Development of Apremilast Solid Dispersion Using TPGS and PVPVA with Enhanced Solubility and Bioavailability.

摘要: Apremilast (APST) is an effective inhibitor of phosphodieasterase 4 (PDE4) which the first oral drug for treatment adult patients with active psoriatic arthritis. However, Apremilast's low solubility restricts its dissolution and bioavailability. In this study, APST solid dispersion D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) Poly(1-vinylpyrrolidone-co-vinyl acetate) (PVPVA) was developed to improve bioavailability by spray drying. A series TPGS were synthesized elucidate effect ratio monoester diester on solubilizing capacity. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectrophotometry (FT-IR) used characterize dispersion, results showed that amorphous in dispersion. vitro study rate phosphate buffered saline (pH 6.8) remarkably increased, reaching a release 90% within 10 min. Moreover, vivo pharmacokinetics revealed rats had significant improvement. particular, Cmax AUClast nearly 22- 12.9-fold greater as compared form B, respectively. conclusion, PVPVA alternative delivery system APST.