目的观察知母微粉体外成分溶出以及体内活性,对微细化工艺在中药中的应用进行评价。方法采用HPLC法定量芒果苷,比较知母微粉和知母粉中芒果苷溶出速度及不同时间点溶出百分率;采用小鼠悬尾和强迫游泳试验,测定最大耐受量,观察知母微粉与知母提取物体内活性和安全性。结果体外溶出时,知母微粉中芒果苷的溶出速度较知母粉明显加快,在不同时间点芒果苷的溶出百分率亦有所提高;以相同治疗剂量给药时,知母微粉与知母提取物表现出相当的作用,知母微粉最大给药剂量为20 g/kg。结论知母制成微粉后能在一定程度上改善体外成分的溶出和体内活性。

Objective To investigate the ingredients dissolution and bioactivities of Anemarrhena asphodeloides micropowder prepared by super fine crushing technique. Methods The dissolution of the marker ingredient—mangiferin of the micropowder was compared with that of the normally processed powder by HPLC for mangiferin; the anti-depression effect of the micropowder and A. asphodeloides extract was investigated in tail suspension test and forced-swimming test. Meanwhile, toxicities were evaluated by the determination of the maximum tolerated dose (MTD). Results The dissolution velocity of mangiferin in the micropowder was more obviously improved than that in the common powder and the dissolution percentages at different intervals had been increased slightly. The micropowder showed as much anti-depression effect as that of the A. asphodeloides extract when administered at the same dosage, while they both resulted in relatively obvious toxicity reactions (MTD is 20 kg/g). Conclusion Super fine crushing technique can help to improve the ingredients dissolution rate and bioactivities of A. asphodeloides micropowder without bringing about additional toxicity.

清华大学基础研究资金资助项目(JC2001050)