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Method for preparing compound beta lactam sodium salt/sodium benemid for injection

A technology of probenecid sodium and lactams, which is applied in the field of preparation of compound β-lactam sodium salt/probenecid sodium for injection, and can solve the problem of low bioavailability, short half-life, and effects on β-lactams. Clinical application of antibiotics and other issues

Inactive Publication Date: 2005-11-23
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its oral administration has low bioavailability, short half-life, and requires multiple doses per day, which affects the clinical application of β-lactam antibiotics

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1: at first 1 part of probenecid is dissolved in 75 parts of water by mass parts to make probenecid suspension, then add the NaOH solution of 1mol / L in probenecid suspension to adjust pH to 8 react to form a salt, then filter through a 0.22 μm microporous membrane, sterilize at 150°C for 30 minutes, and dry aseptically to obtain probenecid sodium; It can be dissolved in 1 portion of infusion solution after mass ratio, intravenous administration can be divided into slow intravenous injection or intravenous infusion; intravenous infusion, 1 ~ 2g (according to ampicillin sodium), instillation 1 / 2 ~ 1h, 2 to 4 times / day. For children, 100-150 mg / kg (according to ampicillin sodium) per day, given in divided doses.

Embodiment 2

[0012] Embodiment 2: at first 8 parts of probenecid are dissolved in 80 parts of water by mass parts to make probenecid suspension, then add the sodium acetate solution of 0.8mol / L in probenecid suspension to adjust When the pH reaches 9, react to form a salt, filter through a microporous membrane of 0.45 μm, sterilize at 200°C for 30 minutes, and dry aseptically to obtain probenecid sodium; mix cefotaxime sodium and the obtained probenecid sodium by 1: The mass ratio of 10 can be dissolved in 100 parts of infusion. Intravenous administration can be divided into slow intravenous injection or intravenous infusion; intravenous infusion, 1 ~ 2g (calculated as cefotaxime sodium) once, instilled for 1 / 2 ~ 1h, 2 ~ 4 times / day. For children, 100-150 mg / kg per day (based on cefotaxime sodium), given in divided doses.

Embodiment 3

[0013] Embodiment 3: at first 5 parts of probenecid are dissolved in 50 parts of water by mass parts to make probenecid suspension, then add the sodium bicarbonate solution of 2.5mol / L in probenecid suspension Adjust the pH to 10 to react into a salt, filter through a 0.22 μm microporous membrane, sterilize at 105°C for 30 minutes, and dry aseptically to obtain probenecid sodium; mix cefoperazone sodium and the obtained probenecid sodium according to the ratio of 10:1 After mass proportioning, it can be dissolved in 80 parts of water. Adults: 1-2g (calculated as cefoperazone sodium), once every 12 hours; for severe infections, it can be increased to 4g once every 12 hours. Children: 50-200mg / kg per day (based on cefoperazone sodium), divided into 2 doses.

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PUM

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Abstract

Disclosed is a method for preparing compound beta lactam sodium salt / sodium benemid for injection, which comprises dissolving 1-10 weight parts of probecid into 1-100 parts of water, charging sodium ion-containing alkaline solution, adjusting pH to 6-11 for reaction into salts, filtering and degerming through microporous filtering film, asepsis drying, or filtering with microporous filtering film and charging 10-100 parts of absolute ethyl alcohol or waterless acetone for evolution of solid body, carrying out asepsis dehydration obtain the end product, mixing sodium salt of beta-lactams with the obtained sodium benemid by the proportion of 10:1-1:10 and dissolving into 1-100 parts of water.

Description

technical field [0001] The invention relates to a preparation method of compound β-lactam sodium salt / probenecid sodium for injection. Background technique [0002] β-lactam antibiotics are widely used clinically. However, its oral administration has low bioavailability, short half-life, and requires multiple doses per day, which affects the clinical application of β-lactam antibiotics. [0003] Probenecid is an organic acid drug, clinically used for the treatment of chronic gout. [0004] In the early 1950s, Boger et al. found that when the anti-chronic gout drug probenecid was combined with penicillin, the blood concentration of the latter could be increased. Kampann et al. found that probenecid also has the effect of increasing the blood concentration of ampicillin and prolonging the half-life of ampicillin. Gibaldi et al pointed out that the use of probenecid in combination with β-lactam antibiotics caused significant changes in the kinetic parameters of the latter: t...

Claims

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Application Information

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IPC IPC(8): A61K45/06
Inventor 曹永孝王佩贤绳金房孟新芳姚鸿萍杨孝江陶小军刘静杨欣
Owner XI AN JIAOTONG UNIV
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