Buscador de Personas - SIGEVA - Universidad Nacional de Córdoba

Introduction Controlled release technology has rapidly emerged over the past three decades as a new interdisciplinary science that offers novel approaches to the delivery of drugs. Multiparticle systems offer several advantages over single unit dosage forms, such as, homogeneous distribution within the contents of the gastrointestinal tract, less risk of drug dumping and local irritation and better flow properties. Extrusion Spheronization (E-S)technique is widely used due to its advantages: ease of operation, high throughput with low wastage, narrower particle size distribution, production of pellets with low friability and better controlled drug-release profile when compared with other techniques1 Materials and Methods Gelucire 50/02® [being a blend of mono-, di- and tri-glycerides and mono- and di-fatty acid esters of poly(ethylene glycol)] was used as matrix former this work. Sodium dodecyl sulfate (SDS) was added in different concentrations to evaluate its influence in morphological characterization and the dissolution rate profiles. E-S was the chosen technique to obtain three formulations of spherical pellets with increasing concentrations of SDS 0.05, 0.25 and 0.5%w/w (F1, F2 and F3 respectively). Size, sphericity index (SI) and solids loss were quantified. The moisture content was assayed during the E-S process and the dissolution rate profiles were obtained by triplicate in phosphate buffer, pH = 7.2 (ap. 1 USP, 75rpm). F1, F2 and F3 were compared with a commercial immediate release tablet in this test. IBU concentration in dissolution samples was determined by Uv-Vis at 273nm. Results Regarding morphological analysis, the amount of SDS influenced the sphere size, increasing as increased SDS concentration (F1:1.448±0.159, F2:1.476±0.220 and F3:1.573±0.178), the same occurred with SI (F1:0.716±0.075, F2:0.813±0.129, F3:0.897±0.052) while solids loss had the opposite tendency (F1:14.31±2.18%, F2:6.82±2.63% and F3: 5.95±1.68%). Gelucire® 50/02 was a conditioning parameter on the dissolution tests, 80% of the initial dose was dissolved at 8 hours. No significant differences were observed between F1, F2 and F3 on the in vitro dissolution assays. The moisture content decreased over the stages of E- S from an initial value of 14% to 1% after 24 hs at room temperature. Discussion SDS concentration was a relevant parameter on morphology characterization and solids loss assays, being F3 the formulation that presented better SI and less solids loss. On the other hand SDS concentration did not show important effects on the dissolution tests. The presence of Gelucire® 50/02 as matrix former was found to strongly affect drug release rate. Conclusions E-S is widely applied method for the production of multiparticulates, like pellets and beads. Today this technology has gained attention because of its simple and fast processing. In this case, E-S provided an effective technique to obtain good quality lipid-based matrix pellets. Every stage over S-E process contributed immediately on water loss and consequently with the pharmaceutical performance of the obtained systems.

enviar mensaje