Xing Han, Zhu Xiaojie, Liao Jianmin, Kong Ying, Lu Yayuan, Zhao Di, Li Ning, Chen Xijing, Qin Zhiying
Department of Pharmacy, First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.
Henan Key Laboratory of Precision Clinical Pharmacy, Zhengzhou University, Zhengzhou, China.
Front Pharmacol. 2023 Mar 2;14:1109084. doi: 10.3389/fphar.2023.1109084. eCollection 2023.
egg polysaccharide (SEP) extracted from sea urchins has potential anticancer activity. However, little is known about its pharmacokinetic properties. To investigate the pharmacokinetics of SEP, it was radiolabeled with tritium. Furthermore, a sensitive, selective, and rapid liquid scintillation counter (LSC) method for quantifying H-SEP in biological matrix was validated. The lower quantification limit of the method was 4 Bq. The relative standard deviations (RSDs) of the intra- and inter-day precision were <3.0% and <3.9%, respectively. H-SEP was successfully applied to investigate the pharmacokinetics of SEP after intravenous administration of 20, 40, and 80 mg/kg (40 μCi/kg) in rats and 5, 10, and 20 mg/kg (6 μCi/kg) in beagles. The AUC of SEP at three different doses was 487.81 ± 39.99 mg/Lh, 1,003.10 ± 95.94 mg/Lh, and 2,188.84 ± 137.73 mg/Lh in rats and 144.12 ± 3.78 mg/Lh, 322.62 ± 28.03 mg/Lh, and 754.17 ± 37.79 mg/Lh in beagles. The terminal elimination half-life (t) of SEP was longer in beagles (204.29 ± 139.34 h) than in rats (35.48 ± 6.04 h). The concentration of SEP in plasma declined rapidly in both rats and beagles. All the study results provide detailed pharmacokinetic profiles of SEP in two kinds of animals, which will be helpful for further development.
从海胆中提取的卵多糖（SEP）具有潜在的抗癌活性。然而，对其药代动力学性质知之甚少。为了研究SEP的药代动力学，用氚对其进行放射性标记。此外，还验证了一种用于定量生物基质中H-SEP的灵敏、选择性和快速的液体闪烁计数器（LSC）方法。该方法的最低定量限为4 Bq。日内和日间精密度的相对标准偏差（RSD）分别<3.0%和<3.9%。H-SEP成功应用于研究大鼠静脉注射20、40和80 mg/kg（40 μCi/kg）以及比格犬静脉注射5、10和20 mg/kg（6 μCi/kg）后SEP的药代动力学。SEP在三种不同剂量下的AUC在大鼠中分别为487.81±39.99 mg/Lh、1003.10±95.94 mg/Lh和2188.84±137.73 mg/Lh，在比格犬中分别为144.12±3.78 mg/Lh、322.62±28.03 mg/Lh和754.17±37.79 mg/Lh。SEP的末端消除半衰期（t）在比格犬（204.29±139.34 h）中比在大鼠（35.48±6.04 h）中更长。大鼠和比格犬血浆中SEP的浓度均迅速下降。所有研究结果提供了SEP在两种动物中的详细药代动力学特征，这将有助于进一步开发。
