Pharmaceutical tazobactam sodium single crystal structure determination, polymorphism and crystallization process

Tazobactam as the third generation antibacterial synergist presented the low toxicity and a wider antimi-crobial spectrum, and dominated in clinical application. Tazobactam sodium powder as pharmaceutical form was usually prepared by lyophilization in the pharmaceutical industry, which was extremely hygro-scopic and required strict storage conditions. In this work, we prepared four new polymorphs of tazobac-tam sodium by antisolvent methods, and optimized the crystallization process. Among them, the single crystal of tazobactam sodium in water/ethanol solvent was obtained and the structure was analyzed. Further, reactive crystallization process was explored and optimized, including amine reagent, salt-forming agent and solvent system. The current work provided more options for the pharmaceutical poly-morphs of tazobactam sodium, supporting the industrial production and transportation of the drug.(c) 2023 Elsevier Ltd. All rights reserved.

Automated summary

In this study, four new polymorphs of tazobactam sodium were prepared by antisolvent methods, and the crystallization process was optimized. A single crystal of tazobactam sodium in water/ethanol solvent was obtained and its structure was analyzed. The reactive crystallization process, including amine reagent, salt-forming agent, and solvent system, was explored and optimized. This research provides more options for pharmaceutical polymorphs of tazobactam sodium, supporting the industrial production and transportation of the drug.