Preparation, Characterization and Pharmacokinetics of HPMC modified Florfenicol Microcrystals

作者：Cao, Hang; Fu, Hualin^*; Lu, Chaocheng; Zhou, Jianyu; Zhang, Yanli; Jin, Chao; Liu, Mengjiao

来源：Latin American Journal of Pharmacy, 2014, 33(9): 1540-1546.

• Florfenicol
• HPMC
• Microcrystal
• Pharmacokinetic
• Recrystallization

In order to enhance the solubility and bioavailability of florfenicol, a novel microcrystalization method was applied to prepare florfenicol microcrystals. In this study, the optimized hydroxy propyl methyl cellulose (HPMC) modified florfenicol microcrystals with small particle size and high solubility were successfully prepared by an improved solvent-antisolvent recrystallization method, and the morphology of microcrystals was investigated. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirmed the original drug has two crystal forms, but one form for microcrystals. For florfenicol microcrystals, an accelerated dissolution velocity and increased saturation solubility were achieved in vitro and a markedly different pharmacokinetic property in vivo was exhibited with magnified area under the curve (AUC) compared with the original drug. These results implied that developing florfenicol as HPMC modified microcrystals is a promising choice for oral delivery and further clinical application.

• 出版日期2014
• 单位四川农业大学