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Pazufloxacin mesylate and preparation method of powder for injection

A technology for pazufloxacin mesylate and pazufloxacin, which is applied in the field of medicine, can solve the problems of difficulty in realization, low yield, and difficulty in fully reacting pazufloxacin, thereby reducing production time and production. cost, the effect of improving product quality

Inactive Publication Date: 2009-03-11
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the addition of methanesulfonic acid and pazufloxacin is relatively small, so it is difficult to fully react pazufloxacin; after the reflux reaction, it is difficult to directly cool and crystallize, and it will not be completely precipitated even for 40 hours. , so this synthetic method yields a low

Method used

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  • Pazufloxacin mesylate and preparation method of powder for injection
  • Pazufloxacin mesylate and preparation method of powder for injection
  • Pazufloxacin mesylate and preparation method of powder for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Preparation of Pazufloxacin Mesylate

[0019] (1) Mix 350g of pazufloxacin and 1050ml of acetone, add 126.8g of methanesulfonic acid, stir, heat and reflux for 4h, fully react, filter to obtain a clear solution, add 1500ml of dichloromethane and mix well, store at 5°C for 8h , filtered with suction, washed with ethanol, and dried under vacuum at 50°C for 4 hours to obtain 387.6 g of the crude product of pazufloxacin mesylate;

[0020] (2) Put 387.6g of pazufloxacin mesylate crude product and 2350ml of 90% ethanol into the reaction flask, stir and heat to reflux, the solution is all clear, add 2.55g of activated carbon with a total volume of 0.1% (g / ml), and keep warm for 30 minutes , hot filtration for decarburization, fine filtration, adding 2000ml of absolute ethanol to the filtrate, and placing it at a low temperature of 2 to 8°C for 12 hours, white crystals precipitated, filtered, the filter cake was washed with absolute ethanol, and vacuum-dried at 50°C f...

Embodiment 2

[0021] Example 2 Preparation of Pazufloxacin Mesylate

[0022] (1) Mix 350g of pazufloxacin and 1750ml of acetone, add 158.5g of methanesulfonic acid, stir, heat and reflux for 2 hours, fully react, filter to obtain a clear solution, add 2000ml of dichloromethane and mix well, in 2-8 Store at ℃ for 12 hours, filter with suction, wash with ethanol, and dry under vacuum at 60℃ for 3 hours to obtain 374.1 g of crude product of pazufloxacin mesylate;

[0023] (2) Put 374.1g of the crude product of pazufloxacin mesylate and 2250ml of 90% (v / v) ethanol into the reaction flask, stir and heat to reflux, the solution is all clear, and add activated carbon in an amount of 0.3 (g / ml) in total volume 7.45g, keep warm for 30 minutes, decarburize by hot filtration, fine filter, add 2000ml of absolute ethanol to the filtrate, place it at a low temperature of 2-8°C for 8 hours, precipitate white crystals, filter, wash the filter cake with absolute ethanol, vacuum at 60°C After drying for 3 h...

Embodiment 3

[0025] Get the refined product of pazufloxacin mesylate prepared in Example 1 and pack it under 100-grade clean conditions in a sterile room. Pazufloxacin mesylate powder for injection.

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PUM

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Abstract

The invention discloses a method for preparing pazufloxacin mesilate and a powder injection thereof. The method is as follows: a reaction system which is formed by pazufloxacin and methane-sulforic acid as well as a solvent of acetone is subjected to heating and reflux, cooling and crystallization, and separation to obtain the pazufloxacin mesilate, and the pazufloxacin mesilate is then subjected to aseptic filling and freeze drying to obtain the powder injection of pazufloxacin mesilate. The preparation method of the invention can produce pazufloxacin mesilate for injection which has stable quality.

Description

technical field [0001] The invention relates to a preparation method of pazufloxacin mesylate, in particular to a preparation method of pazufloxacin mesylate powder for injection, which belongs to the technical field of medicine. Background technique [0002] Pazufloxacin mesilate belongs to the fourth generation of quinolone anti-infective drugs. It was created by Toyama Co., Ltd. and jointly developed by Toyama Chemical Industry Co., Ltd. and Mitsubishi Corporation. Its side effects are significantly lower than similar varieties. In vitro antibacterial effect shows: against G-bacteria, the antibacterial activity is greater than ofloxacin, ciprofloxacin, sparfloxacin (2 to 4 times greater than ofloxacin), against G+ bacteria, the antibacterial activity of this product is the same as that of Similar to ofloxacin. The antibacterial effect in vivo shows that it has a good curative effect on mouse models infected with G+ bacteria and G- bacteria, including quinolone-resistant ...

Claims

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Application Information

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IPC IPC(8): C07D498/06A61K31/5365A61K9/14A61P31/04
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST
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