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目的:研究不同吸收促进剂对柠檬苦素在大鼠体内药动学过程的影响,提高柠檬苦素的生物利用度。方法:各组大鼠分别灌胃柠檬苦素和不同的吸收促进剂,与对照组进行比较,采用液质联用仪测定柠檬苦素在大鼠体内的血药浓度。结果:与对照组比较,合用维拉帕米、十二烷基硫酸钠、聚山梨酯-80和冰片后,柠檬苦素的AUC和Cmax均呈增加趋势。其中合用维拉帕米AUC增加9倍(P<0.05),Cmax增加5倍(P<0.05),合用十二烷基硫酸钠、聚山梨酯-80和冰片后,各组AUC增加3倍(P<0.05),Cmax增加2～3倍(P<0.05)。结论:合用吸收促进剂灌胃柠檬苦素后,维拉帕米、十二烷基硫酸钠、聚山梨酯-80和冰片对柠檬苦素的药动学过程有显著性影响,对柠檬苦素的肠吸收均有一定的促吸收效果。
OBJECTIVE: To study the effect of different absorption enhancers on the pharmacokinetics of limonin in rats and to improve the bioavailability of limonin. Methods: The limonin and different absorption enhancers were respectively instilled into the rats in each group, compared with the control group. The plasma concentrations of limonin in rats were determined by LC / MS. Results: Compared with the control group, the combination of verapamil, sodium lauryl sulfate, polysorbate-80 and borneol, limonin AUC and Cmax showed an increasing trend. The AUC of combined verapamil was increased by 9 times (P <0.05) and Cmax increased by 5 times (P <0.05). Combined with sodium lauryl sulfate, polysorbate-80 and borneol, the AUC of each group increased 3 times P <0.05), Cmax increased 2 ~ 3 times (P <0.05). CONCLUSION: Verapamil, sodium lauryl sulfate, polysorbate-80 and borneol have a significant effect on the pharmacokinetics of limonin when combined with limonene, The intestinal absorption have a certain effect of promoting absorption.