Therapeutic Research

Abstract

Some combination of drugs under one‒dose packaging has been reported to cause changes in tablet appearance and/or dissolution behavior. In this study, changes in appearance and dissolution behavior of Bayaspirin(R) tablet and different telmisartan preparations（a brand‒name drug, Micardis(R), and 11 generic drugs）were examined after one‒week contact with or without one‒dose packaging. Bayaspirin(R) 100 mg tablet and each telmisartan 40 mg tablet were stored at 30℃ with 75％RH for one week, being placed in a 48‒well plate with the surfaces of the two tablets in contact or under one‒dose packaging. Change in appearance was evaluated by visual inspection, and if any change was observed, dissolution behavior and residual rate of Bayaspirin(R) tablet and each telmisartan tablet were assessed. Color changes in the tablet appearance were observed for the combinations of Bayaspirin(R) tablet contacted with 3 telmisartan tablets（Micardis®, telmisartan“DSEP” or telmisartan“YD”tablets）. As for the dissolution test of Bayaspirin(R) tablet contacted with Micardis(R) tablet or telmisartan“DSEP”tablet without one‒packaging, drug dissolution in the 1st fluid for dissolution test（pH 1.2）and rapid resolution in the 2nd fluid for dissolution test（pH 6.8）were observed. Same alternations of the dissolution behavior were observed for the Bayaspirin(R) tablet contacted with Micardis(R) tablet（8 out of 12 samples）or telmisartan“DSEP”tablet（9 out of 12 samples）after one week one‒dose packaging. Dissolution of telmisartan OD“TOWA”was delayed with or without contact with Bayaspirin(R) tablet. No change was observed in the residual rate of aspirin or telmisartan formulations in any preparation. Based on the findings, storage of Bayaspirin(R) tablet in a direct contact with Micardis(R) tablet or telmisartan“DSEP”tablet is not recommended neither with or without one‒dose packaging, since the aspirin tablet with altered dissolution behavior may cause gastric mucosal injury in patients who take those.