixed solution A (the volume ratio of water, acetonitrile and tetrahydrofuran in mixed solution A is 10:3:1) is 1g:50ml;

[0047] 2) Under a sound field with a frequency of 15KHz and an output power of 30W, add dropwise at 50ml / min a mixed solution B made of acetone and ether at 2°C under stirring at a stirring speed of 100 rpm (in the mixed solution B The volume ratio of acetone and ether is 1:3), the volume of the mixed solution B of acetone and ether added dropwise is 3 times of the water / acetonitrile / tetrahydrofuran solution of cefadroxil; after the dropwise addition, turn off the sound field and let ...

Embodiment 2

[0050] Embodiment 2, the preparation of cefadroxil hydrate crystal

[0051] 1) Dissolving the cefadroxil bulk drug in the mixed solution A made of water, acetonitrile and tetrahydrofuran, adjusting the pH value to 2.4 with hydrochloric acid to obtain the water / acetonitrile / tetrahydrofuran solution of cefadroxil, wherein the cefadroxil bulk drug The weight to volume ratio of mixed solution A (the volume ratio of water, acetonitrile and tetrahydrofuran in mixed solution A is 10:6:2) is 1g:100ml;

[0052] 2) Under a sound field with a frequency of 22KHz and an output power of 60W, add dropwise at 100ml / min the mixed solution B (in the mixed solution B) made of acetone and ether at 8°C under stirring at a stirring speed of 120 rpm The volume ratio of acetone and ether is 1:6), the volume of the mixed solution B of acetone and ether added dropwise is 8 times that of the water / acetonitrile / tetrahydrofuran solution of cefadroxil; after the dropwise addition, turn off the sound field ...

Embodiment 3

[0055] Embodiment 3, the preparation of cefadroxil hydrate crystal

[0056] 1) Dissolving the cefadroxil bulk drug in the mixed solution A made of water, acetonitrile and tetrahydrofuran, adjusting the pH value to 2.2 with hydrochloric acid to obtain the water / acetonitrile / tetrahydrofuran solution of cefadroxil, wherein the cefadroxil bulk drug The weight to volume ratio with mixed solution A (the volume ratio of water, acetonitrile and tetrahydrofuran in mixed solution A is 10:5:3) is 1g:80ml;

[0057] 2) Under a sound field with a frequency of 20KHz and an output power of 50W, add dropwise at 80ml / min a mixed solution B (in the mixed solution B) made of acetone and ether at 5°C under stirring at a stirring speed of 110 rpm. The volume ratio of acetone and ether is 1:5), the volume of the mixed solution B of acetone and ether added dropwise is 5 times that of the water / acetonitrile / tetrahydrofuran solution of cefadroxil; after the dropwise addition, turn off the sound field a...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a cefadroxil compound and pharmaceutical composition comprising the same. The cefadroxil compound is a cefadroxil hydrate with the molecular formula of C16H17N3O5S*3.5H2O, and the structural formula is shown in the specification. Various pharmaceutically-acceptable dosage forms can be prepared from the pharmaceutical composition comprising the cefadroxil compound, and chewable tablets and capsules are preferred. The cefadroxil compound has the advantage of capability of significantly improving the water solubility and the hygroscopicity of cefadroxil compounds.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a cefadroxil compound and a pharmaceutical composition thereof. Background technique [0002] Cefadroxil, chemical name is (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, which is a well-known antibiotic with antibacterial activity, was developed by Briestol-Meyer, USA The second-generation oral cephalosporins have the characteristics of broad antibacterial spectrum, weak antigenicity, good curative effect, low toxicity and safe use. [0003] At present, the cefadroxil products on the market are generally cefadroxil monohydrate, which is relatively stable in the external environment and easy to store. The molecular formula of cefadroxil monohydrate is C 16 h 17 N 3 o 5 S·H 2 O, molecular weight 381.41. The chemical structural formula of cefadroxil without water of...

Claims

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Application Information

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IPC IPC(8): C07D501/22C07D501/12A61K31/545
CPCC07D501/12C07D501/22
Inventor 上官清
Owner 金鸿药业股份有限公司
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