title: Molecular dynamics in supercooled liquid and glassy states of antibiotics: azithromycin, clarithromycin and roxithromycin studied by dielectric spectroscopy. Advantages given by the amorphous state.
abstract: Antibiotics are chemical compounds of extremely important medical role. Their history can be traced back more than one hundred years. Despite the passing time and significant progress made in pharmacy and medicine, treatment of many bacterial infections without antibiotics would be completely impossible. This makes them particularly unique substances and explains the unflagging popularity of antibiotics within the medical community. Herein, using dielectric spectroscopy we have studied the molecular mobility in the supercooled liquid and glassy states of three well-known antibiotic agents: azithromycin, clarithromycin and roxithromycin. Dielectric studies revealed a number of relaxation processes of different molecular origin. Besides the primary α-relaxation, observed above the respective glass transition temperatures of antibiotics, two secondary relaxations in the glassy state were identified. Interestingly, the fragility index as well as activation energies of the secondary processes turned out to be practically the same for all three compounds, indicating probably much the same molecular dynamics. Long-term stability of amorphous antibiotics at room temperature was confirmed by X-ray diffraction technique, and calorimetric studies were performed to evaluate the basic thermodynamic parameters. Finally, we have also checked the experimental solubility advantages given by the amorphous form of the examined antibiotics.
authors.affiliation: Institute of Physics, University of Silesia, ul. Uniwersytecka 4, 40-007 Katowice, Poland. kadrjano@us.edu.pl
authors.forename: K
authors.initials: K
authors.lastname: Adrjanowicz
authors.forename: D
authors.initials: D
authors.lastname: Zakowiecki
authors.forename: K
authors.initials: K
authors.lastname: Kaminski
authors.forename: L
authors.initials: L
authors.lastname: Hawelek
authors.forename: K
authors.initials: K
authors.lastname: Grzybowska
authors.forename: M
authors.initials: M
authors.lastname: Tarnacka
authors.forename: M
authors.initials: M
authors.lastname: Paluch
authors.forename: K
authors.initials: K
authors.lastname: Cal
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D017963:Azithromycin / Q000737:chemistry*; D017291:Clarithromycin / Q000737:chemistry*; D058266:Dielectric Spectroscopy / Q000379:methods*; D004355:Drug Stability; D056004:Molecular Dynamics Simulation; D015575:Roxithromycin / Q000737:chemistry*; D013696:Temperature; D014961:X-Ray Diffraction
chemical_list: D000900:Anti-Bacterial Agents; D015575:Roxithromycin; D017963:Azithromycin; D017291:Clarithromycin