Novel organic salts based on fluoroquinolone drugs: synthesis, bioavailability and toxicological profiles.
Int J Pharm
; 469(1): 179-89, 2014 Jul 20.
Article
de En
| MEDLINE
| ID: mdl-24746413
ABSTRACT
In order to overcome the problems associated with low water solubility, and consequently low bioavailability of active pharmaceutical ingredients (APIs), novel organic salts containing fluoroquinolones (e.g. ciprofloxacin and norfloxacin) were prepared, using an optimized synthetic procedure based on direct protonation, with different biocompatible counter ions such as mesylate, gluconate and glycolate. All the prepared organic salts were characterized by spectroscopic techniques, mass spectrometry and thermal analysis. Solubility studies in water and simulated biological fluids at 25°C and 37°C were also performed. Additionally, octanol-water and phospholipid-water partition coefficients were measured at 25°C. The cytotoxicity and anti-inflammatory efficacy using an human cell model of intestinal epithelia (Caco-2 cells) were also evaluated and compared to those of the parent APIs. The adequate selection of the biocompatible anions allows the tuning of important physical, thermal and toxicological properties.
Mots clés
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Ciprofloxacine
/
Norfloxacine
/
Méthanesulfonates
/
Gluconates
/
Glycolates
/
Anti-inflammatoires
/
Antibactériens
Langue:
En
Journal:
Int J Pharm
Année:
2014
Type de document:
Article
Pays d'affiliation:
Portugal