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Conjugate of sarafloxacin and its preparing process and application

A technology of sarafloxacin and conjugates, which is applied in the field of sarafloxacin conjugates and its preparation, achieving the effect of saving inspection time and facilitating on-site operation

Inactive Publication Date: 2006-03-01
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as far as we know, there is no report on the synthesis of sarafloxacin immunogen and its antibody preparation in the world

Method used

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  • Conjugate of sarafloxacin and its preparing process and application
  • Conjugate of sarafloxacin and its preparing process and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Preparation of solution A: In a 50ml circular reaction bottle, add 13.9mg (0.042mmol) of sarafloxacin (0.042mmol), 19.33mg (0.168mmol) of hydroxysuccinic acid imide (NHS), ethyl [3- (Dimethylamino)propyl]carbodiimide hydrochloride (EDC.HCl) 48.3mg (0.252mmol), dissolved in 10ml of dimethylformamide (DMF). React for 4 hours. Solution A is obtained. spare.

[0040] (2) Preparation of Solution B: In a 100ml circular reaction bottle, 476mg of BSA was added to 50ml of PBS (pH=7.4, 0.01M). Solution B is obtained. spare.

[0041] (3) Preparation of sarafloxacin immunogen conjugate: gradually add solution A to solution B at 20°C under stirring. React for 4 hours. Obtain sarafloxacin immunogen solution. Dialyze against PBS buffer for three days, changing the dialysate every 12 hours. Centrifuge at high speed (20,000g) for 30 minutes. The supernatant was freeze-dried to obtain 412 mg of white solid powder, which was the crude sarafloxacin immunogen. Sephadex-G75 (Si...

Embodiment 2

[0045] (1) Preparation of solution A: in a 50ml circular reaction flask, while stirring, add 20.0 mg (0.060 mmol) of sarafloxacin, 19.33 mg (0.240 mmol) of hydroxysuccinimide (NHS), ethyl[3- (Dimethylamino)propyl]carbodiimide hydrochloride (EDC.HCl) 69.0 mg (0.360 mmol) was dissolved in 15 ml of dimethylformamide (DMF). The reaction was carried out for 4 hours. Solution A is obtained. spare.

[0046] (2) Preparation of solution B: In a 100 ml round reaction flask, 685 mg of BSA was added to 60 ml of PBS (pH=7.4, 0.01M). Solution B was obtained. spare.

[0047] (3) Preparation of Sarafloxacin immunogen conjugate: solution A was gradually added to solution B under stirring at 25°C. The reaction was carried out for 4 hours. A Sarafloxacin immunogen solution was obtained. Dialyze against PBS buffer for 78 hours, changing the dialysate every 12 hours. Centrifuge at high speed (20,000 g) for 30 minutes. The supernatant was freeze-dried to obtain 482 mg of white solid powder...

Embodiment 3

[0049] (1) Preparation of solution A: in a 50ml circular reaction flask, while stirring, add 40.0 mg (0.120 mmol) of sarafloxacin, 38.66 mg (0.480 mmol) of hydroxysuccinimide (NHS), ethyl[3- (Dimethylamino)propyl]carbodiimide hydrochloride (EDC.HCl) 138.0 mg (0.720 mmol) was dissolved in 15 ml of dimethylformamide (DMF). The reaction was carried out for 6 hours. Solution A is obtained. spare.

[0050] (2) Preparation of solution B: In a 100 ml round reaction flask, 1.2 g of BSA was added to 80 ml of PBS (pH=7.4, 0.01 M). Solution B was obtained. spare.

[0051] (3) Preparation of Sarafloxacin immunogen conjugate: solution A was gradually added to solution B at 30° C. with stirring. The reaction was carried out for 6 hours. A Sarafloxacin immunogen solution was obtained. Dialyze against PBS buffer for 70 hours, changing the dialysate every 10 hours. Centrifuge at high speed (20,000 g) for 30 minutes. The supernatant was lyophilized to obtain 762 mg of white solid powde...

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Abstract

The present invention discloses a coupled product of salasaxing. Said invention also provides its general formula. It is made up by using Salasaxing hapten and carrier substance capable of producing immunogenicity, optimum is bovine serum protein, and making them undergo the process of coupling reaction. Said invention also provides the concrete steps of its preparation method and its application for preparing enzyme-linked immunosorbent assay kit.

Description

technical field [0001] The invention relates to a conjugate of quinolone antibiotics and its preparation method and application, in particular to a conjugate of sarafloxacin and its preparation method and application. Background technique [0002] The following titles involved in the present invention apply to the entire specification and claims: [0003] BSA=Bovine Serum Albumin (Bovine Serum Albumin), product of Sigma Company [0004] PBS=Phosphate Buffered Saline (0.01M, pH=7.40) [0005] Sephadex-G75 = dextran gel, product of Sigma [0006] Sarafloxacin-EDC=Active intermediate formed by sarafloxacin and carbodiimide [0007] Glutar=(Glutaraldehyde) glutaraldehyde, product of Shanghai Chemical Reagent Company [0008] Dialysis membrane: product of United Carbide [0009] Sarafloxacin (sarafloxacin) belongs to the quinolone antibiotics. Because of its broad antibacterial spectrum and strong bactericidal ability, this kind of antibiotics is widely used in livestock an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N33/53G01N33/531
Inventor 郗日沫卢圣欣张玉兰
Owner SHANDONG UNIV
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