灯盏花素口崩片在Beagle犬体内的药动学及相对生物利用度研究

Breviscapine Orally Disintegrating Tablets In Study on Pharmacokinetics and Relative Bioavailability in Beagle Dogs

为了研究Beagle犬经口给予受试制剂灯盏花素口崩片和参比制剂灯盏花素片的药动学,对比分析了两制剂的药代动力学参数,评价了灯盏花素口崩片的相对生物利用度。6只Beagle犬,分为两组,每组3只,分别给予两种制剂,自身双交叉实验,采用HPLC-MS/MS法检测Beagle犬血浆中灯盏花乙素苷元。结果表明,灯盏花素口崩片和灯盏花素片主要的药动学参数分别是:Cmax为(235.08±112.53)ng/m L、(267.90±111.04)ng/m L,tmax为(6.33±6.05)h、(4.33±1.92)h,AUC(0-t)为(1554.58±548.49)ng/(m L·h)、(1628.08±408.78)ng/(mL·h)。受试制剂灯盏花素口崩片的相对生物利用度为102%。两制剂的tmax、Cmax和AUC(0-t)差异均无统计学意义(p>0.05),灯盏花素口崩片与的灯盏花素片具有相似的生物利用度。

Objective:To study the pharmacokinetics of the test preparation breviscapine orally disintegrating tablets and the reference preparation breviscapine tablets in Beagle dogs,to compare and analyze the pharmacokinetic parameters of the two preparations,and to evaluate the breviscapine oral disintegration Relative bioavailability of tablets.Methods:6 Beagle dogs were divided into two groups,3 dogs in each group.Two preparations were given respectively.The double-crossover experiment was performed by itself,and the scutellarin aglycone in the plasma of Beagle dogs was detected by HPLC-MS/MS.Results:The main pharmacokinetic parameters of scutellarin orally disintegrating tablets and scutellarin tablets were:Cmax(235.08±112.53)ng/m L、(267.90±111.04)ng/m L,tmax(6.33±6.05)h、(4.33±1.92)h,AUC(0-t)(1554.58±548.49)ng/(m L·h)、(1628.08±408.78)ng/(m L·h).The relative bioavailability of the tested preparation breviscapine orally disintegrating tablets was 102%.Conclusion:There is no statistically significant difference in tmax,Cmaxand AUC(0-t)between the two preparations(p>0.05).Breviscapine orally disintegrating tablets and breviscapine tablets have similar bioavailability.