Preparation and Characterization of Lurasidone Hydrochloride Solid Dispersion and Study on the in vitro Dissolution Behavior / 中国药房

ABSTRACT

OBJECTIVE:To prepare the lurasidone hydrochloride solid dispersion,and improve its dissolution rate. METH-ODS:Taking povidone K30 as the carrier,solvent method was used to prepare the lurasidone hydrochloride solid dispersion with different drug-load ratios(1:0.5,1:1,1:2). The in vitro dissolution rates of 3 kinds of lurasidone hydrochloride solid dispersion with physical mixture (lurasidone hydrochloride-povidone K30) and original preparation were compared. X-ray powder diffraction method was adopted to analyze the crystal structures of raw material of lurasidone hydrochloride,povidone K30 and accessories, physical mixture (1:2) and accessories,and lurasidone hydrochloride solid dispersion (1:2) and accessories. RESULTS:Com-pared with physical mixture,the dissolution rate of lurasidone hydrochloride solid dispersion with drug-load ratios of 1:0.5,1:1, 1:2 was significantly improved,and the dissolution rate of solid dispersion was increased as the increase of the carrier ratio. The in vitro dissolution rates of lurasidone hydrochloride solid dispersion with drug-load ratio of 1:2 and original preparation were respec-tively 101.2%and 100.2%in 20 min. X-ray powder diffraction showed,there were characteristic absorption peaks of lurasidone hy-drochloride and accessories in physical mixture;the characteristic absorption peak of lurasidone hydrochloride in solid dispersion disappeared basically,and the characteristic absorption peak of accessories still existed. CONCLUSIONS:The in vitro dissolution of lurasidone hydrochloride solid dispersion with drug-load ratio of 1:2 is similar to original preparation,and lurasidone hydrochlo-ride exists in the solid dispersion as amorphous form.