School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Box 51, 103 Wenhua Road, Shenyang 110016, China.
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
J Ethnopharmacol. 2014 Sep 29;155(3):1568-74. doi: 10.1016/j.jep.2014.07.052. Epub 2014 Aug 4.
Magnolia officinalis is one of the commonly used in traditional Chinese medicine for the treatment of fever, chronic bronchitis and stomach ailments. Magnolol and honokiol are isomers with hydroxylated biphenol compound in the extract of Magnolia officinalis. This study aims to determine the isomers in rat plasma and evaluate their pharmacokinetic pattern after administration emulsion.
Sprague Dawley male rats received either an intravenous (i.v.25, mg/kg) or oral (50mg/kg) dose of the emulsion of the isomer. A sensitive and specific ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) method was developed for the investigation of the pharmacokinetics of magnolol and honokiol in rats. Kaempferol was employed as an internal standard.
The plasma samples were deproteinized with acetonitrile, the post-treatment samples were analyzed on an Agela C18 column interfaced with a triple quadrupole tandem mass spectrometer in negative electrospray ionization mode. Acetonitrile and 5 mmol/L ammonium acetate buffer solution (65: 35, v/v) was used as the mobile phase at a flow rate of 0.2 mL/min. Following oral administration of emulsion to rats, magnolol attained mean peak plasma concentrations of 426.4 ± 273.8 ng/mL at 1.20 h, whereas honokiol reached peak plasma concentrations of 40.3 ± 30.8 ng/mL at 0.45 h. The absolute bioavailability of magnolol and honokiol is 17.5 ± 9.7% and 5.3 ± 11.7%. By comparison, the AUC0-∞ of magnolol was 5.4 times higher than that of honokiol after intravenous administration, but AUC0-∞ of magnolol was about 18-fold higher than honokiol after oral administration.
厚朴是一种常用于传统中药治疗发热、慢性支气管炎和胃病的药物。厚朴酚和和厚朴酚是厚朴提取物中具有羟基化联苯化合物的同分异构体。本研究旨在确定大鼠血浆中的同分异构体，并评估其在乳液给药后的药代动力学模式。
雄性 Sprague Dawley 大鼠分别静脉内（i.v.25，mg/kg）或口服（50mg/kg）给予该同分异构体乳液。建立了一种灵敏且特异的超高效液相色谱/串联质谱（UPLC-MS/MS）方法，用于研究大鼠中厚朴酚和和厚朴酚的药代动力学。山柰酚被用作内标。
血浆样品用乙腈沉淀蛋白，经处理后的样品在 Agela C18 柱上分析，与三重四极杆串联质谱仪在负离子电喷雾模式下联用。乙腈和 5mmol/L 乙酸铵缓冲液（65:35，v/v）以 0.2mL/min 的流速作为流动相。大鼠口服乳液后，厚朴酚的平均达峰血浆浓度为 1.20 小时时 426.4±273.8ng/mL，而和厚朴酚在 0.45 小时时达到峰值血浆浓度 40.3±30.8ng/mL。厚朴酚和和厚朴酚的绝对生物利用度分别为 17.5±9.7%和 5.3±11.7%。相比之下，静脉注射后厚朴酚的 AUC0-∞是和厚朴酚的 5.4 倍，但口服给药后厚朴酚的 AUC0-∞是和厚朴酚的约 18 倍。
