In Vitro and in Vivo Evaluation of Anethole Trithione Solid Dispersions

OBJECTIVE To development anethole trithione(ATT) solid dispersion with high dissolution and bioavailability using hot-melt extrusion. METHODS Solid dispersion with carrier of Plasdone S630 was preparaed by hot-melt extrusion and then characterized by differential sacanning calorimetry(DSC), X-ray powder diffraction(XRPD), in vitro dissolution test, and in vivo bioavailability study. RESULTS ATT exited as amorphous or molecular state in solid state that could be proved by DSC and XRPD. The dissolution rate of ATT was significantly accelerated. The dissolution profile and the solid state properties of the product were maintained after storage at 40 ℃, 75% RH for 6 months. The results of pharmacokinetics in beagles showed that the Cmax and AUC of ATT solid dispersions were 1.66 times and 1.57 times high than reference preparation. CONCLUSION ATT solid dispersion preparaed by hot-melt extrusion is thermodynamically stable system. The dissolution in vitro and bioavailability in beagle dogs after oral administration is markedly improved.