Dai Xiao-yan, Yan Yun-liang, Wu Qiao-feng, Yu Chen-huan, Liu Xin, Jiang Ya-qi
Department of Pharmacy, The Third People׳s Hospital of Hangzhou, Hangzhou 310009, China.
Zhejiang Chinese Medical University, Hangzhou 310053, China.
J Ethnopharmacol. 2014 Apr 28;153(2):338-43. doi: 10.1016/j.jep.2014.02.005. Epub 2014 Mar 15.
Quyu Qingre granules (QYQRGs) are useful traditional Chinese composite prescription in the treatment of blood stasis syndrome. Comparing differences of pharmacokinetic properties of compounds in QYQRG between normal and blood stasis syndrome rabbits can provide much helpful information. The primary objective of this study was to compare the pharmacokinetics of rhein and chrysophanol after orally administering 2.0 g/kg b.w. QYQRG in normal and acute blood stasis model rabbits.
The blood samples were collected subsequently at 5, 10, 15, 20, 30, 45, 60, 75, 90, 120, 240, 360 and 480 min after orally administrating QYQRG. The concentrations of rhein and chrysophanol in rabbit plasma were determined by HPLC and main pharmacokinetic parameters were obtained.
The pharmacokinetic parameters AUC(0-∞), T(lag), Cmax and K21 of both rhein and chrysophanol were markedly different in the acute blood stasis model rabbits. It was also found that parameters A, β, MRT and T(1/2β) of rhein and the parameters α and T1/2α of chrysophanol all exhibited significant difference between the normal and acute blood stasis model rabbits.
The absorption time of rhein and chrysophanol was accelerated and the absorption amount of these two compounds was increased in rabbits with acute blood stasis, suggesting that rhein and chrysophanol would possibly be the two effective compounds in QYQRG.
祛瘀清热颗粒（QYQRG）是治疗血瘀证的一种有效的传统中药复方制剂。比较正常和血瘀证家兔体内QYQRG中化合物的药代动力学特性差异可提供许多有用信息。本研究的主要目的是比较正常家兔和急性血瘀模型家兔口服2.0 g/kg体重的QYQRG后大黄酸和大黄酚的药代动力学。
口服QYQRG后，于5、10、15、20、30、45、60、75、90、120、240、360和480分钟采集血样。采用高效液相色谱法测定家兔血浆中大黄酸和大黄酚的浓度，并获得主要药代动力学参数。
急性血瘀模型家兔中大黄酸和大黄酚的药代动力学参数AUC(0-∞)、T(lag)、Cmax和K21均有显著差异。还发现正常家兔和急性血瘀模型家兔之间，大黄酸的参数A、β、MRT和T(1/2β)以及大黄酚的参数α和T1/2α均有显著差异。
急性血瘀家兔中大黄酸和大黄酚的吸收时间加快，这两种化合物的吸收量增加，提示大黄酸和大黄酚可能是QYQRG中的两种有效成分。
