Abstract

1. 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.

2. 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 (r > 0.99), precision (<10%) and recovery (85.12–104.20%). The plasma concentration profiles showed a quick absorption with the mean T_max of 0.42–0.75 h and t_1/2 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.

3. 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.

摘要

1. 大黄是一种著名的中药，具有广泛的生理活性和药理作用。大黄蒽醌被认为是大黄的药理活性化合物，了解它们的代谢对于确保临床应用的安全性和有效性至关重要。本研究系统地研究了大鼠口服大黄提取物后5种大黄蒽醌类物质（芦荟大黄素、大黄酸、大黄素、大黄酚、Physcion）的药代动力学、组织分布和排泄。

2. 开发并验证了一种 HPLC 方法，用于对大鼠血浆、组织、尿液和粪便中的五种大黄蒽醌进行定量，以研究其药代动力学特征。结果表明，该方法适用于血浆、组织和排泄物样品中五种蒽醌类化合物的定量分析，线性( r  >0.99)、精密度(<10%)和回收率(85.12-104.20%)均令人满意。血浆浓度曲线显示快速吸收，平均T _max为 0.42–0.75 h 和 t _1/25 种蒽醌的 6.60-15.11 小时。分析物广泛分布在大多数组织中。在给药后 132 小时内，尿液和粪便中回收了约 0.13-10.59% 和 28.47-81.14% 的五种蒽醌，这表明主要消除途径是粪便排泄。

3. 综上所述，本研究为阐明大黄蒽醌的药代动力学规律奠定了基础，重要数据可为进一步研究提供可靠的科学资源。