Novel almoxicillin sodium and clavulanate potassium compound powder preparation for injection and technology for preparing same

A technology of amoxicillin sodium clavulanate potassium and amoxicillin sodium, applied in the field of compound antibiotics and preparation process, new injection packaging form, can solve the problems that no one has developed injection preparations, etc.

Active Publication Date: 2010-02-17
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to technical difficulties, no one has devel

Method used

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  • Novel almoxicillin sodium and clavulanate potassium compound powder preparation for injection and technology for preparing same
  • Novel almoxicillin sodium and clavulanate potassium compound powder preparation for injection and technology for preparing same
  • Novel almoxicillin sodium and clavulanate potassium compound powder preparation for injection and technology for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0012] Example 1: Preparation and storage of co-crystal

[0013] First heat the glass-lined reaction pot, drive out the air, fill it with nitrogen with a humidity below 0.2%, and cool. Put 90L of anhydrous methanol / anhydrous ethanol (volume ratio 1:30) mixed solution into a glass-lined pot, then put 35kg of amoxicillin sodium and 5kg of potassium clavulanate into the above solution under continuous nitrogen flow After heating to 25±2℃, mixing and dissolving, cooling to 5℃ to crystallize, remove the solution under aseptic conditions to obtain a sterile amoxicillin sodium / potassium clavulanate 7:1 co-crystal, the crystal particles are complete , Contains low active water. Vacuum drying under sterile and clean nitrogen flow until the moisture content is below 0.5%. And wash the disposable syringes in the GMP injection powder injection dispensing line, and dry the syringes under a stream of clean nitrogen. Fill the dispensing machine and syringes (Part A) with dry nitrogen when dis...

Example Embodiment

[0014] Example 2: Quality study of eutectic stability:

[0015] Properties: The properties of the trial samples are off-white powder.

[0016] Identification: The retention time of the HPLC peak is compared with the retention time of the chromatographic peak of the reference substance. After comparison with the standard substance, it is a qualified product.

[0017] Alkalinity: The pH value of the aqueous solution of this product is 9.0, the quality standard of amoxicillin sodium, its alkalinity range is 8.0~10.0 (aqueous solution, 0.1g / ml), the pH value range of the quality standard of potassium clavulanate is 6.0~ 8.0. The alkalinity range of this trial-produced sample is 8.0~10.0, which is a qualified sample.

[0018] Solution clarity: the clarity of the trial-produced sample solution does not exceed No. 2 turbidity standard solution, which is a qualified sample.

[0019] Related substances: The determination method of related substances is defined as the HPLC reference substance c...

Example Embodiment

[0040] Example 3: Pharmaceutical test of co-crystal

[0041] 1. The protective effect of amoxicillin sodium and clavulanate potassium (7:1) compound preparation on mice infected with Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus in vivo.

[0042] Drugs (1) Amoxicillin sodium for injection (AMPC). (2) Amoxicillin sodium and clavulanate potassium 7:1 ratio (AMPC / CA) for injection. (3) Sigel (Amoxicillin Sodium and Clavulanate Potassium 5:1) and the above drugs are stored in the freezer and diluted with sterile water for injection to the required concentration before use.

[0043] Animal ICR mice, weighing 18-22g, half male and half male.

[0044] There are 3 enzyme-producing bacteria of the experimental strains, Escherichia coli (3128), Pseudomonas aeruginosa (3302) and Staphylococcus aureus (3711), all of which are clinically isolated.

[0045] Protective agent, highly active dry yeast, commercially available.

[0046] Experimental method: In the pre-experiment, the...

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Abstract

The almoxicillin sodium and clavulanate potassium is widely and clinically used due to good curing effect and safety. The formulations of the almoxicillin sodium and clavulanate potassium are mainly oral preparations in different ratios; because of the advantages of quick response and the like, the injection preparation is deeply and clinically welcomed, but only the 5:1 injection preparation is available in the market at present; and because the clavulanate potassium ratio in the preparation is high, the penicillin anaphylaxis and the high-potassium disease are easily caused, and the preparation is relatively high in price. Because the preparation has the defects of higher process requirements, poor preparation stability, easy decoloring and degradation, and necessary storage and transport at a low temperature, the circulation and use of the medicaments are inconvenient. By changing the ratio of the almoxicillin sodium to the clavulanate potassium and improving the preparation process, the safety of the drugs is improved, the cost of the drugs is lowered and the stability of the drug preparations is improved under a condition of ensuring the curing effect; and simultaneously, because of using a special disposable injector, the conventional complex steps of dissolving and mixing are saved.

Description

Technical field: [0001] The invention relates to the field of medicines, in particular to a compound antibiotic, a preparation process and a new injection packaging form. Background technique: [0002] Amoxicillin (or its sodium salt, amoxicillin sodium) is a β-lactam antibiotic with broad antibacterial spectrum, strong bactericidal power in vivo, good absorption (75-90%), and short peak time (1-2 hours) Its characteristics have been widely used clinically since it was launched in the 1960s. However, due to the emergence of more and more pathogenic strains producing β-lactamase, the pathogenic bacteria can easily cause the β-lactam ring in the amoxicillin molecule to be hydrolyzed and lose its activity, resulting in drug resistance. Potassium clavulanate is an oxypenicillane compound isolated from the culture fluid of Streptomyces, containing a β-lactam ring, which has only weak antibacterial activity, but has a strong broad-spectrum β-lactamase inhibitory effect, which can...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/43A61K31/424A61P31/04
Inventor 王霆邓桂兴马宏强孙明杰
Owner XIANGBEI WELMAN PHARMA CO LTD
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