Abstract
The aim of this study was to develop ibuprofen dry suspensions using hot melt extrusion to improve the in vivo performance of ibuprofen. Ibuprofen was melt-extruded into solid dispersions with hydroxypropylmethylcellulose (HPMC) and Eudragit® E PO, respectively. The dry suspensions were prepared by mixing the solid dispersions with other necessary ingredients. Physical state characterization, dissolution tests, physical stability and pharmacokinetics in rats were carried out. Ibuprofen-Eudragit® E PO dry suspensions (Ibu-EPO) showed the highest in vitro drug release rate, whereas incomplete drug release was observed from ibuprofen-HPMC dry suspensions (Ibu-HPMC) and Motrin®. A 30-day stability study under 60 °C/0%RH showed that dissolution profile and physical state of Ibu-HPMC and Ibu-EPO both remained the same as the fresh samples. Pharmacokinetic studies, however, showed the opposite of in vitro results. The Cmax and Tmax of Ibu-HPMC (112.22 ± 50.68 μg/ml and 0.71 ± 0.66 h) and Motrin® (79.00 ± 25.77 μg/ml and 0.54 ± 0.30 h) indicated significantly higher in vivo drug release and absorption rate than Ibu-EPO (35.29 ± 10.26 μg/ml and 2.75 ± 0.86 h). In addition, Ibu-HPMC were confirmed with the highest in vivo drug exposure (AUC0–12h = 450.70 ± 128.82 μg/ml·h). Ibuprofen-HPMC dry suspensions developed in this study were physically stable and could effectively improve the in vivo behavior of ibuprofen.
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