Sanguinarine (SA) is a benzo[c] phenanthridine alkaloid which has a variety of pharmacological properties. However, very little was known about the pharmacokinetics of SA and its metabolite dihydrosanguinarine (DHSA) in pigs. The purpose of this work was to study the intestinal metabolism of SA in vitro and in vivo. Reductive metabolite DHSA was detected during incubation of SA with intestinal mucosa microsomes, cytosol, and gut flora. After oral (p.o.) administration of SA, the result showed SA might be reduced to DHSA in pig intestine. After i.m. administration, SA and DHSA rapidly increased to reach their peak concentrations (Cmax , 30.16 ± 5.85, 5.61 ± 0.73 ng/ml, respectively) at 0.25 hr. Both compounds were completely eliminated from the plasma after 24 hr. After single oral administration, SA and DHSA rapidly increased to reach their Cmax (3.41 ± 0.36, 2.41 ± 0.24 ng/ml, respectively) at 2.75 ± 0.27 hr. The half-life (T1/2 ) values were 2.33 ± 0.11 hr and 2.20 ± 0.12 hr for SA and DHSA, respectively. After multiple oral administration, the average steady-state concentrations (Css ) of SA and DHSA were 3.03 ± 0.39 and 1.42 ± 0.20 ng/ml. The accumulation indexes for SA and DHSA were 1.21 and 1.11. The work reported here provides important information on the metabolism sites and pharmacokinetic character of SA. It explains the reasons for low toxicity of SA, which is useful for the evaluation of its performance.

中文翻译：

---

在体外和体内研究血红素碱的代谢和药代动力学。

Sanguinarine（SA）是苯并[c]菲啶生物碱，具有多种药理特性。但是，关于SA及其代谢物二氢血红蛋白（DHSA）在猪中的药代动力学知之甚少。这项工作的目的是研究SA在体外和体内的肠道代谢。在SA与肠粘膜微粒体，细胞溶质和肠道菌群孵育期间检测到还原性代谢物DHSA。口服（po）施用SA后，结果表明SA可能在猪肠中被还原为DHSA。即时给药后，SA和DHSA在0.25小时迅速增加，达到其峰值浓度（分别为Cmax，30.16±5.85、5.61±0.73 ng / ml）。24小时后，两种化合物均从血浆中完全清除。单次口服后 SA和DHSA在2.75±0.27 hr时迅速增加以达到其Cmax（分别为3.41±0.36、2.41±0.24 ng / ml）。SA和DHSA的半衰期（T1 / 2）值分别为2.33±0.11小时和2.20±0.12小时。多次口服后，SA和DHSA的平均稳态浓度（Css）为3.03±0.39和1.42±0.20 ng / ml。SA和DHSA的累积指数分别为1.21和1.11。此处报道的工作提供了有关SA的代谢位点和药代动力学特征的重要信息。它解释了SA低毒的原因，这对于评估其性能很有用。SA和DHSA的平均稳态浓度（Css）为3.03±0.39和1.42±0.20 ng / ml。SA和DHSA的累积指数分别为1.21和1.11。此处报道的工作提供了有关SA的代谢位点和药代动力学特征的重要信息。它解释了SA低毒的原因，这对于评估其性能很有用。SA和DHSA的平均稳态浓度（Css）为3.03±0.39和1.42±0.20 ng / ml。SA和DHSA的累积指数分别为1.21和1.11。此处报道的工作提供了有关SA的代谢位点和药代动力学特征的重要信息。它解释了SA低毒的原因，这对于评估其性能很有用。