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Methods and Findings
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Methods Find Exp Clin Pharmacol 2010, 32(3): 157
ISSN 0379-0355
Copyright 2010 Clarivate Analytics
CCC: 0379-0355
DOI: 10.1358/mf.2010.32.3.1423886
 
 
Study of the physicochemical properties and oral bioavailability of the solid dispersion of cantharidin with polyethylene glycol PEG 4000
Dang, Y.J., Hu, C.H., An, L.N., Zhu, C.Y.
 
 
Cantharidin (CA) is partially water-soluble. Solid dispersion of CA (CA-SD) in polyethylene glycol 4000 (PEG 4000) was carried out by a solvent-fusion method to increase its dissolution rate and oral bioavailability. The physicochemical properties of this solid dispersion (SD) were evaluated immediately after preparation by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM), and the oral in vivo bioavailability was studied. In in vitro experiments CA was analyzed by high-pressure liquid chromatography (HPLC) and by gas chromatography-mass spectrometry (GC-MS) in in vivo experiments. The solubility and dissolution rate of CA were improved by the SD technique. A comparison of the pharmacokinetics between CA-SD and free CA was performed in rats. The results showed that CA-SD had a higher bioavailability than free CA after oral dosing. By comparing the AUC0-t of CA and CA-SD, the relative bioavailability of CA-SD to free CA was 295.4%. From these observations it could be concluded that the CA-SD has a higher absorption than pure CA and this corresponds with the dissolution result in vitro.


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