ABSTRACT:
Budesonide is widely used drug for treatment of active inflammatory bowel disease (IBD). Core in-cup tablets were prepared to achieve a prolonged release of Budesonide and for alleviating the symptoms of inflammatory bowel disease. The objective of this study was to investigate differences in the pharmacokinetic patterns between an optimized core in cup tablet formulation and pure Budesonide suspension. In-vivo evaluation studies were performed based on the uniform and reliable results of in-vitro drug release studies. Various pharmacokinetic parameters were compared to obtain mean plasma drug concentration curve versus time. The pure drug suspension and Core-in-cup tablets formulation of Budesonide were administered to two groups of white New Zealand rabbits (n=6) through the oral route following cross over design pattern. The drug concentration in plasma samples were measured using LC-MS/MS method. Pharmacokinetic parameters were determined for each formulation. The comparison of the plasma time curves of the dosage forms showed that each dosage form caused significant differences in the drug plasma levels. The optimized core in cup tablet formulation shown some lag phase initially before releasing the drug. The mean residence time of core in cup tablet formulation was found to be more than the pure drug suspension formulation. The oral administration of Budesonide resulted in a low and quite variable AUC of 154.1±1.44 ng/ml/hr., whereas the optimized core-in-cup tablets resulted in AUC of 918.2±3.11 ng/ml/hr. The bioavailability of optimized formulation was enhanced six times compared with pure drug suspension. From the above results, it can be concluded that the prepared core in cup tablet can be considered as one of the promising formulation techniques for chronotherapeutic management of inflammatory bowel disease.