Preparation of Epalrestat Solid Dispersion by Hot-Melt Extrusion Technique / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare epalrestat (EP) solid dispersion by holt-melt extrusion (HME) technique in order to enhance its dissolution rate. METHODS: Optimal formula was obtained by screening the carrier type and drug proportion. The dispersion state of EP in the solid dispersion and physical mixture were studied with differential X-ray diffraction (X-RD), Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) analysis techniques. RESULTS: Poloxamer 188 was selected as the carrier with the optimal ratio of Poloxamer188 to EP of 1∶3. The final solid powder product was homogeneous dispersion in light yellow color without any agglomerate. CONCLUSION: The carrier of EP solid dispersion has significant impact on the dissolution behavior and state of EP. Using Poloxamer 188 as the carrier, holt-melt extrusion is an effective technology for improving the in vitro dissolution of EP.