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Sparfloxacin salt and synthesis method and use thereof

A technology of sparfloxacin and its synthesis method, which is applied in the fields of pharmaceutical formulation, drug combination, organic chemistry, etc., and can solve problems such as not being able to meet the preparation requirements of sparfloxacin aqueous solution preparations and restricting the application of parenteral administration preparations

Inactive Publication Date: 2003-08-06
孙卫东
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the current various sparfloxacin salts cannot meet the preparation requirements of sparfloxacin aqueous solution preparations, which limits its application in parenteral administration preparations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Synthesis of Sparfloxacin Gluconate

[0013] (1) Add 10g of sparfloxacin, 4.6g of gluconolactone, 100ml of water, and shake well.

[0014] (2) Heating to reflux for 20 minutes, adding activated carbon after dissolving everything, stirring and cooling to room temperature, and filtering.

[0015] (3) Distill about 80ml of the filtrate under reduced pressure, pour it into a 500ml beaker, add 300ml of ethanol, and put it in the refrigerator overnight.

[0016] (4) Suction filtration, the solid was washed 3 times with 20 ml of absolute ethanol, drained, put into a vacuum drying oven at −0.095 MPa, and baked at 50° C. for 6 hours, the yield was about 80%.

Embodiment 2

[0018] Synthesis of Sparfloxacin Glucuronate

[0019] Glucuronolactone 4.5g, sparfloxacin 10g, the steps are the same as in Example 1.

Embodiment 3

[0021] Preparation of infusion containing sparfloxacin gluconate (containing 0.2% sparfloxacin), specification 100ml: sparfloxacin 200mg

[0022] Take 3.0 g of sparfloxacin gluconate, dissolve it in 800 ml of solution, adjust the pH to 3.8 with gluconolactone, add 9 g of sodium chloride, dissolve and filter, add water for injection to 1000 ml, pour into nitrogen gas and seal at 115 °C, 30 minutes to sterilize. 100ml per bottle, placed for 24 months at room temperature and protected from light, the solution did not form precipitates, and the pH did not change. After HPLC detection, the appearance content was within the range.

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Abstract

The present invention discloses a neoquinonones antibacterial agent, its synthesis method and application, in particular, discloses a sparflaxacin salt, its synthesis and application. It utilizes sparflaxacin and polyhydroxyl monocarboxylic acid, are used and reacted to obtain the invented sparflaxacin salt. It is made into crystal, easy to dissolve in water, good in aqueous solution stability, and can be made into infusion preparation and injection for antibacterial therapy, and overcomes the defect of existent sparflaxacin salt, for example sparflaxacin lactate whose aqueous solution is not stable.

Description

technical field [0001] The invention relates to a new quinolone antibacterial drug, its synthesis method and application, in particular to a sparflaxacin salt, its synthesis method and application. Background technique [0002] Sparfloxacin is a broad-spectrum antibacterial drug of the new quinolones. Because its antibacterial spectrum is wider than that of ofloxacin quinolones, its capsule preparations and tablets have been widely used at home and abroad, and have good clinical effects. The market The prospects are very promising. However, since sparfloxacin is insoluble in water, it cannot be directly prepared into an aqueous solution dosage form, so its application is limited. In order to improve and make up for this defect, it is made into salt to increase its solubility in water and correspondingly increase its use value. However, the reported sparfloxacin saline solution has poor stability, is easily degraded, and is not easy to store, such as sparfloxacin lactate. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/495A61P31/00C07D241/04
Inventor 孙卫东
Owner 孙卫东
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