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Compound injection with probenecid, potassium and beta-lactam antibiotic and its use

A technology of lactams and probenecid sodium, which is applied in the field of powder injections and freeze-dried powder injections, and can solve problems such as probenecid sodium that have not yet been seen

Inactive Publication Date: 2006-11-01
吴晓辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports of probenecid sodium (potassium) itself and compound prescriptions composed of antibiotics.

Method used

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  • Compound injection with probenecid, potassium and beta-lactam antibiotic and its use
  • Compound injection with probenecid, potassium and beta-lactam antibiotic and its use
  • Compound injection with probenecid, potassium and beta-lactam antibiotic and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153]Example 1: Dissolve 22 kilograms of sodium hydroxide in 200 liters of purified water, add 142 kilograms of probenecid after all the dissolution, heat to 60° C., adjust the pH to above 7.5, and keep stirring until the pH value is basically constant. Under the condition of 60°C, it is sterilized by filtration through a 0.45 μm filter membrane, and then finely filtered through a 0.22 μm filter membrane to remove pyrogens, and dried under sterile conditions to obtain the raw material of probenecid sodium that meets the standards for human drug injections. White or off-white crystalline powder.

[0154] Probenecid sodium and penicillin G sodium are mixed under aseptic conditions at a weight ratio of 1:3, subpackaged under aseptic conditions, and finally made into a powder injection.

Embodiment 2

[0155] Example 2: Dissolve 28 kg of sodium hydroxide in 280 liters of purified water, add 143 kg of probenecid after all the dissolution, heat to 65°C, adjust the pH to above 8, and keep stirring until the pH value is basically constant. Under the condition of 65°C, it is sterilized by filtration through a 0.45 μm filter membrane, and then finely filtered through a 0.22 μm filter membrane to remove pyrogens, and dried under sterile conditions to obtain the raw material of probenecid sodium that meets the standards for human drug injections. White or off-white crystalline powder.

[0156] Probenecid sodium and ampicillin sodium are mixed under aseptic conditions at a weight ratio of 1:2.8, subpackaged under aseptic conditions, and finally made into a powder injection.

Embodiment 3

[0157] Example 3: Dissolve 40 kg of sodium hydroxide in 300 liters of purified water, add 150 kg of probenecid after all dissolved, heat to 70°C, adjust pH to 10, and keep stirring until the pH value is basically constant. Under the condition of 70°C, it is sterilized by filtration through a 0.45 μm filter membrane, then finely filtered through a 0.22 μm filter membrane to remove pyrogens, and dried under sterile conditions to obtain the raw material of probenecid sodium that meets the standards for human drug injections. White or off-white crystalline powder.

[0158] Probenecid sodium and cefazolin sodium are mixed under aseptic conditions at a weight ratio of 1:2, subpackaged under aseptic conditions, and finally made into a powder injection.

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PUM

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Abstract

A compound powder injection or freeze-dried powder injection is prepared from the sodium (or potassium) salt of probenecid and the beta-lactam kind of antibiotics including penicillin G, ampicillin, ancef, cefuroxime, cefotaxime and cefoxitin. It can elongate the half life of antibiotic, increase the AUC and plasma level and prevent the generation of drug-resistant bacteria.

Description

Technical field: [0001] The invention relates to a compound preparation composed of probenecid sodium, potassium and β-lactam antibiotics and its application, including powder injection and freeze-dried powder injection, belonging to the field of chemical pharmacy. Background technique: [0002] Probenecid can competitively inhibit the secretion of many β-lactam antibiotics in the renal tubules and prolong their blood elimination half-life (t 1 / 2β ), increase the area under the curve (AUC), increase the blood drug concentration level, make their blood drug concentration exceed the minimum inhibitory concentration (MIC) of the corresponding bacteria, and significantly prolong the time, thereby increasing their curative effect. At present, there is no compound prescription made of probenecid and β-lactam antibiotics, but only one oral compound preparation composed of probenecid and ampicillin, that is, ampicillin probenecid capsules. In addition, since probenecid itself is no...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K9/14A61K9/19A61K31/195A61K31/546A61P31/04
Inventor 吴晓辉
Owner 吴晓辉
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