Pharmacokinetics, tissue distribution and excretion of five rhubarb anthraquinones in rats after oral administration of effective fraction of anthraquinones from rheum officinale
Creators: name: Zhao, Di
name: Feng, Su-Xiang
name: Zhang, Hao-Jie
name: Zhang, Na
name: Liu, Xue-Fang
name: Wan, Yan
name: Zhou, Yu-Xiao
name: Li, Jian-Sheng
Publisher: name: Taylor & Francis
Year: 2021
Subjects: subject: Biochemistry
subject: Cell Biology
subject: Genetics
subject: FOS: Biological sciences
subject: Pharmacology
subject: Chemical Sciences not elsewhere classified
subject: Mathematical Sciences not elsewhere classified
subject: Inorganic Chemistry
subject: FOS: Chemical sciences

description: Rhubarb, a famous traditional Chinese medicine, shows a wide range of physiological activities and pharmacological benefits. Rhubarb anthraquinones are perceived as the pharmacologically active compounds of Rhubarb, and understanding metabolism of them is crucial to assure safety and effectiveness of clinical application. In this study, the pharmacokinetics, tissue distribution and excretion of five rhubarb anthraquinones (aloe-emodin, rhein, emodin, chrysophanol, physcion) were systematically investigated after oral administration of rhubarb extract to rats.An HPLC method was developed and validated for quantitation of five rhubarb anthraquinones in rat plasma, tissues, urine and faeces to investigate the Pharmacokinetic characteristics. The results showed that the proposed method was suitable for the quantification of five anthraquinones in plasma, tissue and excreta samples with satisfactory linear (<i>r</i> &gt; 0.99), precision (&lt;10%) and recovery (85.12–104.20%). The plasma concentration profiles showed a quick absorption with the mean <i>T</i><sub>max</sub> of 0.42–0.75 h and t<sub>1/2</sub> of 6.60–15.11 h for five anthraquinones. The analytes were widely distributed in most of the tissues. Approximately 0.13–10.59% and 28.47–81.14% of five anthraquinones were recovered in urine and faeces within 132 h post-dosing, which indicated the major elimination route was faeces excretion.In summary, this study lays a foundation for elucidating the pharmacokinetic rule of rhubarb anthraquinone and the important data can provide reliable scientific resource for further research. Rhubarb, a famous traditional Chinese medicine, shows a wide range of physiological activities and pharmacological benefits. Rhubarb anthraquinones are perceived as the pharmacologically active compounds of Rhubarb, and understanding metabolism of them is crucial to assure safety and effectiveness of clinical application. In this study, the pharmacokinetics, tissue distribution and excretion of five rhubarb anthraquinones (aloe-emodin, rhein, emodin, chrysophanol, physcion) were systematically investigated after oral administration of rhubarb extract to rats. An HPLC method was developed and validated for quantitation of five rhubarb anthraquinones in rat plasma, tissues, urine and faeces to investigate the Pharmacokinetic characteristics. The results showed that the proposed method was suitable for the quantification of five anthraquinones in plasma, tissue and excreta samples with satisfactory linear (<i>r</i> &gt; 0.99), precision (&lt;10%) and recovery (85.12–104.20%). The plasma concentration profiles showed a quick absorption with the mean <i>T</i><sub>max</sub> of 0.42–0.75 h and t<sub>1/2</sub> of 6.60–15.11 h for five anthraquinones. The analytes were widely distributed in most of the tissues. Approximately 0.13–10.59% and 28.47–81.14% of five anthraquinones were recovered in urine and faeces within 132 h post-dosing, which indicated the major elimination route was faeces excretion. In summary, this study lays a foundation for elucidating the pharmacokinetic rule of rhubarb anthraquinone and the important data can provide reliable scientific resource for further research.