Preparation method of piperacillin sodium and tazobactam sodium sterile powder injection

A technology of tazobactam sodium and piperacillin sodium, which is applied in the direction of medical preparations containing active ingredients, antibacterial drugs, powder delivery, etc., and can solve the problem of poor stability and stable The stability needs to be improved and other issues, to achieve the effect of increasing the stability of the finished product, reducing the production cost and ensuring the singleness

Active Publication Date: 2021-08-06
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Piperacillin sodium-tazobactam sodium compound preparations currently have a good market in China, mainly aseptic powder injections, but due to the poor stability of piperacillin sodium and tazobactam sodium, currently commercially available The stability of piperacillin sodium tazobactam sodium sterile powder injection needs to be improved

Method used

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  • Preparation method of piperacillin sodium and tazobactam sodium sterile powder injection
  • Preparation method of piperacillin sodium and tazobactam sodium sterile powder injection
  • Preparation method of piperacillin sodium and tazobactam sodium sterile powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1 A kind of synthetic method of tazobactam sodium

[0076] This embodiment is a synthetic method of tazobactam sodium, and the specific synthetic process includes the following steps carried out in sequence:

[0077] 1) Synthesis of diphenylmethyl penicillanic acid sulfoxide

[0078] After mixing 600mL of acetone and 100mL of water, add 108g (0.5mol) of 6-aminopenicillanic acid (6-APA), stir and cool down to -15°C, add 184g of saturated hydrochloric acid aqueous solution, and slowly add it dropwise while maintaining -15°C Hypophosphorous acid aqueous solution with a concentration of 50wt% [prepared by adding 62.7g (0.95mol) hypophosphorous acid to 62.7mL of ice water] was added dropwise for 1.5 hours. Sodium nitrite aqueous solution [prepared by adding 65.55g (0.95mol) sodium nitrite to 152mL ice water], add dropwise for 2 hours, after dropping, keep at -15°C for deamination reaction until the residual amount of 6-APA is less than 1% ( TLC detection), add 2...

Embodiment 2～5

[0109] The synthetic method of embodiment 2~5 tazobactam sodium

[0110] Examples 2 to 5 are respectively a synthetic method of tazobactam sodium, and their steps are basically the same as in Example 1, the difference is only in the amount of raw materials and process parameters, see Table 1 for details:

[0111] List of each technological parameter in the embodiment 2~5 of table 1

[0112]

[0113]

[0114]

Embodiment 6

[0115] Example 6 Preparation method of piperacillin sodium-tazobactam sodium sterile powder injection In this example, the tazobactam sodium M1 synthesized in Example 1 was used to prepare a piperacillin sodium-tazobactam sodium-free Bacteria powder injection, the specific preparation process includes the following steps carried out in sequence:

[0116] Take water for injection, boil it and let it cool for later use;

[0117] Under the protection of nitrogen, take 2000mL of boiled water for injection, add 100g of piperacillin sodium and 12.5g of tazobactam sodium, stir to dissolve, add 1g of activated carbon for needles, stir for 30min to decolorize, filter to remove carbon, and then use 0.22μm micro The pore filter membrane is sterilized and filtered to obtain the medicinal solution for subsequent use;

[0118] Take the liquid medicine and pack it according to the required specifications (in this embodiment, the powder injection specification is 2.25g / bottle), half-stoppere...

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Abstract

The invention provides a preparation method of a piperacillin sodium and tazobactam sodium sterile powder injection, belongs to the technical field of medicine preparation. The preparation method comprises the following steps of under the protection of an inert gas, taking water for injection, adding piperacillin sodium and tazobactam sodium for dissolution, performing decoloration, sterilization and filtration, and enabling the obtained feed liquid to be subjected to pre-freezing, four times of sublimation drying and desorption drying to obtain the piperacillin sodium and tazobactam sodium sterile powder injection. According to the invention, through slow heating and segmented drying, the decomposition of piperacillin sodium and tazobactam sodium is effectively inhibited, and the stability of the finished product is improved. The preparation method provided by the invention can effectively improve the drug stability, appearance shape and looseness of the finished product.

Description

technical field [0001] The invention relates to the preparation of sterile powder injection, in particular to a preparation method of piperacillin sodium tazobactam sodium sterile powder injection. Background technique [0002] Piperacillin sodium is a semi-synthetic penicillin antibiotic with broad-spectrum antibacterial effect. It plays a bactericidal effect by inhibiting the synthesis of bacterial cell walls. It is effective against Escherichia coli, Proteus, Serratia, Klebsiella, Enterobacteriaceae, including Enterobacter, Citrobacter, Salmonella, and Shigella, and other Gram-negative bacteria, including Pseudomonas aeruginosa, Acinetobacter, Haemophilus influenzae, and Neisseria All have good antibacterial effect. [0003] Tazobactam sodium is a derivative of sulbactam sodium. It is a type II-V type β-lactamase inhibitor with strong enzyme inhibitory activity and can effectively inhibit various plasmid-mediated β-lactamases, including new Extended-spectrum enzymes and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/496A61K31/431A61P31/04C07D499/87C07D417/12C07D499/86C07D499/08C07D499/04C07D499/06C07D499/18C07D499/16
CPCA61K9/19A61K31/496A61K31/431A61P31/04C07D499/87C07D417/12C07D499/86C07D499/08C07D499/04C07D499/06C07D499/18C07D499/16A61K2300/00Y02A50/30
Inventor 符永红林方育肖汉文林小雪唐雄肇
Owner HAINAN GENERAL & KANGLI PHARMA
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