Development of ibuprofen dry suspensions by hot melt extrusion

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.

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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. Continue on ibuprofen dry suspensions

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