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Novel amoxicillin and sulbactum composition

A technology of amoxicillin-sulbactam and amoxicillin, which is applied in the field of novel amoxicillin-sulbactam compositions, can solve the problems of very demanding preparation process conditions, increase the economic burden of patients, and protect active ingredients, and achieves the The effect of reducing production and treatment costs, reducing the frequency of medication, and reducing toxic and side effects

Active Publication Date: 2014-12-17
石药集团中诺药业(石家庄)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent improves the purity of the preparation to a certain extent, but it is only prepared by simple aseptic packaging of the two components, without corresponding protection for the active components, resulting in poor product stability and affecting clinical efficacy
[0006] Chinese patent CN101890008A provides a microsphere injection of amoxicillin sodium sulbactam sodium pharmaceutical composition, which makes microspheres of amoxicillin sodium and sulbactam sodium through certain combination of raw and auxiliary materials, and then aseptically packaged Obtained; Chinese patent CN101822669A provides a liposome injection of amoxicillin sodium sulbactam sodium pharmaceutical composition, adopts the liposome injection prepared from auxiliary materials such as dipalmitoylphosphatidylcholine and sodium deoxycholate, These two preparations have increased the stability of the active ingredient to a certain extent, and have certain advantages compared with traditional injections, but there are still low encapsulation efficiency, easy adhesion and aggregation, easy rupture, burst release effect, and may cause immunity. Response and other issues
In addition, the scale-up production of these new dosage forms in China is not mature enough, and the preparation process conditions are very strict, the production is difficult, the process reproducibility is poor, and the production cost is high, which virtually increases the financial burden of patients, so it does not not ideal

Method used

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  • Novel amoxicillin and sulbactum composition
  • Novel amoxicillin and sulbactum composition
  • Novel amoxicillin and sulbactum composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1 Amoxicillin-monomethoxy polyethylene glycol sulbactam compound medicine

[0037] One, the preparation of amoxicillin-monomethoxypolyethylene glycol

[0038] Amoxicillin—the reaction scheme of monomethoxypolyethylene glycol:

[0039]

[0040] (1) Preparation of aminated monomethoxy polyethylene glycol (mPEG-NH 2 )

[0041] Add 1.5L of 1M dichloromethane solution of azide acid into 10L of 896g (0.5mol) monomethoxy polyethylene glycol (mPEG) tetrahydrofuran solution, and then add 0.3L (1.5mol) diisopropyl azodicarboxylate 2 L of tetrahydrofuran solution of ester (DIAD), and 5 L of tetrahydrofuran solution of 787 g (3.0 mol) triphenylphosphine was added to the obtained mixture, stirred at room temperature for 30 minutes, and heated at 65° C. for 2 hours. Finally, 1 L of 1M hydrochloric acid was added, heated at 65°C for another 2 hours, cooled to room temperature, filtered, and dried in vacuo. The yield is 99%.

[0042] (2) Preparation of amoxicillin-mo...

Embodiment 2

[0051] Embodiment 2 amoxicillin sodium sulbactam-glucuronate compound medicine

[0052] The compound drug involved in this embodiment is composed of unmodified amoxicillin and modified sulbactam, wherein amoxicillin sodium is used as the active ingredient. The method is as follows:

[0053] 1. Preparation of sulbactam-glucuronate

[0054] We chose to modify the carboxyl group of sulbactam to undergo esterification reaction with the hydroxyl group in glucuronic acid. Since the steric hindrance of the isomerized carboxyl group of sulbactam is relatively large, the esterification reaction only occurs on the hydroxyl group of the para-position carbon of the carboxyl group in glucuronic acid, and the product is single, and the modified product can be released quickly after entering the body. active ingredient. In addition, in order to improve the esterification activity of sulbactam, its carboxyl group is first converted into acid chloride, and then esterified with the hydroxyl ...

Embodiment 3

[0066] Embodiment 3 Amoxicillin—monomethoxypolyethylene glycol and sulbactam—preparation of glucuronate

[0067] Among the pharmaceutical ingredients involved in this example, the active ingredients are amoxicillin and sulbactam in modified forms.

[0068] One, the preparation of amoxicillin-monomethoxypolyethylene glycol

[0069] (1) Preparation of aminated monomethoxy polyethylene glycol (mPEG-NH 2 )

[0070] Add 1.5L of 1M dichloromethane solution of azide acid into 10L of 896g (0.5mol) monomethoxy polyethylene glycol (mPEG) tetrahydrofuran solution, and then add 0.3L (1.5mol) diisopropyl azodicarboxylate 2 L of tetrahydrofuran solution of ester (DIAD), and 5 L of tetrahydrofuran solution of 787 g (3.0 mol) triphenylphosphine was added to the obtained mixture, stirred at room temperature for 30 minutes, and heated at 65° C. for 2 hours. Finally, 1 L of 1M hydrochloric acid was added, heated at 65°C for another 2 hours, cooled to room temperature, filtered, and dried in v...

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Abstract

The invention discloses a modified novel amoxicillin and sulbactum composition. According to the composition, the water solubility of the medicament can be improved by performing pegylation on amoxicillin, and excellent stability of the composition can be guaranteed, so that the physicochemical property can be improved after the two active components are respectively subjected to molecular modification, the stability can be greatly improved, the effective content after the composition enters a body can be guaranteed, the problem that the content of a commercial conventional preparation product is greatly reduced after the preparation product is prepared to form infusion can be solved, and the problem of quality stability of the compound preparation in production, storage, preparation and infusion processes can be fundamentally solved; and dosage of sulbactum is greatly reduced, the sulbactum is modified with glucuronic acid, the instability of the original molecular structure can be improved, and the problems of low content, high related substance and the like after sulbactum is deteriorated and degraded can be solved.

Description

technical field [0001] The invention relates to an antibiotic drug, in particular to a novel amoxicillin-sulbactam composition. Background technique [0002] Sulbactam is a synthetic irreversible competitive β-lactamase inhibitor. Its antibacterial activity is weak and slightly stronger than clavulanic acid. When used alone, it only has bactericidal effect on Neisseria gonorrhoeae and Acinetobacter. Most of the β-lactamases produced by gram-positive and gram-negative bacteria have a strong inhibitory effect, but they are ineffective against metallo-β-lactamases. When sulbactam is used in combination with penicillins or cephalosporins, there is generally a significant synergistic effect, which greatly improves the antibacterial activity of the former two and expands the antibacterial spectrum. For example, when sulbactam is used in combination with amoxicillin as a bactericidal broad-spectrum antibiotic, sulbactam can effectively inhibit the β-lactamase produced by drug-resi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/43A61K47/48A61K31/7012A61P31/04A61P39/02A61K47/60
Inventor 马慧丽董朝蓬王忠王荣端王燕燕
Owner 石药集团中诺药业(石家庄)有限公司
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