In vivo evaluation of floating tablet clarithromycin 500mg

Abstract

Floating drug delivery system (FDDS) containing Clarithromycin 500mg (CLA) designed to prolong the retention time in the stomach is also an approach to optimize the plasma CLA concentration in the gastric. However, the development of FDDS meets many obstacles about physiology such as cannot control and locate FDDS in gastrointestinal because of the process of stomach emptying. CLA is rapidly absorbed from the gastrointestinal tract, bioavailability in intact form is only about 55% with a relatively short half-life, about 5-7 hours when taking a 500mg dose. Therefore, this research approaching a dosage form CLA to prolong the gastric retention time by in vivo in living body is local dog because the test subject is a dog beagle because anatomically it is quite similar in size to the gastrointestinal tract with the human model. The technical to show CLA image in vivo by X - ray method each time before and after oral administration of a pill and finished until there is no more pill images in the stomach. In addition, plasma drug concentrations were also calculated at each time point using the HPLC with LCMS IT-TOF method and compared with tablets without buoyancy properties. Results of research FDDS containing CLA has been the floating tablet time is 3,5 to 4,5 hours. And plasma concentration between testing group reached at 6 and 8 hours (1964,00 ± 104,25 ng/ml and 1203,00 ± 191,68 ng/ml); and the drud’s peak group reached at 2,5 -3 hours (1169,88 ± 109,42 ng/ml and 1982,63 ± 266,48 ng/ml), respectivety.