摘要
目的考察吸收促进剂对人参皂苷Rg1鼻腔黏膜的吸收促进作用以及对鼻腔黏膜毒性。方法采用大鼠在体鼻腔循环考察人参皂苷Rg1鼻腔吸收及吸收促进剂的促吸收作用,在体蟾蜍上腭纤毛法评价药物对纤毛运动的影响;考察吸收促进剂对家兔血红细胞的溶血作用、对鼻腔循环液中总蛋白和乳酸脱氢酶的影响及对鼻腔黏膜形态学的影响。结果人参皂苷Rg1鼻腔吸收必须加入吸收促进剂。各种吸收促进剂的促进作用为:1%去氧胆酸钠作用显著;1%甘草酸二钾和1%氮酮作用中等;1%Tween-80,2%β-环糊精、0.5%冰片、0.5%壳聚糖、5%羟丙-β-环糊精和0.1%EDTA等作用微弱。吸收促进剂对鼻腔黏膜毒性影响:1%去氧胆酸钠、1%氮酮和1%甘草酸二钾毒性大;1%Tween-80,2%β-环糊精及5%羟丙-β-环糊精等毒性中等;0.5%冰片、0.5%壳聚糖和0.1%EDTA毒性小。结论0.5%冰片与0.5%壳聚糖可安全有效地促进人参皂苷Rg1的鼻腔吸收。
Aim The enhancing activity and safety of several absorption enhancers were evaluated as potential nasal absorption enhancers to increase intranasal absorption of ginsenoside Rgl. Methods Nasal circulatory perfusion test in vivo had been employed to investigate the effect of absorption enhancers for nasal mucosa absorption of ginsenoside Rgl in rats. The safety of the absorption enhancers were evaluated by testing cilia movement of the in situ toad palate model, the hemolysis of erythrocyte membrane of the rabbit, leaching of protein and LDH from the mice nasal mucosa and the effect on cilia structural and specific cellular changes of nasal mucosa. Results Absorption enhancers were necessary to facilitate ginsenoside Rgl absorption by nasal mucosa. Among the absorption enhancers 1% sodium deoxycholate had great effect to facilite ginsenoside Rgl absorption by nasal mucosa; 1% dipotassium glycyrrhizinate and 1% azone had moderate effect to facilitate ginsenoside Rgl absorption by nasal mucosa; 1% Tween- 80, 2% β-cyclodextrin, 0.5% borneol （dissolved in paraffin liquid）, 0.5% chitosan, 5% hydroxypropyl-β-cyclodextrin and 0. 1% EDTA had low effect to facilitate ginsenoside Rgl absorption by nasal mucosa. 1% sodium deoxycholate, 1% azone and 1% dipotassium glycyrrhizinate had serious nasal toxicity; 1% Tween-80, 2% β-cyclodextrin, 5% hydroxypropyl-β-cyclodextrin had moderate nasal toxicity; 0. 5% borneol （dissolved in paraffin liquid）, 0. 5% chitosan and 0. 1% EDTA have little nasal toxicity. Conclusion 0. 5% borneol and 0. 5% ehitosan were the promising candidates having a good balance between enhancing activity and safety for nasal ginsenoside Rgl delivery.
出处
《药学学报》
CAS
CSCD
北大核心
2006年第2期149-155,共7页
Acta Pharmaceutica Sinica
关键词
鼻腔给药
吸收促进剂
人参皂苷RG1
intranasal drug delivery
absorption enhancers
ginsenoside Rg1
