| 摘要: |
| 目的评价基于纳米粒-微球系统(NiMS)的氢溴酸东莨菪碱口崩片对晕动病的防治作用。方法(1)将小鼠放进旋转刺激装置中进行旋转刺激，制备小鼠晕动综合征模型，出现立毛、肌肉震颤、大小便失禁症状等，观察实验前20 min灌胃给予口崩片6、12、24 mg/kg对小鼠晕动病样综合征的预防和治疗作用。(2)家兔右侧颈总动脉局部敷贴胆碱酯酶抑制剂对氧磷，家兔出现逆向(左向)转圈，逆向转圈3转/min以上为阳性症状；实验前10 min将口崩片按0.12、0.24、0.36、0.48、0.72、0.96、1.44 mg/kg置于家兔口中令其自然崩解后吞咽，观察对晕动病的防治作用。结果对于小鼠晕动病样综合征，氢溴酸东莨菪碱口崩片6 mg/kg与等剂量普通片相比差异无统计学意义(P=0.674)，与空白组相比差异有统计学意义(P=0.001)。口崩片抗晕动效果在6~24 mg/kg范围内具有剂量依赖性。对于家兔逆向转圈综合征，氢溴酸东莨菪碱口崩片的半数有效量(ED50)为0.476 mg/kg，剂量取对数后对抑制率进行曲线拟合，方程为y=0.679x+0.724，R=0.929。结论基于NiMS的氢溴酸东莨菪碱口崩片具有抗晕动效果。 |
| 关键词: 口崩片 东莨菪碱 晕动病 治疗结果 |
| DOI：10.3724/SP.J.1008.2011.0299 |
| 投稿时间：2010-12-20修订日期：2011-02-01 |
| 基金项目:国家科技重大专项基金(2009ZX09004-069). |
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| Efficiency of scopolamine hydrobromide orally disintegrating tablets in treatment of motion sickness |
| ZHAO Yi, HU Jin-hong*, ZHU Quan-gang, LIU Ji-yong |
| (Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| 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. |
| Key words: orally disintegrating tablets scopolamine motion sickness treatment outcome |
