Preparation and property study of levofloxacin multi-component crystals

Abstract Multi-component crystal is an effective way to improve the physicochemical and biochemical properties of drugs. Levofloxacin (LEV) is an antibacterial and anti-infective drug with high solubility and high antibacterial activity, but still exists some adverse effects. In this study, LEV was selected as the model drug, and partial least squares regression (PLS) models were used to predict the co-formers that might form multi-component crystals with levofloxacin. Guided by the prediction results, LEV multi-component crystals were prepared, then the stability and in vitro antibacterial activity of the samples were investigated. The results show that 7 of the 17 selected co-formers are successfully prepared as multi-component crystals with LEV, and 5 co-formers are successfully hit by the prediction results. Among the prediction models, the Hansen solubility parameter/COSMO-RS two-parameter prediction model has the highest accuracy, with an overall accuracy of 82.4% and a positive accuracy of 83.3% for the experimental systems, respectively. The stability of 5 multi-component crystal samples prepared is not significantly altered compared to the stable raw LEV, and the antibacterial activity against E. coli and S. aureus of all 7 prepared multi-component crystal samples is obviously improved. While achieving the same antibacterial activity as the raw LEV, it is expected that the prepared multi-component crystals would be effective in reducing the dose of the drug and reducing adverse effects.

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	CHEN Wu
	GU Zhendong
	ZHENG Zhiyong
	LIANG Xiaoxiao
	LIU Shiyuan
	JIANG Yanbin

Keywords： levofloxacin multi-component crystal co-former screening preparation property

Received 2023-07-03;

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CHEN Wu, GU Zhendong, ZHENG Zhiyong, LIANG Xiaoxiao, LIU Shiyuan, JIANG Yanbin.Preparation and property study of levofloxacin multi-component crystals[J] Chemcial Industry and Engineering, 2024,V41(6): 136-148

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