论文部分内容阅读
目的用超高效液相色谱-质谱联用技术(UPLC-MS/MS)研究大鼠ig 给药桦木酸的血浆药动学。方法大鼠颈静脉插管后ig 给予250 mg/kg 的桦木酸棉籽油悬浊液(100 mg/mL),于给药前和给药后0.08、0.17、0.33、0.5、1、2、4、6、8、12、24 和48 h 时取血,血液样品经醋酸乙酯提取,对甲苯磺酰异氰酸酯(PTSI)柱前衍生化后,采用UPLC-MS/MS 法测定大鼠血浆中桦木酸的量。结果桦木酸以 250 mg/kg 剂量大鼠ig 给药以后,桦木酸在(1.2±0.4)h 达到最大血药浓度值(158.5±26.8)ng/mL,24 h 后基本检测不到。药时曲线下面积AUC0-24 和AUC0-∞分别为(292.41±100.6)ng·h/mL 和(331.45±113.3)ng·h/mL,半衰期(t1/2)和平均滞留时间(MRT)分别为(3.8±1.4)h 和(4.8±2.1)h。结论 UPLC-MS/MS 方法可成功用于经口给药桦木酸大鼠血浆药动学研究,桦木酸的口服吸收极差。
OBJECTIVE To study plasma pharmacokinetics of ig administration of betulinic acid in rats by ultra performance liquid chromatography-mass spectrometry (UPLC-MS / MS). Methods After the jugular vein was cannulated in rats, 250 mg / kg of betulinic acid cottonseed oil suspension (100 mg / mL) was given before and 0.08,0.17,0.33,0.5,1,2,4 , Blood samples were taken at 6, 8, 12, 24 and 48 h. The blood samples were extracted with ethyl acetate, and the PTSI column was derivatized with UPLC-MS / MS. The amount of acid. Results Betulinic acid reached the maximum plasma concentration of (158.5 ± 26.8) ng / mL at (1.2 ± 0.4) h after administration of betulinic acid at a dose of 250 mg / kg, and was undetectable after 24 h. The area under the curve of AUC0-24 and AUC0-∞ were 292.41 ± 100.6 ng · h / mL and 331.45 ± 113.3 ng · h / mL, respectively. The half-life (t1 / 2) and mean residence time (3.8 ± 1.4) h and (4.8 ± 2.1) h. Conclusion The UPLC-MS / MS method can be successfully applied to the plasma pharmacokinetics of betulinic acid in rats. The orally absorbed betulinic acid is very poor.