Water-soluble salt of aspartic acid carbostyril series antibacterial drugs and injection dosage forms thereof

A technology of aspartate quinolone and aspartate quinolone, which is applied in the field of injection dosage forms, can solve the problems of nosocomial infection, insufficient understanding of antibiotic side effects, abuse of prescription drugs and the like

Inactive Publication Date: 2008-05-21
SHENYANG WOSEN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the lack of awareness of the side effects of antibiotics and the abuse of prescription drugs, adverse reactio...

Method used

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  • Water-soluble salt of aspartic acid carbostyril series antibacterial drugs and injection dosage forms thereof
  • Water-soluble salt of aspartic acid carbostyril series antibacterial drugs and injection dosage forms thereof
  • Water-soluble salt of aspartic acid carbostyril series antibacterial drugs and injection dosage forms thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Add 0.01mol of sparfloxacin, 0.01mol of L-aspartic acid and 40ml of water into a 100ml beaker, stir at room temperature for 10min, the raw materials dissolve rapidly, the resulting solution is a transparent liquid, measure the pH value of the solution with a pH meter is 6.2. Concentrate the obtained salt solution under reduced pressure, then transfer it to a petri dish and place it in a desiccator, let it volatilize the water, after the water is removed, it becomes a transparent glassy solid, and then continue to place it to let the water evaporate completely, gradually turning into a yellow solid , The obtained product weighs 5.20g. The product is the water-soluble salt of the quinolone drugs of the present invention. Add 30ml of water to the solid, shake it, and within about 3 minutes, the solid is completely dissolved.

Embodiment 2

[0029] Take 1.34 g of sparfloxacin L-aspartate prepared in Example 1, add 9.0 g of sodium chloride and add water to 1000 ml to dissolve, add 0.1% charcoal for needles, stir at room temperature for 15 min, filter, pass through 0.2 μm Microporous filter membrane, filled in a colorless infusion bottle, 100ml / bottle, made into an infusion according to the routine, to get final product.

Embodiment 3

[0031] Take 1.34 g of sparfloxacin L-aspartate prepared in Example 1, add water to 20 ml, dissolve, add 0.1% charcoal for needles, stir at room temperature for 15 min, filter, pass through a 0.2 μm microporous filter membrane, pour Packed in colorless glass ampoules, 2ml / branch, made into injection solution according to routine, that is to say.

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Abstract

The invention provides an aspartate quinolone antibiotics water-soluble salt and the injection formulation thereof, including sparfloxacin, gatifloxacin, rufloxacin, pefloxacin, tosufloxacin, moxifloxacin, and so on; the invention improves the water solubility of quinolone antibiotics and enhances the anti-bacterial effect of quinolone antibiotics. Compared with the oral liquid of quinolone drugs of the prior art, the invention has the advantages that: water solubility of the drug is good, as the drug enters the blood directly, the invention can not only achieve treatment function rapidly, but can also be absorbed by the human body fully, and the invention has significant effects in the two aspects of fast onset of action and low consumption. Compared with the injection of the quinolone drugs of the prior art, the invention has the advantages that: due to the existence of the L-aspartate, the antibacterial activity of quinolone drugs can be enhanced.

Description

technical field [0001] The invention relates to a water-soluble salt of aspartic acid quinolone antibacterial drugs and an injection form made of the water-soluble salt. Background technique [0002] The advent of quinolones has brought good news to many patients. With the long-term application of drugs, bacterial drug resistance has gradually attracted people's attention and has become a hot spot in many countries around the world. Due to the lack of understanding of the side effects of antibiotics and the abuse of prescription drugs, adverse reactions also occur from time to time, which also lead to the growth of drug-resistant bacteria and serious nosocomial infections. In the face of new national regulations on antibiotics, the pharmaceutical industry has strengthened the development of new products. In the past two years, many new faces have appeared in quinolone drugs in typical urban sample hospitals, such as sparfloxacin, gatifloxacin, rufloxacin, Pefloxacin, Tosufl...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K31/4375A61K31/542A61K9/08A61K9/14A61P31/04
Inventor 徐飒
Owner SHENYANG WOSEN PHARMA INST
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