Thermodynamic and structural study of norfloxacin cocrystals

• Grant number: 22/00239-2
• Support Opportunities: Scholarships abroad - Research Internship - Scientific Initiation
• Start date: July 08, 2022
• End date: November 07, 2022
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Analytical Chemistry
• Principal Investigator: Flávio Junior Caires
• Grantee: Giovanna de Paula Costa
• Supervisor: Maria Ermelinda da Silva Eusebio
• Host Institution: Faculdade de Ciências (FC). Universidade Estadual Paulista (UNESP). Campus de Bauru. Bauru , SP, Brazil
• Institution abroad: Universidade de Coimbra (UC), Portugal
• Associated to the scholarship: 20/07724-8 - Mechanochemical synthesis, characterization, thermoanalytical study and evaluation of the solubility of norfloxacino cocrystals, BP.IC

Abstract

Currently, several drugs that have low aqueous solubility are found in circulation, this deficiency reduces the absorption of the drug in the body and causes them to be administered in higher daily doses and for a longer period of time, which can cause adverse effects to patients. In view of this, the formation of pharmaceutical cocrystals is an approach that aims to improve the physicochemical properties of drugs under development and commercialization without interfering with their therapeutic activity. The cocrystal formation process occurs through the intermolecular interaction between an active pharmaceutical ingredient (API) and one or more coformers, which remain linked together through supramolecular synthons, which modify the physicochemical properties, without compromising their ability therapy. The present work aims to build ternary phase diagrams of Norfloxacin cocrystals with the co-formers pyrazinoic acid and p-aminobenzoic acid, already obtained by the mechanochemical method, using the Crystal16 equipment and to determine the crystalline structure of the cocrystals obtained using the X-ray technique of single crystal. The study will consist in the construction of ternary phase diagrams obtained through equilibrium solubility data of the compounds and the determination of the crystalline structure of the compounds using the single crystal X-ray technique. With the ternary diagrams, it is expected to find the best crystallization conditions for the production of cocrystals on a large scale and for obtaining suitable single crystals for structural elucidation and, therefore, a better understanding of the interactions that occur between the API and the coformer. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

FERREIRA, PATRICIA O.; DE ALMEIDA, AMANDA C.; COSTA, GIOVANNA DE P.; TORQUETTI, CAROLINA; BAPTISTA, JOAO A.; EUSEBIO, M. ERMELINDA S.; CAIRES, FLAVIO J.; CASTRO, RICARDO A. E.. Norfloxacin Cocrystals: Mechanochemical Synthesis and Scale-up Viability Through Solubility Studies. Journal of Pharmaceutical Sciences, v. 112, n. 8, p. 10-pg., 2023-08-01. (22/00239-2, 18/24378-6, 20/07724-8)