[关键词]
[摘要]
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。
[Key word]
[Abstract]
Objective The pharmacokinetic study of betulinic acid in rat plasma after oral administration of betulinic acid was studied by UPLC-MS/MS. Methods The rats were orally administered with betulinic acid (100 mg/mL suspended in cottonseed oil) at the dose of 250 mg/kg after taken jugular vein cannulation. The blood samples were collected before administration and 0.08 h, 0.17 h, 0.33 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 24 h and 48 h after administration. The plasma sample was extracted with ethyl acetate and derivatized with p-toluenesulfonylisocyanate (PTSI), and the concentration of betulinic acid was determined using UPLC-MS/MS. Results After oral dosing, betulinic acid reached the maximum concentration of (158.5 ± 26.8) ng/mL at (1.2 ± 0.4) h, and could not be detectable after 24 h. AUC0-24 and AUC0-∞were (292.41 ± 100.6) and (331.45 ± 113.3) ng·h/mL, respectively. t1/2 and MRT were (3.8 ± 1.4) and (4.8 ± 2.1) h, respectively. Conclusion The UPLC-MS/MS method is successfully applied to the pharmacokinetic study of betulinic acid in rat plasma. The absorption of betulinic acid is extremely low.
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[基金项目]
黑龙江省自然科学基金项目(C201101);黑龙江中医药大学优秀创新人才支持计划