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目的:探讨姜黄素纳米混悬剂在大鼠体内的药代动力学过程。方法:将同等剂量的姜黄素原料药与姜黄素纳米混悬剂分别灌胃给2组大鼠,于灌胃后20,40 min和1,2,4,6,8,12,24 h眼底静脉丛取血,采用HPLC测定血浆姜黄素含量,Xterra C18色谱柱(4.6 mm×250 mm,5μm),C18预柱(4.0 mm×2.0 mm),柱温35℃,流动相甲醇-1%乙酸水溶液(78∶22),流速1.0 mL·min-1,进样量20μL,计算姜黄素最低定量限,同时测定血浆中姜黄素原料药与姜黄素纳米混悬剂的药代动力学参数。结果:血浆中姜黄素的定量限15μg·L-1(S/N>10),低、中、高质量浓度的提取回收率(x珋±s,n=5)分别为(91.3±5.7)%,(93.0±4.1)%,(93.3±5.2)%。姜黄素纳米混悬剂的C max和AUC均显著高于姜黄素原料,C max分别为(863.1±390.4),(91.8±22.9)μg·L-1;原料药和混悬剂的T max分别为(4.4±2.2),(4.8±4.4)h,t1/2分别为(4.6±3.2),(5.4±3.7)h,均无显著性变化。结论:建立的HPLC分析条件稳定可靠,纳米混悬剂能明显促进姜黄素的吸收,提高其生物利用度,但吸收和代谢速度无明显差异。
Objective: To investigate the pharmacokinetics of curcumin nanosuspension in rats. Methods: The same dose of curcumin drug material and curcumin nanosuspension were administered to two groups of rats, respectively, at 20,40 and 1, 2, 4, 6, 8, 12 and 24 h after intragastric administration Blood samples were obtained from the venous plexuses by HPLC. The concentration of curcumin was determined by HPLC on a Xterra C18 column (4.6 mm × 250 mm, 5 μm), C18 (4.0 mm × 2.0 mm), column temperature 35 ℃, mobile phase methanol-1% acetic acid (78:22). The flow rate was 1.0 mL · min-1. The injection volume was 20 μL. The minimum quantitative limit of curcumin was calculated. The pharmacokinetic parameters of curcumin and curcumin nanosuspension were also determined. Results: The quantitative recovery of curcumin in plasma was 15μg · L-1 (S / N> 10), and the recoveries of low, middle and high concentration were (91.3 ± 5.7) %, (93.0 ± 4.1)%, (93.3 ± 5.2)%. The C max and AUC of curcumin nanosuspensions were significantly higher than those of curcumin, with C max of (863.1 ± 390.4) and (91.8 ± 22.9) μg · L -1, respectively (4.4 ± 2.2), (4.8 ± 4.4) h, t1 / 2 were (4.6 ± 3.2), (5.4 ± 3.7) h, no significant changes. CONCLUSION: The established HPLC analysis conditions are stable and reliable. The nanosuspension can obviously promote the absorption of curcumin and increase its bioavailability, but the absorption and metabolism speed have no obvious difference.