Faculty of Pharmacy, School of Medicine, Xi'an Jiaotong University, Xi'an 710061, China.
J Ethnopharmacol. 2013 Jan 9;145(1):25-31. doi: 10.1016/j.jep.2012.10.028. Epub 2012 Nov 6.
Libanotis buchtormensis is the source of an important traditional medicine from Shaanxi province of China used in the treatment of many illnesses. Libanotis buchtormensis supercritical extract (LBSE) has analgesic, sedative and anti-inflammatory qualities. Osthole is one of the major bioactive components of LBSE; it is known for its significant anti-tumor, analgesic, and anti-inflammatory properties, it also alleviates hyperglycemia.
The purpose of the present study was to compare the pharmacokinetics and tissue distribution of osthole in Sprague-Dawley (SD) rats after oral administration of pure osthole and LBSE. The two preparations were administered at the same osthole dose (approximately 130 mg/kg). The results should provide some guidance for the clinical applications of Libanotis buchtormensis.
Comparative pharmacokinetics and tissue distribution of osthole in SD rats after oral administration of pure osthole and LBSE were analyzed using reversed-phase high-performance liquid chromatography (RP-HPLC). All pharmacokinetic data were analyzed using 3P97 software. Samples of blood and internal organs (heart, liver, spleen, lungs and kidney) were collected and pretreated according to the experimental schedule. After pretreatment, plasma and tissue samples were extracted using ether-ethyl acetate mixture (3:1, v/v). The concentration of osthole in the plasma and tissues were determined using the RP-HPLC method.
The procedure described in this paper shows good precision and stability and is suitable for the osthole assays in biological samples. We found that the average plasma concentration-time profile of osthole after oral administration of osthole and LBSE showed a single peak. There were also clear differences between plasma concentrations of osthole after oral administration of pure osthole and LBSE. Non-osthole ingredients in LBSE showed some pharmacokinetic interactions with osthole and hence decreased its absorption levels (p<0.05). Our results show different tissue distribution of osthole in the single and composite administration regimens.
This study compares the pharmacokinetic characteristics and tissue distribution of osthole in rats after oral administration of pure osthole and LBSE; the results might be useful in clinical application of this traditional Chinese herbal medicine.
滨蒿是中国陕西省一种重要传统药物的来源，用于治疗多种疾病。滨蒿超临界提取物（LBSE）具有镇痛、镇静和抗炎作用。蛇床子素是 LBSE 的主要生物活性成分之一；它以其显著的抗肿瘤、镇痛和抗炎特性而闻名，还能缓解高血糖。
本研究旨在比较口服纯蛇床子素和 LBSE 后蛇床子素在 SD 大鼠体内的药代动力学和组织分布。两种制剂以相同的蛇床子素剂量（约 130mg/kg）给药。该结果应为滨蒿的临床应用提供一些指导。
采用反相高效液相色谱法（RP-HPLC）分析 SD 大鼠口服纯蛇床子素和 LBSE 后蛇床子素的比较药代动力学和组织分布。所有药代动力学数据均采用 3P97 软件进行分析。根据实验方案采集血液和内脏（心、肝、脾、肺和肾）样本并进行预处理。预处理后，采用乙醚-乙酸乙酯混合液（3:1，v/v）提取血浆和组织样品。采用 RP-HPLC 法测定血浆和组织中蛇床子素的浓度。
本文所述方法具有良好的精密度和稳定性，适用于生物样品中蛇床子素的测定。我们发现，口服蛇床子素和 LBSE 后蛇床子素的平均血浆浓度-时间曲线呈单峰。口服纯蛇床子素和 LBSE 后蛇床子素的血浆浓度也有明显差异。LBSE 中的非蛇床子素成分与蛇床子素表现出一些药代动力学相互作用，从而降低其吸收水平（p<0.05）。我们的结果显示，蛇床子素在单次和复合给药方案中的组织分布不同。
本研究比较了口服纯蛇床子素和 LBSE 后大鼠体内蛇床子素的药代动力学特征和组织分布，研究结果可能对该中药的临床应用有用。
