刺五加叶黄酮脂质体和滴丸的药动学差异比较

采用液质联用(LC-MS/MS)方法,分析刺五加叶黄酮脂质体、刺五加叶滴丸和刺五加叶黄酮提取物经大鼠灌胃给药后其主要成分金丝桃苷的药代动力学和生物利用度,考察刺五加叶黄酮的适宜剂型。用PKsolver软件进行药代动力学数据处理,大鼠灌胃刺五加叶黄酮提取物、刺五加叶滴丸和刺五加叶黄酮脂质体后测得金丝桃苷的最大血药浓度(C_(max))分别为(210.24±10.3)、(254.12±9.2)、(349.34±12.5)μg/L;0~t时间内药时曲线面积(AUC_(0-t))分别为(30.7±2.7)、(35.01±1.98)、(45.2±2.8)μg/(m L·min);平均驻留时间(MRT)分别为(334.42±75.36)、(394.56±90.26)和(640.35±84.26)min。结果表明,刺五加叶黄酮脂质体血药达峰浓度增加,清除速率降低,药时曲线下面积加大,生物利用度显著提高,脂质体有望成为刺五加叶黄酮的适宜剂型。

Comparison of the Pharmacokinetics Difference Between Acanthopanax Leaf Flavonoids Liposome and Acanthopanax Leaf Drop Pills

Acanthopanax leaf flavonoids liposome, acanthopanax leaf drop pills, and acanthopanax leaf flavonoid extract were fed to rats by intragastric administration to study the bioavailability and pharmacokinetics of hyperoside, and appropriate dosage form of acanthopanax leaf flavonoid by liquid chromatography-tandem mass spectrometry(LC-MS/MS). Pharmacokinetic data were processed with PKsolver software. The main pharmacokinetic parameters maximum plasma concentrations(C_max) are (210.24±10.3), (254.12±9.2), and (349.34±12.5) μg/L for acanthopanax leaf flavonoids liposome, acanthopanax leaf drop pills and acanthopanax leaf flavonoid extract, respectively; area under the curve from zero to t(AUC_0-t) is (30.7±2.7), (35.01±1.98), and (45.2±2.8) μg/(mL·min), respectively; mean retention time(MRT) is (334.42±75.36), (394.56±90.26), and (640.35±84.26) min, respectively. The results show that compared with acanthopanax leaf flavonoids extracts and acanthopanax leaf drop pills, the C_max and bioavailability of acanthopanax leaf flavonoids liposome are increased, the elimination rate of acanthopanax leaf flavonoids liposome is reduced. Liposome is expected to be the suitable dosage form of acanthopanax leaf flavonoids, and may become the new research direction in the field of chinese medicine chemistry.