布洛芬丁香酚酯微乳的镇痛作用及大鼠体内药动学研究

Analgesic effect and pharmacokinetics of ibuprofen eugenol ester microemulsion in rats

目的:研究布洛芬丁香酚酯微乳剂的镇痛作用及其在大鼠体内的药动学。方法:采用小鼠热板法考察布洛芬丁香酚酯微乳的镇痛作用。大鼠尾静脉给药后,分别于给药后5,10,25,40 min和1,1.5,2,3,4,5,7和9 h取血。采用高效液相色谱法测定血浆中布洛芬的浓度。结果:布洛芬丁香酚酯微乳可剂量依赖性延长小鼠热板痛阀时间,且效果等同于同剂量布洛芬。布洛芬丁香酚酯微乳及布洛芬溶液组静脉注射后的消除半衰期(t1/2)分别为(6.30±0.56)和(2.79±0.29)h,清除率(CL)分别为(94.93±12.09)和(112.17±7.00)mL.h-1.kg-1,稳态表观分布容积(Vss)分别为(543.62±64.68)和(243.12±6.87)mL.kg-1,两组存在显著性统计学差异(P<0.05)。结论:布洛芬丁香酚酯微乳与布洛芬溶液剂镇痛作用相当,静脉注射后消除时间较布洛芬明显延长。

Objective： To investigate the analgesic effect and pharmacokinetics of ibuprofen eugenol ester microemulsion （IEE-ME） in rats. Methods ： The analgesic effect of IEE-ME was assessed by a hot plate test in mice. Following the intravenous injection of IEE-ME or ibuprofen solution into rats, the blood samples were collected at 5,10,25,40 min and 1,1.5,2,3,4,5,7,9 h and the plasma ibuprofen concentration was then quantified by HPLC. Results： The IEE-ME improved the analgesic effects as well as the ibuprofen solution in a dose-dependent manner. The t1/2, CL and Vss of the IEE-ME and the ibuprofen solution were （6.30 ± 0.56） and （2.79 ± 0.29 ） h, （ 94.93 ± 12. 09 ） and （ 112. 17 ± 7.00 ） mL· h^- 1· kg^ - 1, （543.62 ± 64.68 ） and （ 243.12 ± 6.87 ） mL· kg ^- 1, respectively （ P 〈 0.05 ）. Conclusion ： IEE-ME offered more potent and latent analgesic effects than the ibuprofen solution.