Premium
Effect of Wuzhi Tablet ( Schisandra sphenanthera extract ) on the Pharmacokinetics of Cyclosporin A in Rats
Author(s) -
Xue Xinping,
Qin Xiaoling,
Xu Chenshu,
Zhong Guoping,
Wang Ying,
Huang Min,
Bi Huichang
Publication year - 2013
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.4849
Subject(s) - pharmacokinetics , pharmacology , cyp3a , schisandra , oral administration , chemistry , pharmacokinetic interaction , medicine , drug interaction , traditional medicine , metabolism , cytochrome p450 , biochemistry , alternative medicine , traditional chinese medicine , pathology
In our previous reports, Wuzhi tablet (an herbal preparation of ethanol extract of Wuweizi ( Schisandra sphenanthera )) can significantly increase the blood concentration of tacrolimus and paclitaxel in rats by inhibiting the CYP3A‐mediated metabolism and the P‐gp‐mediated efflux. Cyclosporin A (CsA), a well‐known immunosuppressant agent, is also a substrate of CYP3A and P‐gp. Therefore, this study aimed to investigate whether and how WZ affects pharmacokinetics of CsA in rats. The AUC 0–48h and C max of CsA were increased by 40.1% and 13.1%, respectively, with a single oral co‐administration of WZ and high dose of CsA (37.8 mg/kg). Interestingly, after a single oral co‐administration of WZ and low dose of CsA (1.89 mg/kg), the AUC 0–36 h and C max of CsA were dramatically increased by 293.1% (from 1103.2 ± 293.0 to 4336.5 ± 1728.3 ng.h/mL; p < 0.05) and 84.1% (from 208.5 ± 67.9 to 383.1 ± 92.5 ng/mL; p < 0.05), respectively. The CL/F was decreased from 1.7 L/h/kg to 0.5 L/h/kg. Thus, the effect of WZ on high dose of CsA was not significant, but pharmacokinetic parameters of CsA at low dose were significantly influenced by co‐administration of WZ. The herb–drug interaction should be taken into consideration at this situation. Copyright © 2012 John Wiley & Sons, Ltd.