Norfloxacin Cocrystals: Mechanochemical Synthesis and Scale-up Viability Through Solubility Studies.

Autor:	Ferreira PO; School of Sciences, São Paulo State University, 17033-360, Bauru, Brazil., de Almeida AC; School of Sciences, São Paulo State University, 17033-360, Bauru, Brazil., Costa GP; School of Sciences, São Paulo State University, 17033-360, Bauru, Brazil., Torquetti C; School of Sciences, São Paulo State University, 17033-360, Bauru, Brazil., Baptista JA; CQC/IMS, Chemistry Department, University of Coimbra, 3004-535, Coimbra, Portugal., Eusébio MES; CQC/IMS, Chemistry Department, University of Coimbra, 3004-535, Coimbra, Portugal., Caires FJ; School of Sciences, São Paulo State University, 17033-360, Bauru, Brazil. Electronic address: flavio.caires@unesp.br., Castro RAE; CQC/IMS, Chemistry Department, University of Coimbra, 3004-535, Coimbra, Portugal; Faculty of Pharmacy, University of Coimbra, 3000-548, Coimbra, Portugal. Electronic address: rcastro@ff.uc.pt.
Jazyk:	angličtina
Zdroj:	Journal of pharmaceutical sciences [J Pharm Sci] 2023 Aug; Vol. 112 (8), pp. 2230-2239. Date of Electronic Publication: 2023 Mar 13.
DOI:	10.1016/j.xphs.2023.03.003
Abstrakt:	Cocrystals are recognized as one of the most efficient approaches to improve aqueous solubility of Biopharmaceutical Classification System, BCS, classes II and IV drugs. Cocrystal discovery and the establishment of experimental conditions suitable for scale-up purposes are some of the main challenges in cocrystal investigation. In this work, the investigation of mechanochemical synthesis of norfloxacin cocrystals with picolinic and isonicotinic acids is performed, leading to the discovery of two new cocrystals of this important BCS class IV antibiotic, which were characterized through thermal, spectral and diffractometric analysis. Norfloxacin apparent aqueous solubility using the cocrystals is also presented, with higher values being obtained for all the investigated systems when compared to the pure drug. Norfloxacin has 3 polymorphs and several solvents/hydrates, which represents a challenge for obtaining pure cocrystal forms from solvent crystallization. This challenge was successfully overcome in this work, as experimental conditions to obtain the pure cocrystals (the new ones and also norfloxacin-nicotinic acid and norfloxacin-saccharin) were established using Crystal16 equipment. This is a crucial step to envisage future scale-up procedures and therefore a valuable information for the pharmaceutical industry. Competing Interests: Declaration of Competing Interests The authors declare that they have no known competing financial interestss or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2023 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.)
Databáze:	MEDLINE
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