微细化工艺制备的葛根微粉溶出度和生物利用度的研究

Study on the dissolution rate and bioavailability of Radix Pueraria micropowder prepared by super fine crushing process

目的 研究葛根微粉在溶出和生物利用度方面的效果,为微细化工艺在中药中的应用提供理论依据。方法 以葛根黄酮为指标,用紫外分光光度法测定葛根微粉和葛根粉在不同时间点葛根黄酮溶出的量,计算累积释放率;采用透析袋为屏障观察葛根微粉和葛根粉的溶出情况。按葛根素100mg·kg-1体重分别给大鼠口服葛根微粉和提取物,用HPLC测定葛根素含量,以葛根提取物为对照,计算葛根微粉的相对生物利用度。结果 用桨法测定体外溶出度时,葛根微粉累积释放度显著高于葛根粉;用透析袋作为屏障时,两者差异不明显。葛根微粉的生物利用度是葛根提取物的50％强。结论 葛根制成微粉后,能改善其有效成分的溶出,但是与提取物相比,服药量大,生物利用度低,因此微米中药的应用有待进一步评价。

OBJECTIVE: To study the dissolution rate and bioavailability of Radix Pueraria prepared by (SFCP) provide theory proof for the application of SFCP to Chinese herb. METHODS: The isoflavones in the micropowder and powder of Radix Pueraria were determined by UV to calculate the cumulative release at different time with and without the barrier of dialytic membrane. The concentration of puerarin was detemined by HPLC to calculate the bioavailability of micropowder relative to extract after po administration in rats at the dose of 100 mg&middot kg-1. RESULTS: The dissolution rate of isoflavones in micropowder was significantly improved in contrast to powder. The bioavailability of micropowder was 50% or more of the extract. CONCLUSION: Micropowdering could improve the dissolution rate of isoflavones of Radix Pueraria, but reduce the bioavailability in contrast to the extract.