Medicine composition of piperacillin sodium and tazobactam sodium

Abstract

The invention discloses a medicine composition of piperacillin sodium and tazobactam sodium. Raw material medicine comprises piperacillin sodium micro powder and tazobactam sodium micro powder of d95 within the range of 120 micrometers to 180 micrometers. Experiments prove that the medicine composition is high in antimicrobial activity, good in redissolving performance and high in product safety.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a compound antibiotic, in particular to a piperacillin sodium-tazobactam sodium pharmaceutical composition. Background technique [0002] Piperacillin Sodium-Tazobactam Sodium for Injection was successfully developed by Wyeth Corporation of the United States, and its marketed dosage form is powder injection. Piperacillin is a broad-spectrum β-lactam antibiotic. It introduces a heterocyclic substituted amide group on the amino group of ampicillin. It has a strong and rapid effect because it can quickly penetrate the cell membrane of a variety of Gram-positive bacteria. , has an enhanced effect on Pseudomonas aeruginosa, and is a penicillin derivative with a wider antibacterial spectrum, but it is hygroscopic and unstable in room temperature solution, which will lead to the formation of particulate matter. Piperacillin is easily destroyed by β-lactamase, and tazobactam is an irreversible ...

AI Technical Summary

Problems solved by technology

[0003] In the process of preparing by freeze-drying method, piperacillin sodium and tazobactam sodium are in a solution state during the liquid preparation and drying process, which are prone to degradation and deterioration, resulting in unqualified product quality; and the common preparations on the market have poor stability and cannot Meet the quality requirements within the validity period; the liquid medicine is unstable at room temperature and is easy to form granules, especially after the frozen piperacillin sodium tazobactam sodium solution is re-thawed or the product prepared as freeze-dried powder is reconstituted into a solution The longer the storage time, the more particles will be generated. The particles in the solution for intravenous injection are very harmful to the patient and may cause infusion phlebitis

[0004] Chinese patent CN1802179A discloses that Wyeth of the United States adds ion chelating agent ethylenediaminetetraacetic acid sodium salt (EDTA) and buffering agent sodium citrate to piperacillin sodium and tazobactam sodium, and controls the interaction between the drug and the excipients. Ratio, solves the problem of microparticles formed in the pharmaceutical composition during reconstitution and thawing in the prior art, can be used safely for parenteral administration, the disadvantage is that ion chelating agents, especially ethylenediaminetetraacetic acid (EDTA ) is likely to cause the loss of sodium, potassium, and calcium ions in the bones, resulting in risks such as osteoporosis

[0005] Chinese patents CN101890016A and CN101890015A respectively disclose a microsphere injection and a liposome injection of piperacillin sodium and tazobactam sodium pharmaceutical composition, which can improve the problem of poor stability of common injections to a certain extent

The compound preparation (8:1) or (4:1) composed of piperacillin sodium and tazobactam sodium, in order to increase the solubility, usually put tazobactam sodium or piperacillin sodium and tazobactam sodium together After freeze-drying, crush and repackage, especially when piperacillin sodium and tazobactam sodium are freeze-dried together, the amount of solvent water used is particularly large, which increases energy consumption a lot, increases the process, and the production and processing time is longer than the direct aseptic The powder packaging has increased hundreds of times, but the effect is still unsatisfactory

Because the β-lactam ring is easy to hydrolyze, the β-lactam compound is easy to degrade in the solution state, and the related substances will increase after being placed for a long time, which brings great hidden dangers to the safety of medication

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