Prulifloxacin water-soluble salt and its injection formulation

A technology of prulifloxacin and water-soluble salts, which is applied in the fields of organic active ingredients, powder delivery, drug delivery, etc., can solve problems that have not yet been marketed, and achieve quick results and good water solubility

Inactive Publication Date: 2004-12-29
魏雪纹 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it has not been listed for sale in other countries including China

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 0.01mol prulifloxacin, 0.01mol lactic acid and 30ml water were added in a 100ml glass bottle, stirred at room temperature for 10 minutes and the raw materials were dissolved rapidly, the resulting solution was colorless and transparent, and the pH value of the solution measured with a pH meter was 4.3. 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, and turn into a transparent glassy solid after the water is removed, continue to place it to let the water evaporate completely, and gradually turn into a white solid , The obtained product weighs 5.85g. The product is the water-soluble salt of prulifloxacin of the present invention. Add 30 ml of water to the solid and stir with a glass rod. Within one minute, the solid is completely dissolved.

[0019] The solution is diluted with water according to the predetermined solubility, sterilized and filtered, put into an am...

Embodiment 2

[0021] Add 0.01mol prulifloxacin, 0.01mol methanesulfonic acid and 30ml water into a 100ml glass bottle, stir at room temperature for 10 minutes and the raw material dissolves rapidly, the resulting solution is colorless and transparent, and the pH of the solution measured with a pH meter is 5.1. 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, and turn into a transparent glassy solid after the water is removed, continue to place it to let the water evaporate completely, and gradually turn into a white solid , the weight of the obtained product is about 6.15g. This product is the sexual salt of prulifloxacin of the present invention. Add 30 ml of water to the solid and stir with a glass rod. Within one minute, the solid is completely dissolved.

[0022] The solution is diluted with water according to the predetermined solubility, sterilized and filtered, put into an ampo...

Embodiment 3

[0024] 0.01mol prulifloxacin, 0.01mol hydrochloric acid and 30ml water were added in a 100ml glass bottle, stirred at room temperature for 10 minutes and the raw materials were dissolved rapidly, the resulting solution was colorless and transparent, and the pH value of the solution measured with a pH meter was 4.6. 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, and turn into a transparent glassy solid after the water is removed, continue to place it to let the water evaporate completely, and gradually turn into a white solid , The obtained product weighs 4.1g. The product is the water-soluble salt of prulifloxacin of the present invention. Add 30 ml of water to the solid and stir with a glass rod. Within one minute, the solid is completely dissolved. The solution is diluted with water according to the predetermined solubility, sterilized and filtered, put into an ampoul...

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PUM

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Abstract

The present invention aims at providing one kind of water soluble Prulifloxacin salt for muscular injection or intravenous injection and its proper injection form. The water solution of these soluble salts is easy to release Prulifloxacin salt, and the injection of Prulifloxacin salt has the same antiseptic effect as orally taken Prulifloxacin preparation. In addition, the injected medicine enters blood directly to produce treating effect and thus has faster effect and less medicine consumption compared with available orally taken form.

Description

technical field [0001] The invention relates to a water-soluble salt of prulifloxacin and an injection form made of the water-soluble salt. Background technique [0002] Prulifloxacin, developed by the Japanese Meiji Pharmaceutical Company, was approved to be listed in Japan in July 2002. This product is the prodrug of NM394, and its antibacterial ability against Gram-negative bacteria and Gram-positive bacteria, especially against Gram-negative bacteria headed by Pseudomonas aeruginosa far exceeds that of other sandacins. It also surpasses other antibiotic drugs currently on the market; and oral absorption is good, repeated administration has no accumulation in the body, and the incidence of side effects is 3.4%, mainly digestive tract symptoms (accounting for 2.1%). The drug is mainly used for the treatment of infectious enteritis, suppurative diseases, biliary tract infection and gynecological infection. At present, it has not been listed for sale in other countries inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/14A61K9/19A61K31/496A61P31/04
Inventor 魏雪纹王小树申洁
Owner 魏雪纹
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