Comparative pharmacokinetics of active anthraquinones ingredients after oral administration of Rhei Radix et Rhizoma and Niuhuang Jiedu Tablets to rats
10.11665/j.issn.1000-5048.20180410
- VernacularTitle:大黄及牛黄解毒片大鼠给药后血浆中大黄活性成分的药代动力学比较研究
- Author:
Yuexin LIU
1
;
Xiao WU
;
Rong GUAN
;
Taijun HANG
;
Min Taijun
Author Information
1. 中国药科大学药物分析系
- Publication Type:Journal Article
- Keywords:
Rhei Radix et Rhizoma;
Niuhuang Jiedu Tablets;
LC-MS/MS;
pharmacokinetics
- From:
Journal of China Pharmaceutical University
2018;49(4):449-455
- CountryChina
- Language:Chinese
-
Abstract:
The study aims to investigate different pharmacokinetic profilesof anthraquinones after oral administration of Rhei Radix et Rhizoma and Niuhuang Jiedu Tablets(NHJDT)in rats, respectively. Rats were administrated with 96 mg/kg of Rhei Radix et Rhizoma(1. 83 mg/kg of total anthraquinone, equivalent to 0. 28 mg/kg of rhein, 0. 30 mg/kg of emodin, 0. 81 mg/kg of chrysophanol, 0. 23 mg/kg of aloe-emodin and 0. 20 mg/kg of physcion)or 250 mg/kg of NHJDT(equal dose of total anthraquinone as Rhei Radix et Rhizoma, equivalent to 0. 33 mg/kg of rhein, 0. 38 mg/kg of emodin, 0. 71 mg/kg of chrysophanol, 0. 24 mg/kg of aloe-emodin and 0. 17 mg/kg of physcion), respectively. Followed by protein precipitation with methanol, the anthraquinones in plasma samples were determined by LC-MS/MS. The pharmacokinetic parameters were calculated by WinNonlin 7. 0. The cmaxof rhein were(121±103)and(474±251)μg/L, and the AUC0-twere(275±176)and(406±194)μg ·h/L for Rhei Radix et Rhizoma and NHJDT, respectively. The cmaxof chrysophanol isomer were(2 325±1 390)and(3 580±2 169)μg/L, and the AUC0-twere(8 170±2 661)and(8 856±4 023)μg ·h/L, respectively. Emodin in very low levels was only detected in rat plasma samples after oral gavage of NHJDT. The cmax, AUC and t1/2 of rhein, as well as Vd and CL of chrysophanol isomer were observed with a much increased degree in comparison with Rhei Radix et Rhizoma counterparts. However, much shorter tmaxwas found in NHJDT group. Therefore, NHJDT with co-existing components enhanced the absorption and influenced the pharmacokinetic behaviors of active ingredients in Rhei Radix et Rhizoma.
