Risedronate-loaded Eudragit S100 microparticles formulated into tablets

Abstract

Risedronate, an anti-osteoporotic drug, is associated with low patient compliance due to the upper gastrointestinal side-effects and stringent dosing regimes. This study aimed to prepare and characterize risedronate-loaded Eudragit® S100 microparticles and develop a final dosage form by the compression of microparticles using direct tableting excipients. Microparticles were prepared by spray-drying and presented yield of 54%, encapsulation efficiency higher than 90%, mean diameter of 3.3 µm, moisture content around 8% and exhibited spherical shape and poor flowability. At pH 1.2, 23% of risedronate was released from microparticles in 120 min, while at pH 6.8 the drug took 90 min to reach 99.5%. Microparticles were compressed into tablets using microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide and 2 polyvinylpyrrolidone concentrations (5% and 15%). Tablets presented low variations in weight, thickness and drug content. Besides, the formulations showed sufficient hardness, low friability and disintegrated in less than 15 min. In acid medium, no more than 16% of the drug was released in 120 min, while in intestinal medium the formulations prolonged the risedronate release for 240 min. Finally, the developed tableted microparticles can be considered a promising dosage form for oral risedronate administration.

Pullulan: an advantageous natural polysaccharide excipient to formulate tablets of alendronate-loaded microparticles

“…In this sense, the selection of a suitable excipient can be considered an interesting approach to form multiple unit tablets. In general, materials that deform plastically, such as microcrystalline cellulose, give the best protective effect (Torrado, Augsburger, 1994;Beckert, Lehmann, Schmidt, 1996;Velasquez et al, 2014). Moreover, an ideal excipient should result in hard and disintegrating tablets at low compression forces and should not affect drug release (Bodmeier, 1997).…”