Desenvolvimento de sistemas microparticulados a partir da blenda Eudragit® L100 e goma gelana para liberação oral de cetoprofeno

Abstract

Ketoprofen is a non-steroidal anti-inflammatory drug with analgesic and antipyretic properties. However, this drug has a short half-life, and causes adverse effects on the gastrointestinal tract by limiting its application in the pharmaceutical field. This way, microparticulate systems become an alternative to overcome these problems. In this study, polymer microparticles containing ketoprofen were prepared from three proportions (1:1, 2:1 and 1:2) of the Eudragit® L100 blend and gellan gum by spray-drying technique. Three formulations were obtained in yield ranging from 28% to 47%, with a ketoprofen content of close to 100%. The mean particle size ranged from 7.8 μm to 11 μm with narrow size distribution and spherical shape. The Carner Index and Hausner's Factor indicated low fluidity. Microparticles with highest proportion of Eudragit® L100 presented a better gastroresistance profile. At pH 1.2, 12% of ketoprofen was released in 120 min, whereas in simulated intestinal medium the formulation was able to prolong the release of the drug. Mathematical modeling showed that the release of this drug followed first-order kinetics and occurred by anomalous transport. These microparticles suffered direct compression. Microparticulate tablets had acceptable mean weights, drug content and content uniformity close to 100%, suitable hardness and thickness. In vitro studies showed that gastroresistance was maintained because no more than 7% of the drug was released for 120 min at pH 1.2 while at pH 6.8 the drug release was prolonged for 180 min following first order kinetics and release by anomalous transport. In view of this, it can be concluded that formulations containing ketoprofen are promising systems for oral administration and release control of this drug.