Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin
Shengfeng Wang1, Yanfei Ding, Yao Yao
1Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University, Changsha, PR China.
Drug Development and Industrial Pharmacy
|April 2, 2009
Summary
Fluorofenidone (AKF-PD) inclusion complexes with beta-cyclodextrin (beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD) were prepared to enhance drug solubility. These complexes significantly improved the dissolution rate of fluorofenidone.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Fluorofenidone (AKF-PD) is a novel antifibrotic agent with poor aqueous solubility.
- Low solubility limits the therapeutic efficacy of many drug candidates.
Purpose of the Study:
- To prepare and characterize inclusion complexes of fluorofenidone (AKF-PD) with beta-cyclodextrin (beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD).
- To enhance the solubility and dissolution properties of fluorofenidone.
Main Methods:
- Inclusion complexes were prepared using coprecipitation and freeze-drying techniques.
- Solubility was assessed via the phase solubility method.
- Solid-state characterization employed X-ray diffraction (XRD) and differential thermal analysis (DTA).
- Dissolution profiles were compared against physical mixtures and the pure drug.
Main Results:
- Phase solubility diagrams indicated an A(L)-type interaction between AKF-PD and both cyclodextrins.
- Solubility increased by 51.5% with beta-CD and a remarkable 794.0% with HP-beta-CD.
- XRD and DTA confirmed the formation of inclusion complexes.
- Dissolution rates from complexes were substantially faster than for AKF-PD alone.
Conclusions:
- Formulation of AKF-PD/cyclodextrin inclusion complexes effectively improves the dissolution properties of fluorofenidone.
- This approach offers a promising strategy for enhancing the bioavailability of poorly soluble drugs like fluorofenidone.
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