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土木香内酯是藏药土木香中挥发油的主要成分,具有较好的驱虫、抗炎等药理活性。本研究以高效液相色谱(HPLC)方法测定大鼠血浆中的土木香内酯含量,评价静脉和口服给予大鼠土木香内酯的药代动力学特征。研究采用C18柱(4.6 mm×250 mm,5.0μm),以甲醇–水(70:30,v/v)为流动相,流速1.0 m L/min的进行分离,检测波长为239 nm。结果发现土木香内酯在0.08–10μg/m L的浓度范围,具有良好的线性关系(R~2=0.9998),且日内和日间精密度RSD均低于2.27%,血浆中土木香内酯的平均绝对回收率为88.09%–95.57%。静脉给药后,土木香内酯显示了较快的清除(CL=(0.11±0.014)L/h/kg)和较小分布(Vd=(0.71±0.14)L/kg),消除半衰期(t_(1/2))为56.24 min。口服14和28 mg/kg的剂量后,土木香内酯在大鼠中显示了较快的吸收,Tmax分别为(45.02±0.88)min和(45.13±0.39)min。进一步的分析显示,大鼠口服土木香后土木香内酯的生物利用度为50.88%,提示具有土木香药材中土木香内酯具有较好的吸收。
Civil incense lactone is the main component of the essential oil of Tibetan medicine wood, has good deworming, anti-inflammatory and other pharmacological activity. In this study, HPLC was used to determine the content of geraniallactone in rat plasma and the pharmacokinetic characteristics of geranyllactone in rats administered intravenously and orally were evaluated. The separation was performed on a C18 column (4.6 mm × 250 mm, 5.0 μm) with a mobile phase of methanol-water (70:30, v / v) at a flow rate of 1.0 mL / min with a detection wavelength of 239 nm. The results showed that there was a good linearity (R ~ 2 = 0.9998) in the range of 0.08-10μg / m L, and the RSD of intra-day and inter-day precision was less than 2.27% The average absolute recovery was 88.09% -95.57%. Gemcitabine showed faster clearance (CL = (0.11 ± 0.014) L / h / kg and smaller distribution (Vd = 0.71 ± 0.14) L / kg after iv administration and elimination half-life (1/2)) was 56.24 min. Geranyllactone showed a faster absorption in rats after 14 and 28 mg / kg oral doses, with Tmax of (45.02 ± 0.88) min and (45.13 ± 0.39) min, respectively. Further analysis showed that the bioavailability of gentiolanol was 50.88% after oral administration of gentian, indicating that Geosmin had good absorption in gentian herbs.