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Application of Mefoxin (cefoxitin sodium) pharmaceutical preparation in infection prevention in gastrointestinal surgery

A technology of cefoxitin sodium and cefoxitin is applied in the directions of antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., to achieve the effects of uniform particle size range, simple process flow and low impurity content

Active Publication Date: 2019-11-01
广东金城金素制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, there is still a lot of room for improvement of cefoxitin sodium

Method used

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  • Application of Mefoxin (cefoxitin sodium) pharmaceutical preparation in infection prevention in gastrointestinal surgery
  • Application of Mefoxin (cefoxitin sodium) pharmaceutical preparation in infection prevention in gastrointestinal surgery
  • Application of Mefoxin (cefoxitin sodium) pharmaceutical preparation in infection prevention in gastrointestinal surgery

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preparation example Construction

[0038] The preparation method comprises the following steps:

[0039] Step 1: adding cephalothin sodium (cephalothin) to the reaction solvent, adding methanesulfonic acid and halogenated succinimide, adding sodium methoxide after the reaction is complete, to obtain 7-methoxy cephalothin;

[0040] Step 2: dissolving 7-methoxycefalotin in methanol solution, adding an aqueous solution of inorganic alkali after cooling, adding benzathine acetate after the reaction is complete, stirring and crystallizing to obtain a deacetylated intermediate;

[0041] Step 3: reacting the deacetylated intermediate with chlorosulfonyl isocyanate to obtain cefoxitin acid after treatment;

[0042] Step 4: Add cefoxitin acid into the crystallization solvent, add dropwise sodium salt solution, filter and dry after completion of the reaction to obtain cefoxitin sodium.

[0043] The synthetic route of described preparation method is as follows:

[0044]

[0045] Specifically, in step 1,

[0046] The...

Embodiment 1

[0134] Step 1: Add 6000ml of dichloromethane, 450ml of methanol and 627g of cephalothin into a 10L four-neck round bottom flask, cool down to -65°C, add 105g of methanesulfonic acid, and slowly add a total of 241g of chlorosuccinimide in 8 batches , stirred for 3 hours; HPLC monitoring until the reaction was complete, dropwise added methanol solution containing 132g of sodium methoxide within 3 hours, and continued to stir for 2 hours. Sodium chloride solution 300ml, stirred for 3 hours, then warmed up to 0°C; hydrochloric acid adjusted to pH 2, liquid separation, organic layer washed, dropwise added cyclohexylamine solution to pH 6, added 500ml isopropyl ether, stirred at 0°C for 2h , white crystals were precipitated, filtered and dried to obtain 7-methoxycephalothin.

[0135] Step 2: In a 10L four-neck round bottom flask, add 500g of 7-methoxycefalotin into 2200g of water and 3000g of methanol, cool to -25°C, add dropwise 2.0mol / l sodium hydroxide aqueous solution until the ...

Embodiment 2

[0139] Step 1: Add 6330ml of dichloromethane, 420ml of methanol and 627g of cephalothin into a 10L four-neck round bottom flask, cool down to -70°C, add 115g of methanesulfonic acid, and slowly add a total of 230g of chlorosuccinimide in 10 batches , stirred for 2 hours; HPLC monitoring until the reaction was complete, dropwise added methanol solution containing 138g of sodium methoxide within 2 hours, and continued to stir for 2 hours. Sodium chloride solution 300ml, stirred for 3 hours, then warmed up to 0°C; hydrochloric acid adjusted to pH 3, liquid separation, organic layer washed, dropwise added cyclohexylamine solution to pH 7, added 500ml of isopropyl ether, stirred at 0°C for 2h , white crystals were precipitated, filtered and dried to obtain 7-methoxycephalothin.

[0140] Step 2: In a 10L four-neck round bottom flask, add 500g of 7-methoxycefalotin into 2550g of water and 4250g of methanol, cool to -30°C, add dropwise 3.0mol / l sodium hydroxide aqueous solution until ...

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Abstract

The present invention provides cefoxitin sodium or a composition thereof, a preparation process of the cefoxitin sodium or the composition thereof, a prescribed preparation, a compound preparation, and use. In the cefoxitin sodium or the composition thereof, the mass content of the cefoxitin (C16H17N3O7S2) is 92% or above on an anhydrous basis. The cefoxitin sodium or the composition thereof has good quality stability and a uniform particle size range, can reduce the process difficulty for preparing preparations, can improve clinical curative effects and safety, and can be used for gastrointestinal surgery infection prevention and postoperative infection treatment.

Description

technical field [0001] The invention relates to an antibiotic drug, in particular to cefoxitin sodium, its preparation and its application in preventing infection during operation. Background technique [0002] Cefoxitin sodium is a semi-synthetic derivative of cefoxitin C. The original R&D units are MERCK and Mylan, and the original R&D and production company is Antibioticos Do Brasil Ltda, a subsidiary of ACS DOBFAR. BRAND-NAME (brand name): Mefoxin, Mefoxin. ACS DOBFAR authorized Jincheng Pharmaceutical (Guangdong Jincheng Jinsu Pharmaceutical Co., Ltd.) to realize the localization of the quality of Cefoxitin Sodium for Injection originally developed in China. [0003] In recent years, cephalosporin-resistant bacteria are increasing, which may be related to the highly active β-lactamase induced by bacteria. The methoxy group in the structure of cefoxitin sodium has a steric hindrance effect, which makes it more stable to β-lactamase, making it more active against Gram-p...

Claims

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Application Information

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IPC IPC(8): C07D501/57C07D501/04A61K31/546A61P31/04
CPCA61P31/04C07D501/04C07D501/57
Inventor 伊茂聪吴丰喆赵春涛毕秀莲李秋荣应鹏
Owner 广东金城金素制药有限公司
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