用药效学指标筛选人参皂苷Rg1鼻用制剂的促吸收剂

Screening for Ginsenoside Rg1 Nasal Absorption Enhancers Through Pharmacodynamic Study

目的:用药效学指标筛选人参皂苷Rg1鼻用制剂的促吸收剂.方法:大鼠在体鼻腔灌流实验研究人参皂苷Rg1的鼻粘膜吸收特性;在体蟾蜍上腭法研究人参皂苷Rg1及辅料对纤毛运动的影响;东莨菪碱致小鼠记忆获得障碍模型法粗筛人参皂苷Rg1鼻用制剂的促吸收剂;以正常小鼠空间学习能力为指标筛选人参皂苷Rg1鼻用制剂的促吸收剂.结果:在100～500 μg/mL的浓度范围内,随着人参皂苷Rg1的浓度增加,其吸收速度呈剂量依赖性增加;人参皂苷Rg1、CMC-Na、液体石蜡、冰片组成的鼻用制剂对纤毛无毒、对东莨菪碱导致的记忆获得障碍具有恢复作用;对正常小鼠的空间学习能力有提高作用.结论:人参皂苷Rg1无纤毛毒性,鼻腔给药安全;冰片对人参皂苷Rg1的鼻腔吸收有促进作用.

AIM： Screening for Ginsenoside Rgl nasal absorption enhancers through pharmaeodynamie study. METHOD： Nasal circulatory perfusion test in vivo had been employed to investigate the characteristics of nasal mucosa absorption ginsenoside Rgl in rats. ginsenoside Rgl and exeipients on cililary movement were evaluated with in situ toad palate model. Screening for ginsenoside Rgl nasal absorptiong enhancers through scopolamine induced memory deficits in mice in step-down test and normal mice in water maze test. RESULT： The absorption rate constant was increased with the elevated ginsenoside Rgl at the range of 1130 ～ 500 μg/mL. The preparation composed of ginsenoside Rgl, CMC-Na, borneol or liquid paraffin are safe to ciliary of toad and can improve the memary function of scopolamine induced memory deficits in mice in step-down test and normal mice in water maze. CONCLUSION： Ginsenoside Rgl nasal preparation is safe and effective. Ginsenoside Rgl can be absorbed via nasal safely and effectively. Borneol can promote the nasal absorption of ginsenoside Rg1.