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Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof

A technology of cyclodextrin inclusion compound and cefixime, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, nano-medicines, etc., to achieve high water solubility, easy dissolution, and small hemolytic side effects Effect

Inactive Publication Date: 2008-09-17
NANJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the use of cyclodextrin in the preparation of cefixime preparations

Method used

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  • Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof
  • Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof
  • Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Mix 10 grams of β-cyclodextrin with 10 milliliters of pure water, heat, add 4.0 grams of cefixime (equimolar) at a temperature of 50 ° C, mix and stir for 3 hours, then cool at 5 ° C for 24 hours; filter, Wash twice with water, and dry under pressure at room temperature to obtain a solid clathrate.

Embodiment 2

[0073] Mix 14 grams of hydroxypropyl-β-cyclodextrin with 20 milliliters of pure water, heat, add 4.0 grams of cefixime at a temperature of 50 ° C, add dilute alkali and mix thoroughly to dissolve, then add dilute acid to neutralize properties, stirring and cooling, and then 0.25 membrane filtration, 50 ° C drying under reduced pressure, that is, a solid clathrate.

Embodiment 3

[0075] Essentially the same as Example 2, but with 16 grams of sulfobutyl-β-cyclodextrin.

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PUM

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Abstract

The invention provides a medicine composition comprising the cefixime cyclodextrin inclusion compound. The basic composition comprises the cefixime and the pharmacy-acceptable cyclodextrin; the cyclodextrin is chosen from one or a plurality of Beta -cyclodextrin, sulfobutyl- Beta -cyclodextrin, hydroxypropyl- Beta -cyclodextrin or hydroxypropyl-sulfobutyl- Beta -cyclodextrin. The invention has the advantages of increasing the solubility and stability of the medicine, and higher activity. The invention also provides the preparation method of the medicine composition.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing cefixime cyclodextrin inclusion complex and a preparation method thereof. Background technique [0002] Cefixime (cefixime) is a third-generation oral cephalosporin, an important antibiotic, chemical name: (6R, 7R)-7-{[(Z)-2-(2-aminothiazol-4-yl )-2-[(carboxymethoxy)imine]acetyl]amino}-3-vinyl-8-oxo-5-thia-1-azabicyclo[4,2,0]-2- Octene-2-carboxylic acid, molecular formula: C 16 h 15 N 5 o 7 S 2 , molecular weight: 453.44. The drug was developed and marketed by Fujisawa Pharmaceutical Industry Co., Ltd., and its trade name is Cefspan. At present, cefixime has become the oral cephalosporin with the largest market share. It has been widely clinically used in more than 80 countries. [0003] Cefixime has broad antibacterial spectrum, strong effect, long duration of effective concentration, stable to β-lactamase, wide distribution in the body, etc. It is used for urinary system inflamm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K47/40A61P31/04
CPCA61K9/0019A61K9/1652C08B37/0015A61K31/724A61K31/545B82Y5/00A61K31/546A61K47/48969A61K9/19A61K47/6951A61P31/04
Inventor 任勇王晓洁马学琴
Owner NANJING NORMAL UNIVERSITY
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