Xiao-yan Dai1, Yun-liang Yan2, Qiao-feng Wu3, Chen-huan Yu4, Xin Liu3, Ya-qi Jiang3. 1. Department of Pharmacy, The Third People׳s Hospital of Hangzhou, Hangzhou 310009, China. 2. Zhejiang Chinese Medical University, Hangzhou 310053, China. Electronic address: yylhz123456@sina.com. 3. College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053, China. 4. Experimental Animal Centre, Zhejiang Academy of Medical Sciences, Hangzhou 310013, China.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.
ETHNOPHARMACOLOGICAL RELEVANCE: 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 syndromerabbits 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.
Authors: Mohd Aslam Yusuf; Brahma N Singh; Surya Sudheer; Ravindra N Kharwar; Saba Siddiqui; Ahmed M Abdel-Azeem; Leonardo Fernandes Fraceto; Kavya Dashora; Vijai K Gupta Journal: Biomolecules Date: 2019-02-18