Use of new stable Ulifloxacin hydrochloride in preparation of anti-infection medicine

A hydrochloride and drug technology, applied in the application field of preparing an anti-bacterial infection drug, can solve the problems of difficult clinical treatment of bacterial drug resistance, etc., and achieve improved bioavailability, high bioavailability, and rapid onset of effect Effect

Active Publication Date: 2011-09-28
深圳麦德凯诺医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these antibacterial drugs cannot meet the growing and refractory diseases in recent years, namely the treatment of chronic Pseudomonas aeruginosa infection and Gram-ne

Method used

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  • Use of new stable Ulifloxacin hydrochloride in preparation of anti-infection medicine
  • Use of new stable Ulifloxacin hydrochloride in preparation of anti-infection medicine
  • Use of new stable Ulifloxacin hydrochloride in preparation of anti-infection medicine

Examples

Experimental program
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Effect test

preparation example 1

[0044] Preparation 1: 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazetidino[3,2-a]quinone Preparation of phen-3-hydrochloride

[0045] 1) Preparation of 3,4-difluoro-dithioformic acid-aniline-triethylamine salt (A):

[0046] Under nitrogen protection, put 129g (1.00mol) of difluoroaniline in a 1L reaction flask, then add 202g (2.00mol) of triethylamine, cool to 5°C, slowly add 84g (1.10mol) of carbon disulfide dropwise, and complete the addition in 5 ~10°C, stirred and reacted overnight, filtered, rinsed the filter cake with diethyl ether, and dried under vacuum at room temperature to obtain 294.2 g of light yellow solid with a yield of 96.0%.

[0047] TLC developer: petroleum ether: ethyl acetate: 4:1, Rf=0.60

[0048] 2) Preparation of 3,4-difluorophenylisothiocyanate (B):

[0049] Under the protection of nitrogen, add 306g (1.00mol) of homemade A and 450mL of dichloromethane to a 1L reaction flask in sequence, stir evenly, cool to 5°C with ice water, add 119g (1...

Embodiment 1

[0066] a. Preparation of Ulifloxacin Hydrochloride

[0067] Add 10 g of the ulifloxacin prepared in Preparation Example 1 and 500 mL of acetonitrile into a 1 L three-necked flask, stir for half an hour under reflux to dissolve, then add 15 mL of 2 mol / L hydrochloric acid three times, and react for half an hour after each addition of hydrochloric acid. After adding hydrochloric acid, add 40mL of distilled water and 1.0g of activated carbon, gradually raise the temperature to reflux, and keep warm for 2h. The reaction was almost complete, filtered while it was hot, and the filtrate was refrigerated overnight, a large number of crystals were precipitated, filtered with suction, and the filter cake was washed twice with ethanol, 25 mL each time. The obtained solid was dried under reduced pressure at 40° C. for 10 h to obtain 9.44 g of off-white or light yellow solid, with a yield of 85.5%.

[0068] b. Preparation of Ulifloxacin Hydrochloride for Injection

[0069] Take 50g of ul...

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PUM

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Abstract

Ulifloxacin has low water solubility and low bioavailability. The invention relates to an Ulifloxacin salt, a preparation thereof, a kit having the medicinal antibiotic preparation and the use of the new Ulifloxacin salt in the preparation of an anti-bacterial-infection medicine. The invention particularly relates to a new medicinal preparation which is used for injection and can be stored stablyand the chemical name of which is 6-fluoro-1-methy-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazeto[3,2-alpha]quinoline-3-carboxylate. In the invention, the medicinal preparation is administrated by direct injection in form of thiabutyldine quinoline carboxylate, the solubility is improved, the bioavailability is improved and treatment effect is enhanced.

Description

Technical field: [0001] The present invention relates to a new ulifloxacin hydrochloride and its preparation, a kit containing the pharmaceutical antibiotic preparation, and an application of the new ulifloxacin salt in preparing an antibacterial infection medicine. In particular, it relates to a new stable chemical name for injection: 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-[1,3 ] Pharmaceutical formulation of thiazetidino[3,2-a]quinoline-3-hydrochloride. Background technique: [0002] Microbial infection is the main factor that threatens human health. In the process of fighting against diseases, humans have discovered a variety of antibacterial drugs: β-lactams, macrolides, aminoglycosides, other antibiotics and synthetic drugs. Synthetic drugs include the largest class of antibacterial drugs: quinolones, among which ciprofloxacin, ofloxacin, levofloxacin, pefloxacin, etc. have been widely used in clinical practice and have become a clinically important class of anti...

Claims

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Application Information

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IPC IPC(8): A61K31/496C07D513/04A61P31/04A61K9/08A61K9/14A61K9/19
Inventor 单爱莲邱凯
Owner 深圳麦德凯诺医药科技有限公司
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