ObjectiveTo evaluate the efficiency of scopolamine hydrobromide orally disintegrating tablets (SHODT) based on nanoparticles-in-microsphere system in treatment of motion sickness. Methods(1) Each mouse was placed in a rotation device to induce motion sickness; the animals received gastric infusion of SHODT (6 mg/kg, 12 mg/kg, and 24 mg/kg) 20 min before rotation to observe the preventive and therapeutic effect of SHODT. (2) Paraoxon (10 μl) was locally applied to the right carotid artery of rabbits to induce forced reverse circling (exceeding 3 round/ min was taken as positive). Ten minutes before application of paraoxon, SHODT (0.12 mg/kg, 0.24 mg/kg, 0.36 mg/kg, 0.48 mg/kg, 0.72 mg/kg, 0.96 mg/kg, and 1.44 mg/kg) was put into rabbit mouths for natural disintegration and swallow; symptoms of motion sickness was observed 40 min after paraoxon application. ResultsWe found that SHODT at 6 mg/kg had a similar effect to the same dosage of normal tablets for motion sickness in mice (P=0.674) and had a significantly different effect with blank control (P=0.001). The anti-motion sickness effect of SHODT was in a dose-dependent manner within the range of 6-24 mg/kg. The ED50 value of SHODT was 0.476 mg/kg in rabbits treated with local paraoxon. The linearity formula between the dose in logarithmic and the efficiency was y=0.679x+0.724, R=0.929. ConclusionSHODT based on nanoparticles-in-microsphere system possess an effective anti-motion sickness effect.