微细化工艺制备的三七的溶出度及活性研究(九)

Investigation on dissolution and in vivo activity of Panax notoginseng prepared by super fine crushing technique

目的 探讨三七制成微粉 (粒径 99%以上分布在 0～ 30 μm)后 ,与粗粉 [过 5 0目筛 ( 35 5± 13) μm]相比 ,体外溶出情况的变化 ,为微粉技术在中药中的应用提供理论依据并建立相应的评价方法。方法 选取三七中主要成分Rg1为指标成分 ,用反相HPLC测定不同时间点三七微粉和粗粉中Rg1溶出的量 ,并采用透析袋作为屏障观察三七微粉和粗粉中Rg1在透析袋中的溶出情况。并以凝血时间、最大耐受量为指标 ,观察微粉对小鼠凝血系统的影响及急性毒性。结果 一定时间后 ,三七微粉中Rg1溶出的速度和程度均较粗粉的有明显提高 ( 15～ 4 5min ,P <0 .0 5 ,4 5～ 6 0min ,P <0 .0 1)。但用透析袋作为屏障时 ,两者差异不明显。小剂量凝血时间 [( 12 2 .85± 5 4 .82 )s]与蒸馏水组 [( 6 7.98± 2 2 .6 7)s]相比 ,有明显差异 (P <0 .0 5 )。结论 三七制成微粉后 ,能有效改善其有效成分的溶出效率 ;对药物作用有一定的促进作用 ,但进一步的评价有待于更多的实验数据。

OBJECTIVE: To investigate the experimental proof for the application of super fine crushing technique (SFCT) to the traditional Chinese medicinal herb and develope new methods to evaluate the effect of SFCT on drug. METHOD: The dissolution of Panax notoginseng prepared by different techniques were investigated by determining ginsenoside Rg1 as the test marker. Ginsenoside Rg1 in micropowder (mostly over 0 ∼ 30μm) and crude powder [filtered by 50 mesh sifter (355 ± 13) μm] with and without the barrier of dialytic membrane was determined at different time by RP-HPLC. RESULT: The speed and degree of dissolution of Rg1 were improved in micropowder than those in crude powder after a certain time (15 ∼ 45 min, P -1 of Panax notoginseng significant increased the time of blood coagulation comparing to control (P < 0.05). CONCLUSION: Both the dissolution of effect component in panax notoginseng and the effect of Panax notoginseng can be improved by SFCT, at the same time, the toxicity was not increased.