The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of Glipizide. An anti-diabetic drug, Glipizide, is delivered through the microparticulate system using ethyl cellulose as the controlled release polymer. Microspheres were developed by the emulsion solvent diffusion-evaporation technique by using the modified ethanol,-dichloromethane co-solvent system. The polymer mixture of ethyl cellulose and Eudragit® S100 was used in different ratios (1:0, 1:1, 2:3, 1:4 and 0:1) to formulate batches F1 to F5. The resulting microspheres were evaluated for particle size, densities, flow properties, morphology, recovery yield, drug content, and in vitro drug release behavior. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. Among different formulations, the fabricated microspheres of batch F3 had shown the optimum percent drug encapsulation of microspheres and the sustained release of the Glipizide for about 12 h. Release pattern of Glipizide from microspheres of batch F3 followed Korsmeyers-peppas model and zero-order release kinetic model. The value of ‘n’ was found to be 0.960, which indicates that the drug release was followed by anomalous (non-fickian) diffusion. The data obtained thus suggest that a microparticulate system can be successfully designed for sustained delivery of Glipizide and to improve dosage form characteristics for easy formulation.
The aim of this study was to develop a pH responsive enteric coated extended release multiparticulate dosage form containing a model drug ketoprofen, a nonsteroidal anti-inflammatory drug used for rheumatoid arthritis. The drug loaded pellets in matrix form were prepared by using extrusion/spheronization method. The optimized pelletization method revealed that extrusion using 1 mm sieve plate and spheronization friction disc of 2mm carried out at 700 rpm for 5-10 minutes resulted in good spherical pellets and uniformity in size. Evaluated core pellets were coated with polymer Eudragit® RS 30D on Fluid bed coater to achieve a sustainable release for 12 hours. Ketoprofen as like other NSAID have been reported for gastric mucosal irritation so a pH responsive barrier coat of Eudragit L®100-55 was employed on a pan coater for abstaining release in acidic media. The formulated pellets were characterized for shape and size uniformity, friability, surface morphology studies. The particle size of core and polymer coated pellets were found to be in the range of 0.95-1.2 mm and 1.32-1.51 mm respectively. The pellets were spherical in shape with smooth texture and uniformity in size. In-vitro dissolution tests were carried out for pellets in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the ketoprofen from formulated pellets was established in pH 1.2 for a period of 2 h, followed by pH 7.5 for rest of the study. The study concluded that the formulated multiparticulate dosage form of ketoprofen was able to relieve symptoms of rheumatoid arthritis.
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