Trisofen Ceftriaxone Sodium Compound Drug Preparation and Its New Indication for Treatment of Pelvic Inflammation

A technology of ceftriaxone sodium and solvent, which is applied in the field of drug preparation, can solve the problems of potential safety hazards, no therapeutic effect, toxicity, etc., and achieves the effects of limited reaction temperature reduction, improved clinical treatment effect, and accelerated reaction progress.

Active Publication Date: 2021-06-08
广东金城金素制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Ceftriaxone sodium is unstable to strong acid, strong alkali, oxidation and temperature. In addition, impurities in raw materials and impurities produced in the production process remain in the finished product, which further weakens the stability of the finished product during storage.
However, no effective solution has been proposed in the production process of the single preparation and the compound preparation of ceftriaxone sodium at present.
[0010] At present, a large number of studies have confirmed that most of the impurities in drugs have potential biological activities, which affect the safety and effectiveness of drugs, and even cause toxicity.
Although no research has been able to fully confirm the harm caused by some of these impurities to the human body, they are, after all, pollutants in medicines and have no therapeutic effect, so they should be reduced to the lowest level as possible
[0011] Further, the current production process of ceftriaxone sodium still has problems such as limited conversion rate of reaction raw materials, difficulty in treating boron trifluoride-containing wastewater, and environmental pollution.
[0012] Based on the consideration of the drug effect and safety of ceftriaxone sodium, as well as the improvement of production process and post-production treatment efficiency, it is necessary to study the production process and formulation form of ceftriaxone sodium preparations to improve production efficiency and reduce boron trifluoride content. The generation of waste water solves the problems of insufficient stability of ceftriaxone sodium during storage and poor stability and potential safety hazards of ceftriaxone sodium preparations caused by impurities

Method used

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  • Trisofen Ceftriaxone Sodium Compound Drug Preparation and Its New Indication for Treatment of Pelvic Inflammation
  • Trisofen Ceftriaxone Sodium Compound Drug Preparation and Its New Indication for Treatment of Pelvic Inflammation
  • Trisofen Ceftriaxone Sodium Compound Drug Preparation and Its New Indication for Treatment of Pelvic Inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] The synthesis of embodiment 1 ceftriaxone sodium

[0127] Preparation of 7-ACT:

[0128] Step 1: In a reaction flask, disperse 544g (2mol) 7-ACA in 2000ml of dichloromethane, add 334g (2.10mol) of TTZ, 284g (2.2mol) of N,N-diisopropylethylamine, stir and cool down To below 5°C, add TiCl dropwise to the reaction system 4 378g (2mol), tetrabutyl titanate 102g (0.30mol), after the addition is complete, keep warm for 4h;

[0129] After the reaction, add 10% sodium bicarbonate solution dropwise to the reaction system to adjust the pH to 7.5, separate the liquids, extract the water phase once with dichloromethane, add glacial acetic acid dropwise to the water phase, adjust the pH to 2.0, and cool to Below 5°C, crystals were precipitated, suction filtered, and dried to obtain 704g of 7-ACT, with a yield of 95%;

[0130] Preparation of ceftriaxone sodium crude product:

[0131] Step 2: Add 371g (1.0mol) of 7-ACT prepared in step 1, 368g (1.05mol) of AE-active ester, and 15...

Embodiment 2

[0135] The synthesis of embodiment 2 ceftriaxone sodium

[0136] The same as the synthesis process of Example 1, the only difference is: in step 1), TiCl is added dropwise to the reaction system 4 340g (1.8mol), tetrabutyl titanate 61g (0.18mol), ie TiCl 4 The molar ratio with 7-ACA is 0.9:1, TiCl in the catalyst 4 The molar ratio to tetrabutyl titanate is 1:0.1.

Embodiment 3

[0137] The synthesis of embodiment 3 ceftriaxone sodium

[0138] The same as the synthesis process of Example 1, the only difference is: in step 1), TiCl is added dropwise to the reaction system 4 416g (2.2mol), tetrabutyl titanate 150g (0.44mol), namely TiCl The mol ratio of and 7-ACA is 1.1:1, TiCl in the catalyst 4 The molar ratio to tetrabutyl titanate is 1:0.2.

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Abstract

The invention relates to the technical field of medicine preparation, and discloses a new indication for treating pelvic inflammatory disease with a medicine preparation of tresofen ceftriaxone sodium. The ceftriaxone sodium provided by the specific production process of the present invention has extremely low impurity content, remarkable drug effect, improves the quality of the preparation product, helps to ensure the safety and effectiveness of the preparation product, and has the application of preparing medicine for treating pelvic inflammatory disease.

Description

technical field [0001] The invention relates to medicine preparation technology, in particular to a ceftriaxone sodium composition, a preparation method and an application thereof. Background technique [0002] Ceftriaxone Sodium (Ceftriaxone Sodium), the chemical name is (6R,7R)-7-[[(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-8-oxo-3- [[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio]methyl]-5-thio Generation-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid disodium salt triple hemihydrate is a third-generation cephalosporin antibiotic. Originally researched and marketed by Roche Company in Switzerland, the product name is Rocephin. The internationally recognized brands include: Traxofen, Junbizhi, Acantex, and Cefaxone. [0003] Ceftriaxone sodium has strong antibacterial activity, is stable to some β-lactamases, has strong penetrating power to the outer membrane of cells and tissues, has high drug concentration in serum and tissues, long elimination ha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36C07D501/12A61P15/00A61K31/546A61K31/43A61K31/431A61K31/439
CPCA61K31/43A61K31/431A61K31/439A61K31/546A61P15/00C07D501/12C07D501/36A61K2300/00
Inventor 伊茂聪吴丰喆傅苗青周白水李秋荣马庆双应鹏朱旭伟
Owner 广东金城金素制药有限公司
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