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Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin.
Drug Dev Ind Pharm. 2009 Jul; 35(7):808-13.DD

Abstract

BACKGROUND

Fluorofenidone is a novel antifibrotic drug and its aqueous solubility is low.

AIM

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).

METHOD

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.

Authors+Show Affiliations

Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University, Changsha, PR China.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

19337873

Citation

Wang, Shengfeng, et al. "Inclusion Complexes of Fluorofenidone With Beta-cyclodextrin and Hydroxypropyl-beta-cyclodextrin." Drug Development and Industrial Pharmacy, vol. 35, no. 7, 2009, pp. 808-13.
Wang S, Ding Y, Yao Y. Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. Drug Dev Ind Pharm. 2009;35(7):808-13.
Wang, S., Ding, Y., & Yao, Y. (2009). Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. Drug Development and Industrial Pharmacy, 35(7), 808-13. https://doi.org/10.1080/03639040802612944
Wang S, Ding Y, Yao Y. Inclusion Complexes of Fluorofenidone With Beta-cyclodextrin and Hydroxypropyl-beta-cyclodextrin. Drug Dev Ind Pharm. 2009;35(7):808-13. PubMed PMID: 19337873.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inclusion complexes of fluorofenidone with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. AU - Wang,Shengfeng, AU - Ding,Yanfei, AU - Yao,Yao, PY - 2009/4/2/entrez PY - 2009/4/2/pubmed PY - 2011/2/18/medline SP - 808 EP - 13 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 35 IS - 7 N2 - BACKGROUND: Fluorofenidone is a novel antifibrotic drug and its aqueous solubility is low. AIM: 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). METHOD: 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. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/19337873/Inclusion_complexes_of_fluorofenidone_with_beta_cyclodextrin_and_hydroxypropyl_beta_cyclodextrin_ L2 - http://www.tandfonline.com/doi/full/10.1080/03639040802612944 DB - PRIME DP - Unbound Medicine ER -