Enhancement of ketoprofen bioavailability by formation of microsponge tablets.

The release of ketoprofen incorporated into modified release ketoprofen microsponge 200 mg tablets and Profenid Retard 200 mg was studied in vitro and in vivo. The formulation containing ketoprofen microsponges yielded good modified release tablets. An in vivo study was designed to evaluate the pharmacokinetic parameters and to compare them with the commercially available ketoprofen retard tablets containing the same amount of the active drug. Commercial ketoprofen retard tablets showed a more rapid absorption rate than modified release tablets and peak levels were reached within almost 3.6 h after administration. However, the new modified release tablets showed a slower absorption rate and peak levels were reached 8 h after administration.

The consolidation and compressibility properties of some novel directly compressible filler-binders.

The aim of this study was to investigate the consolidation and compressibility properties and also the dilution potentials of some novel directly compressible filler-binders. For this purpose, Ludipress and Cellastose 80 (one-body compounds), Tablettose 70 and Tablettose 80 (alpha-mono agglomerated lactose) were selected. They were diluted at predetermined percentages with Spherolac 100 which is a coarse sieved hydrous crystalline lactose. The consolidation and compressibility properties of the prepared powder mixtures were determined. The experimental data were evaluated by using a computer programme (Basic 80).

Design of vitamin E d-α-Tocopheryl Polyethylene Glycol 1000 Succinate-Emulsified Poly (D,L-Lactide-co-Glycolide) Nanoparticles: Influence of Duration of Ultrasonication Energy.

The aim of this research was to investigate the effect of the duration of ultrasonication energy on the physicochemical characteristics of the nano-sized particulate drug delivery systems. For this purpose, meloxicam-loaded vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)-emulsified poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles were designed by using ultrasonication-solvent evaporation technique and were characterized by photon correlation spectroscopy for size and size distribution, scanning electron microscopy for surface morphology and laser Doppler anemometry for surface charge. Ultraviolet -spectrophotometer was used to measure the drug encapsulation efficiency and to obtain in vitro drug release profile. The results showed that the physicochemical properties of the prepared nanoparticles are effectively controlled by the amount of shear stress transferred from the energy source to the emulsion, which is strongly correlated to the ultrasonication time.

Development and in vitro evaluation of pantoprazole-loaded microspheres.

Pantoprazole is a proton pump inhibitor prodrug used in the treatment of gastric ulcers and gastroesophageal disease. Pantoprazole must be absorbed in the gastrointestinal tract and because it is unstable under acidic conditions, enteric delivery systems are required. The purpose of this study was to prepare pantoprazole-loaded microspheres by emulsion-solvent evaporation technique using two different types of enteric-coating polymers: Eudragit S 100 and hydroxypropyl methylcellulose phtalate. The microspheres have been characterized in terms of their morphology, encapsulation efficiency, and ability of stabilizing pantoprazole in acidic media. Pantoprazole determinations were carried out using a validated spectrophotometric method for the analysis of drug in dissolution media. All microspheres, except F2 formulation, were successfully obtained. The in vitro assay showed that especially F1 and F4 microspheres were more effective in protecting the drug than F3 microspheres in acidic media.