New indication of trisofen ceftriaxone sodium drug preparation in the treatment of infection in immunocompromised patients

A technology of ceftriaxone sodium and compound, applied in the field of drug preparation, can solve the problems of strong acid, strong base, oxidation and temperature instability, poor stability of ceftriaxone sodium preparation, weakened stability of finished preparation, etc., so as to reduce clinical complications. Sensitive risk, beneficial to long-term storage and placement, and the effect of improving safety in use

Active Publication Date: 2020-09-25
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

[0005] We have studied the stability of ceftriaxone sodium and found that ceftriaxone sodium is unstable to strong acid, strong alkali, oxidation and temperature. In addition, the residues of raw material impurities and impurities produced in the production process in the finished product make the finished preparation Further weakening of stability during storage
At present, the production process or storage method of the single preparation and the compound preparation of ceftriaxone sodium have not been able to propose an effective solution
[0006] Based on the consideration of ceftriaxone sodium impurities on drug efficacy and safety, it is necessary to study the production process and formulation form of ceftriaxone sodium preparations to solve the problems of poor stability and decreased antibacterial effect of ceftriaxone sodium preparations caused by impurities

Method used

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  • New indication of trisofen ceftriaxone sodium drug preparation in the treatment of infection in immunocompromised patients
  • New indication of trisofen ceftriaxone sodium drug preparation in the treatment of infection in immunocompromised patients
  • New indication of trisofen ceftriaxone sodium drug preparation in the treatment of infection in immunocompromised patients

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-2

[0123] The synthesis of embodiment 1-2 ceftriaxone sodium

[0124] The same as the synthesis process of Example 1-1, the only difference is: in step 1), 14.5gAlCl is added dropwise to the reaction system 3 -BF3-dimethyl carbonate solution [(wBF 3 )=18%] (wherein, AlCl 3 0.64g (0.0048mol), BF 3 2.6g (0.038mol)), that is, aluminum trichloride AlCl 3 -BF 3 AlCl in dimethyl carbonate composite catalyst 3 and BF 3 The weight ratio is 1:8.

[0125] The synthesis of embodiment 1-3 ceftriaxone sodium

[0126] The synthesis process is the same as that of Example 1-1, except that in step 2), the reaction solvent is changed from dichloromethane to acetonitrile, and the crystallization solvent is acetone.

Embodiment 1-4

[0127] The synthesis of embodiment 1-4 ceftriaxone sodium

[0128] The synthesis process is the same as that of Example 1-1, except that in step 3), the reaction solvent is changed from 20% methanol-water for injection to water for injection, and the crystallization solvent is acetone.

Embodiment 2-1

[0129] The synthesis of embodiment 2-1 sulbactam sodium

[0130]Step A), 330mL (3.6mol) of 25% hydrobromic acid was cooled to 0°C, and the pH was adjusted to about 2.5 by adding dilute sulfuric acid dropwise; 120mL water and 108g 6-APA (0.5mol) were weighed to prepare a suspension, Cool to 5°C, add dropwise to the hydrobromic acid solution; weigh 34.5g (0.5mol) of sodium nitrite and dissolve it in 55mL of water, add dropwise to the above system, keep stirring during the dropwise addition, and continue to stir after the dropwise addition is completed The reaction was carried out for 1.5 hours, and the temperature was controlled at 0-5° C. during the reaction. After the reaction is completed, 14 (weight)% hydrogen peroxide (1.5 mol) is added dropwise to the above system, and the reaction is stirred for 1 hour after the dropwise addition, and the temperature is controlled at 0-5° C. during the reaction. After the reaction was completed, 15% sodium bisulfite was slowly added unti...

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Abstract

The invention belongs to the technical field of drug preparation, and discloses new indications of a troxofine ceftriaxone sodium pharmaceutical preparation for treatment of infection of patients withimmunodeficiency. By improving a raw material synthesis process, ceftriaxone sodium with the high effective constituent content and the low impurity content is provided so as to solve the problems ofpoor stability and reducing of the antibacterial effect of a ceftriaxone sodium preparation due to impurities. The ceftriaxone sodium provided by the specific production process is very low in impurity content and significant in efficacy, the quality of a preparation product is improved advantageously, safety and effectiveness of the preparation product are ensured, and the preparation product has uses in the aspects of preparing drugs for treating infection of the patients with immunodeficiency.

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 is a third-generation cephalosporin antibiotic. 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-1-azabicyclo[4.2 .0] Oct-2-ene-2-carboxylic acid disodium salt triple hemihydrate. Its chemical structural formula is as follows: [0003] [0004] The possibility of adverse drug reactions may occur during drug use. Common factors include dosage, dosing regimen, course of treatment, demographic characteristics, combination medication, efficacy characteristics, etc., but are important and controllable factors related to adverse drug reactions as drug impurities. Although the pharmacopoeia stipulates the limits of drug content,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/546A61P31/04C07D501/36C07D501/06C07D501/12
CPCA61K31/546A61P31/04C07D501/06C07D501/12C07D501/36
Inventor 伊茂聪吴丰喆马庆双俞玉萍朱旭伟
Owner 广东金城金素制药有限公司
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