Abstract

Objective To 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.Results We 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.Conclusion SHODT based on nanoparticles-in-microsphere system possess an effective anti-motion sickness effect.

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