Mendes Cassiana, Wiemes Bárbara Paula, Buttchevitz Aline, Christ Ana Paula, Ribas Karla Giacomelli, Adams Andréa Inês Horn, Silva Marcos Antônio Segatto, Oliveira Paulo Renato
Department of Pharmaceutical Sciences, Health Science Centre, Federal University of Santa Catarina, Quality Control Laboratory, J/K 207, 88040-900, Florianópolis-SC, Brazil.
Expert Rev Anti Infect Ther. 2015 Jan;13(1):119-29. doi: 10.1586/14787210.2015.982091.
Drugs classified as class IV by the Biopharmaceutical Classification System present significant problems in relation to effective oral administration. In the case of antibiotics, the subsequently high doses required can enhance the emergence of microorganism resistance and lead to a low rate of patient treatment adherence.
In an attempt to improve physicochemical properties and microbiological activity of norfloxacin, the aim of this study was to investigate different methods (coevaporation, kneading followed by freeze-drying or spray-drying) to obtain complexes of norfloxacin and different cyclodextrins.
Guest-host interactions were investigated through a complete physical-chemical characterization and the dissolution profile and microbiological activity were determined.
The formation of a complex of norfloxacin and β-cyclodextrin (1:1), obtained by kneading followed by freeze drying, led to increased drug solubility, which could maximize the oral drug absorption.
Moreover, the microbiological activity was enhanced by around 23.3%, demonstrating that the complex formed could represent an efficient drug delivery system.
生物药剂学分类系统中归类为IV类的药物在有效口服给药方面存在重大问题。就抗生素而言，随后所需的高剂量会增加微生物耐药性的出现，并导致患者治疗依从率较低。
为了改善诺氟沙星的物理化学性质和微生物活性，本研究的目的是研究不同方法（共蒸发、捏合后冷冻干燥或喷雾干燥）以获得诺氟沙星与不同环糊精的复合物。
通过全面的物理化学表征研究客体-主体相互作用，并测定溶出曲线和微生物活性。
通过捏合后冷冻干燥获得的诺氟沙星与β-环糊精（1:1）复合物的形成导致药物溶解度增加，这可以使口服药物吸收最大化。
此外，微生物活性提高了约23.3%，表明形成的复合物可以代表一种有效的药物递送系统。
