In vitro - In vivo Correlation Study of Colon-targeted Metronidazole Microparticle in Corncob Hemicellulose Capsule

Abstract

: Colon-targeted therapy requires a strategy to keep the medicine pass the stomach and release in the colon, which is hard to reach by conventional dosage form of metronidazole in gelatin capsule. In this study, microparticles dosage form of metronidazole which was placed inside corncob-hemicellulose capsule shell need to be compared with conventionally gelatin capsule of metronidazole preparation to examine whether it meets medications standards. The aim of this study was to find out the in vitro and in vivo assay correlation of metronidazole microparticle which covered by corncob hemicellulose capsules. In vitro test was carried out to observe the profile of differences in the percent release of metronidazole from various formulations with various media and times. It was performed using a dissolution tester, in an artificial stomach medium of pH 1.2 for 6 hours in artificial intestinal medium of pH 7.4 for 10 hours, and in artificial colonic medium of pH 8 for 10 hours. The in vivo test design was conducted using six rabbits. The drug released in plasma was measured by HPLC using 1% glacial acetic acid solvent in aqua bidest and methanol-water with a ratio of 80: 20. The test was performed using the cross over design method. Metronidazole microparticle capsules were administered orally according to the test design (metronidazole in microparticles and metronidazole in conventional forms). Based on the plotted graph (data retrieval was started from the drug released in the colon because the drug began to be absorbed at that time), a correlation value was obtained (R 2 = 0.8785). It can be stated that there is a correlation between the formulations tested in vitro and in vivo because the correlation value was greater than 0.8, it is assumed to have a correlation.