1986 年 17 巻 4 号 p. 669-676
A newly-designed sustained-release suspension, Pharma Zomes ®-acetaminophenliquid, was evaluated for its release characteristics in vitro and its bioavailability following oral administration to human volunteers.
The in vitro studies showed sustained release of acetaminophen in which the release rate was not influenced by pH, ionic strength, or the presence of a surfactant inthe release media. The release profiles and scanning electron micrographic observation indicated that Pharma Zomes®suspension contained polymer microchips encasing the drugs and the mechanism of sustained release was mainly by diffusionthrough water-insoluble monolithic system.
The extent and rate of bioavailability of acetaminophen following oral administration of Pharma Zomes ® suspension were studied in five normal volunteers. Pharmacokinetic parameters were determined by measuring the salivary concentrations of thedrug after single administration. Comparing Pharma Zomes ® with simple solution and powder, AUC0-∞ values were not significantly different. On the other hand MRT0-∞and kei were significantly longer or smaller, respectively . The in vivo study demonstrated that Pharma Zomes® showed sustained release properties with adequatebioavailabiity.