Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin.
BACKGROUND
Fluorofenidone is a novel antifibrotic drug and its aqueous solubility is low.


OBJECTIVE
This study was to prepare and characterize inclusion complexes of fluorofenidone (AKF-PD) with beta-cyclodextrin (beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD).


METHODS
The AKF-PD/cyclodextrins (CDs) inclusion complexes were prepared by coprecipitation and freeze-drying, respectively. The solubility enhancement of AKF-PD was evaluated by phase solubility method. Inclusion complexation in solid phase was studied by X-ray diffraction (XRD) and differential thermal analysis (DTA). The dissolution profiles of AKF-PD/CDs inclusion complexes were investigated and compared with those of their physical mixtures and AKF-PD alone.


RESULTS
The phase solubility diagrams of AKF-PD with beta-CD and HP-beta-CD were of A(L)-types, and the solubility of AKF-PD could be increased by 51.5% for beta-CD at 0.014 M and 794.0% for HP-beta-CD at 0.254 M. The results from XRD and DTA suggested that AKF-PD could form inclusion complex with beta-CD or HP-beta-CD. The dissolution rate of AKF-PD from the inclusion complexes was much more rapid than AKF-PD alone.


CONCLUSIONS
The formulation of AKF-PD/CDs inclusion complexes showed superior performance in improving dissolution properties of AKF-PD.
Wang
Shengfeng
S
Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University, Changsha, PR China.
Ding
Yanfei
Y
Yao
Yao
Y