Abstract

PREPARATION AND CHARACTERIZATION OF FLORFENICOL INCLUSION COMPLEXES WITH THREE CYCLODEXTRINS

Suying Ma, Yongli Shi, Jincai Wang and Xiaojun Shang

Abstract

Florfenicol inclusion complexes with three cyclodextrins were prepared for the improvement of the solubility and dissolution rate of florfenicol. The inclusion complexes were prepared by the saturated aqueous solution method with hydroxypropyl -β-cyclodextrin, γ- cyclodextrin and hydroxypropyl -γ-cyclodextrin as carriers. The products were characterized by phase solubility diagram, differential thermal analysis and dissolution rate. Stability constants for florfenicol in the three carrier solutions were calculated. The solubility of florfenicol, physical mixture and inclusion complex were measured. The results showed that the florfenicol was included by the three carriers and obeyed a typical AL-type. The stability constant was 719.73 L/mol, 352.7 L/mol and 678.91 L/mol for HP-β-CD, γ-CD and HP-γ-CD, respectively. The spectra of differential thermal analysis of the inclusion complexes were different from florfenicol and the physical mixture. Solubility of florfenicol was enhanced for the formation of inclusion complex. The dissolution rate of florfenicol inclusion complex made with HP-β-CD was higher than that of inclusion complexes made with HP-γ-CD andγ-CD. The florfenicol inclusion complexes made with three cyclodextrins showed superior performance in improving dissolution rate properties, The method was simple and practical on preparation the inclusion complexes.

Keywords: Florfenicol, Hydroxypropyl-?-Cyclodextrin, ?-Cyclodextrin, Hydroxypropyl - ?-Cyclodextrin, Inclusion Complexes, Dissolution rate, Solubility.