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三七总皂苷脂质体的药剂学性质及大鼠肺部给药药动学研究 被引量:36

Panax notoginseng saponin liposomes:Characterization of pharmaceutics and pharmacokinetics on pulmonary instillation in rats
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摘要 目的 制备三七总皂苷 ( Panax notoginseng saponins,PNS)脂质体 ,研究其药剂学性质及在大鼠体内药动学行为。方法 采用薄膜分散法制备 PNS脂质体 ,考察其形态、粒径、包封率及稳定性 ,采用肺部滴注给药考察脂质体在大鼠体内的药动学行为。结果  PNS脂质体包封率为 78.5 0 % ,平均粒径为 1.5 μm,外形圆整 ,体外泄漏慢 ,需低温保存。 PNS脂质体经大鼠肺部滴注给药后 ,体内人参皂苷 Rb1的药动学参数分别为 T1 /2 α=7.0 0 h,T1 /2 β=2 7.72 h,AU C=2 2 18.9μg· h/m L,绝对生物利用度为 70 .14 %。结论  PNS脂质体包封率高 ,性质稳定 ,延长PNS在血循环的时间 ,提高了经血管外给药途径的 PNS生物利用度。 Object To prepare Panax notoginseng saponin (PNS) liposomes and investigate their characterization of pharmaceutics and pulmonary pharmacokinetics in rats. Methods The film-disperion method was used to prepare PNS liposomes by investigating its form, vesicle size, entrapping efficiency and stability. The study of pulmonary pharmacokinetics in rats was carried out by pulmonary instillation. Results The entrapment of PNS liposomes was 78.50%. The mean vesicle size was 1.5 μm with uniform externality. The drug leakage from PNS liposomes was slow. Low temperature was required for its storage. The pulmonary pharmacokinetics parameters were as follows: T 1/2 α=7.00 h, T 1/2 β=27.72 h, AUC= 2 218.9 μg·h/mL, the absolute bioavailability was 70.14%. Conclusion PNS liposomes with high entrapment and stability can prolong its circulation in blood and improve the PNS bioavailability via lung approach.
作者 沈央 方晓玲
出处 《中草药》 CAS CSCD 北大核心 2004年第7期745-749,共5页 Chinese Traditional and Herbal Drugs
基金 复旦大学研究生创新基金资助
关键词 三七总皂苷脂质体 包封率 粒径 稳定性 药动学 Panax notoginseng saponin (PNS) liposomes entrapping efficiency vesicle size stability pharmacokinetics
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  • 1Liu F Y,Pharmacol Res,1993年,10卷,2期,228页
  • 2Sone S,J Biol Response Modif,1984年,3卷,185页

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