石菖蒲挥发油β-环糊精、羟丙基-β-环糊精包合物在大鼠体内药代动力学研究  

Study of Pharmacokinetics and Bioavailability of Beta-cyclodextrin and Hydroxypropyl-beta-cyclodextrin Inclusion Compound of Volatile Oil from Rhizoma Acori Tatarinowii in Rats

作　　者：胡奎[1] 苏梦[1] 徐鑫[1] 薛雪梅[1] 刘艳菊[1,2] 许汉林[1,2] 

机构地区：[1]湖北中医药大学药学院,湖北武汉430065 [2]湖北省中药炮制工程技术中心,湖北武汉430065

出　　处：《中药新药与临床药理》2017年第2期187-190,共4页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：科技部科技基础专项(2014FY111100-2);湖北省老年病中药新产品协同创新中心项目

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/C^2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。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.

关 键 词：石菖蒲 挥发油 Β-环糊精 羟丙基-Β-环糊精 包合物 药动学 生物利用度 

分 类 号：R284.1[医药卫生—中药学]