中文摘要：

目的研究石菖蒲挥发油的β-环糊精β-CD）、羟丙基-β-环糊精（HP-β-CD）包合物在大鼠体内的药代动力学及生物利用度,从而确定最佳的包合材料。方法SD大鼠分别灌胃给予石菖蒲挥发油药、β-CD包合物及HP-β-CD包合物,采用HPLC法测定给药后不同时间的血药浓度,并采用DAS2.0.1软件计算主要药动学参数。结果灌胃给药石菖蒲挥发油、β-CD包合物、HP-β-CD包合物后,血浆中α-细辛醚血药浓度-时间曲线依次符合权重系数为1,1,1/C2的二室模型,主要药动学参数：C_（max）分别为（2.580±0.247）、（3.598±0.756）、（5.645±0.363）μg·mL~（-1）;T_（max）分别为（10.120±0.760）、（8.082±0.483）、（5.073±0.610）min;AUC_（0-t）分别为（125.121±4.161）、（263.335±16.377）、（432.138±11.208μg·min·mL~（-1）;AUC_（0-∞）。分别为（135.309±9.278）、（295.713±29.775）、（456.652±3.904）μg·min·mL~（-1）。3组间C_（max）、AUC_（0-t）。两两比较,差异有统计学意义（P〈0.05）,β-CD包合物的相对生物利用度为210.46%,HP-β-CD包合物的相对生物利用度为345.38%。结论石菖蒲挥发油与β-CD、HP-β-CD包合后,在大鼠体内的吸收速度明显加快,生物利用度显著提高,且HP-β-CD包合后效果优于β-CD包合。

英文摘要：

Objective To study the pharmacokinetics and bioavaiIability of beta-cyclodextrim（CD）,hydroxypropylbeta-cyclodextrin（HP-β-CD） inclusion compound of the volatile oil from Rhizoma Acori Tatarinowii（RAT） in rats,thus to optimize the inclusion material.Methods After the rats were given gastric gavage of RAT volatile oil,p-CD inclusion compound of RAT volatile oil and HP-p-CD inclusion compound of RAT volatile oil,the plasma concentration was monitored by HPLC at different time points.And DAS2.0.1 software was used to calculate the pharmacokinetic parameters.Results After oral administration in rats,α-asarone plasma-time curve for RAT volatile oil,β-CD inclusion compound of RAT volatile oil and HP-β-CD inclusion compound of RAT volatile oil in rats followed two-compartment model with the weight coefficient being 1,1,1/c~2.And their main pharmacokinetics parameters were as follows：C_（max） was（2.580±0.247）,（3.598±0.756）,（5.645±0.363）μg·mL~（-1）,T_（max）,was（10.120±0.760）,（8.082±0.483）,（5.073±0.610）min,AUC_（0-t） was（125.121±4.161）,（263.335±16.377）,（432.138±11.208）μg·min·mL~（-1）;AUC_（0-∞） was（135.309±9.278）,（295.713±29.775）,（456.652±3.904）μg·min·mL~（-1）.The differences of C_（max）,AUCo_（0-t） between the 3 groups were significant（P〈0.05）.The relative bioavailability of p-CD complex was 210.46%and that of HP-p-CD complex was 345.38%.Conclusion The absorption rate,especially the bioavailability of RAT volatile oil was significantly increased in rats after the volatile oil was included with p-CD and HP-β-CD,and the bioavailability of HP-β-CD connplex was better than that of β-CD connplex.