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Prulifloxacin active body injection

An injection, ulifloxacin technology, applied in the directions of organic active ingredients, drug delivery, antibacterial drugs, etc., can solve the problems of unsatisfactory antibacterial activity, and achieve the effects of reliable action, fast absorption, and reduced production costs.

Inactive Publication Date: 2008-05-07
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is considered that the antibacterial activity in vivo is not ideal, and therefore its prodrug Prulifloxacin (Prulifloxacin) was developed (Masakuni Ozakia et al. Chemotherapy 1998, 44(1): 21-30)

Method used

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  • Prulifloxacin active body injection
  • Prulifloxacin active body injection

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Take 10g of Ulifloxacin, add it to a 20L batching bucket, add 8L of water, stir evenly, add about 8mL of 10% hydrochloric acid while stirring, stir until dissolved, measure the pH to 6.0, add 800g of glucose, stir to dissolve, add water for injection To 10L, heat up to 80°C, heat and stir for 30 minutes, cool to 30°C, decarbonize through filter paper, then fine filter through a 0.22μm filter membrane, fill, cap, and sterilize at 110°C for 30 minutes.

Embodiment 2

[0030] Take 50g of Ulifloxacin, add it to a 20L batching bucket, add 7L of water, stir evenly, add about 25mL of 10% hydrochloric acid while stirring, stir until it dissolves, add 500g of glucose, stir to dissolve, adjust the pH to 4.5 with dilute hydrochloric acid, and replenish Add water for injection to 10L, heat up to 70°C, heat and stir for 50 minutes, cool to 30°C, decarbonize through filter paper, then fine filter through a 0.22μm filter membrane, fill, cap, and sterilize at 110°C for 30 minutes.

Embodiment 3

[0032] Take 100g of ulifloxacin, add it to a 20L batching bucket, add 8L of water, stir evenly, add about 20mL of 10% lactic acid while stirring, stir until dissolved, add 1000g of glucose, stir to dissolve, adjust the pH to 5 with 10% lactic acid, Add water for injection to 10L, heat up to 80°C, heat and stir for 30 minutes, cool to 30°C, decarbonize through filter paper, then fine filter through a 0.22μm filter membrane, fill, cap, and sterilize at 110°C for 30 minutes .

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PUM

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Abstract

The invention relates to the injectant of Prunus africana bark active mass Ulifloxacin (Ulifloxacin, code name NM394) with a chemical name of (minus and plus)-6-fluorine-1-methyl-7-(1-piperazine radical)-4-oxo-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic acid and the preparation method thereof. The invention aims at providing Ulifloxacin injectant directly used for intravenous injection, so as to lead the active medicine Ulifloxacin to directly enter in blood liquid and exerting action quickly.

Description

technical field [0001] The present invention relates to the injection of Ulifloxacin (Ulifloxacin), the active substance of antibacterial drug prulifloxacin, and its preparation method, especially its intravenous injection and its preparation method. Background technique [0002] The chemical name of Ulifloxacin is (±) 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazine[3,2-a]quinone Phenyl-3-carboxylic acid, the structural formula is as follows: [0003] [0004] JP63107990 disclosed this quinolone compound on May 12, 1988, and JP3218383 disclosed the preparation of optically pure compounds of ulifloxacin on September 25, 1991. However, there is no relevant report on ulifloxacin injection in the literature. [0005] Ulifloxacin has strong antibacterial activity against Gram-positive bacteria and negative bacteria in vitro, especially the activity against Pseudomonas aeruginosa is significantly higher than that of similar products on the market. It is a new high-...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/08A61P31/04
Inventor 高勇陆艳红
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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