Drug delivery systems comprising weakly basic selective serotonin 5-HT3 blocking agent and organic acids

摘要

Disclosed is a pharmaceutical multiparticulate dosage form comprising one or more populations of sustained-release (SR) beads and/or one or more populations of timed, pulsatile release (TPR) beads of a weakly basic drug; wherein the weakly basic drug comprises a nitrogen (N)-containing selective serotonin 5-HT3 blocking agent, or a pharmaceutically acceptable salt thereof, having a pKa in the range of from about 5 to 14 and a solubility of not more than about 200 micrograms/mL at pH 6.8; wherein the SR beads comprise organic acid core particles coated with a SR coating, the TPR beads comprise organic acid core particles coated with a lag-time coating, and the organic acid core particles comprise at least one pharmaceutically acceptable organic acid and the weakly basic drug; and wherein the weakly basic drug and the organic acid do not contact each other in the dosage form and a method to prepare the same.