Medicinal composition containing cefdinir cyclodextrin inclusion compound and preparation thereof
A technology of cyclodextrin inclusion complex and cefdinir, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, nano-drugs, etc., to achieve easy dissolution, high water solubility, and little hemolytic side effect. Effect
Inactive Publication Date: 2008-09-17
NANJING NORMAL UNIVERSITY +1
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- Description
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Problems solved by technology
There is no report on the use of cyclodextrin in the preparation of cefdinir preparations
Method used
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Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0074] Mix 28g of β-cyclodextrin with 30ml of pure water, heat, add 10g of cefdinir at 50°C, mix well, add dilute NaHCO drop by drop 3 (0.1M) solution, stirred for 3 hours, neutralized by adding an equal volume of dilute hydrochloric acid (0.1M) dropwise, then cooled at 5°C for 24 hours; removed water under reduced pressure at a temperature not higher than 50°C, and dried to obtain a solid clathrate.
Embodiment 2
[0076] Basically the same as Example 1, but with 100 g of β-cyclodextrin mixed with 100 ml of pure water.
Embodiment 3
[0078] Basically the same as Example 1, but with 1000 g of β-cyclodextrin mixed with 1000 ml of pure water.
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The invention relates to a medicine composition comprising the cefdinir cyclodextrin inclusion compound. The basic composition comprises the cefdinir 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 an advantage of increasing the solubility, stability and activity of the cefdinir. The invention also provides the preparation method of the medicine composition.
Description
technical field [0001] The invention relates to a pharmaceutical composition containing cephalosporin antibiotic cyclodextrin inclusion complex and a preparation method thereof. Background technique [0002] Cefdinir (cefdinir; cefuroxime axetil), trade name: cefdinir or Cefzon, chemical name: [6R-[6α, 7β(z)]]-7-[[(2-amino-4- Thiazolyl)-(oximino)acetyl]amino]-3-vinyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, molecular formula :C 14 h 13 N 5 o 5 S 2 , molecular weight: 395.42. The routine dosage of this product for adults is about 100mg each time, three times a day; the routine dosage for children is 9-18mg / kg per day, taken in three divided doses. Cefdinir is the third generation of new oral cephalosporin antibacterial drugs. The characteristic structure of the aminothioxime side chain not only enhances the antibacterial activity against Gram-negative bacteria and the stability against β-lactamase, but also has strong Gram-positive cocci activity, ...
Claims
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Patent Timeline
Login to View More IPC IPC(8): A61K31/546A61K47/40A61P31/04
CPCC08B37/0015A61K31/724A61K31/545A61K47/48969B82Y5/00A61K31/546A61K47/6951A61P31/04
Inventor 任勇高剑锋韩彬彬马学琴
Owner NANJING NORMAL UNIVERSITY
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