Abstract:
The aim of this study was to prepare sustained release multiple unit dosage form (MUDF) for the oral day delivery of the
frequently administered and the highly water soluble drug, dexketoprofen trometamol (DT). The drug was encapsulated
into Eudragit RS100 microspheres using emulsification solvent evaporation technique. A D-optimal design was used to
determine the effect of amount of polymer (X1), the percentage of hydrophobic plasticizer (X2), the percentage of
hydrophilic plasticizer (X3), and stirring rate (X4), on the % entrapment efficiency (Y1), amount of drug released at 1h
(Y2), 4h (Y3), and 8 h (Y4). The optimized formulation was prepared using 1.39 g Eudragit, 0.063 g Dibutyl phthalate
(DBP), 0.093 g Polyethylene Glycol 400 (PEG 400) and processed using stirring rate of 683 rpm. The optimized
microspheres were evaluated by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and X-
ray Diffraction (XRD). Results of the optimized formula showed that the microspheres were spherical with a rough
surface and a particle size of 32±1.41 µm, with entrapment efficiency 76.0±1.76%. The amount of drug released was
33.7±0.82%, 60.2±0.05%, and 75.1±1.84%, at 1, 4, and 8 h, respectively. Complete drug release was achieved after 16 h.
The sustained release pattern of DT for up to 16 h with an acceptable initial release suggests that the developed MUDF
may be useful for oral day delivery of the highly soluble and frequently administered drug such as DT
