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Sulphur butyl ether-beta-schardinger dextrin inclusion compound of cephalosporin sulbactam ester

A technology of inclusion compound of cephalosporin sulbactam mexetil and cyclodextrin, which is applied in the field of medicine and can solve problems such as not involving

Inactive Publication Date: 2009-12-23
ZHEJIANG YONGNING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] There is no research on the inclusion complex of cephalosporin sulbactam mexoxil compound with β-lactamase resistance and sulfobutyl ether-β-cyclodextrin in the published information

Method used

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  • Sulphur butyl ether-beta-schardinger dextrin inclusion compound of cephalosporin sulbactam ester
  • Sulphur butyl ether-beta-schardinger dextrin inclusion compound of cephalosporin sulbactam ester
  • Sulphur butyl ether-beta-schardinger dextrin inclusion compound of cephalosporin sulbactam ester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 0.643 g of ceftamethoxil to 40 ml of an aqueous solution containing 8.8 g of sulfobutyl ether-β-cyclodextrin, stir, sonicate, dissolve, filter, and freeze-dry to obtain white ceftamet sulbactam Ester sulfobutyl ether-β-cyclodextrin inclusion compound powder.

[0031] Preparation of powder injection:

[0032] 500 g of the clathrate powder (calculated as ceftaxime) was aseptically divided into 1000 or 500 tubes to obtain ceftamet sulbactam medoxomil powder injections of different specifications.

Embodiment 2

[0034] Add 0.67 g of cefuroxime sulbactam axetil to 45 ml of an aqueous solution containing 11 g of sulfobutyl ether-β-cyclodextrin, stir, sonicate, dissolve, filter, and freeze-dry to obtain white cefuroxime sulbactam axetil The sulfobutyl ether-β-cyclodextrin inclusion compound powder.

[0035] Powder injection preparation

[0036] 500 g of the clathrate powder (calculated as cefuroxime) was aseptically divided into 2000 or 500 or 250 tubes to obtain cefuroxime sulbactam mexetil powder injections of different specifications.

Embodiment 3

[0038] Add 0.6 g of cephradine sulbactam medoxotil to 50 ml of an aqueous solution containing 13.3 g of sulfobutyl ether-β-cyclodextrin, stir, sonicate, filter, concentrate, and freeze-dry to obtain white sulfobutamic acid cephradine sulbactam mexetil Ether-β-cyclodextrin inclusion compound powder.

[0039] Powder injection preparation

[0040] Above-mentioned clathrate powder (calculated as cephradine) 1000g, aseptically sub-packed into 2000 or 1000, to obtain cephradine-sulbactam medoxomil powder injections of different specifications.

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Abstract

The invention provides a sulphur butyl ether-beta-schardinger dextrin inclusion compound of a beta-lactam enzyme-resistant cephalosporin ester compound. In the invention, a sulphur butyl ether-beta-schardinger dextrin water solution and a cephalosporin sulbactam ester compound are mixed, stirred, dissolved and concentrated into a dry state or dried by spraying or freeze-dried to obtain inclusion compound powder, and powder needles used for injection and oral preparations can be prepared by adding or not adding preparation auxiliary materials. The inclusion compound has the characteristics of good water-solubility, good stability and high bioavailability, and the curative effect of cephalosporin sulbactam ester is fully ensured after the inclusion compound is prepared into a preparation. The oral administration of the preparation prepared from the inclusion compound can achieve the aim of quick acting, and injection administration can meet the demands of different requirements in clinic; in addition, the bioavailability of the oral administration is high, wastes are reduced, and conditions for safe application and reasonable application are created.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sulfobutyl ether-beta-cyclodextrin inclusion compound of cephalosporin sulbactam medoxil and a preparation method thereof. Background technique [0002] Patent CN1637002A discloses the general formula (I) of cephalosporin sulbactam mexetil compound: [0003] [0004] But the cephalosporin sulbactam mexil of this general formula (I) is insoluble in water, and the bioavailability is poor. [0005] The structures of the six cephalosporin sulbactam mexoxil are as follows: [0006] Ceftamet sulbactam axetil Cefuroxime sulbactam axetil [0007] [0008] Cephradine sulbactam mexetil Cefalexin sulbactam mexetil [0009] [0010] Cefadroxil sulbactam mexetil Cefaclor sulbactam mexetil [0011] [0012] Sulbactam is not absorbed directly when taken orally. This cephalosporin sulbactam mexoxil is hydrolyzed into two active substances, cephalosporin and sulbactam, thereby av...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/545A61K31/546A61K9/20A61K9/48A61K9/16A61K9/14A61K9/19A61K31/04A61K47/69
Inventor 叶凤起方善综卢敏余葆春张君
Owner ZHEJIANG YONGNING PHARMA
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