口服布洛芬丁香酚酯微乳在大鼠体内药动学研究

Study on Pharmacokinetics of Oral Ibuprofen Eugenol Ester Microemulsion in Rats

目的研究布洛芬丁香酚酯微乳剂的抗溃疡作用及其在大鼠体内的药动学。方法采用显微镜法考察布洛芬丁香酚酯微乳的抗溃疡作用。大鼠口服给药后,分别于0.5,1,2,3,4,5,6,8,10和12h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明显降低小鼠溃疡的发生率。布洛芬丁香酚酯微乳及布洛芬溶液组口服后的AUC0-12分别为(270.31±58.32)和(155.07±39.77)mg.h.L-1,ρmax分别为(64.6±10.34)和(39.94±9.72)mg.L-1,tmax均为1h。MRT0-12分别为(3.69±0.06)和(3.62±0.54)h。结论布洛芬丁香酚酯微乳能降低由布洛芬引起的胃溃疡的发生率,口服给药后可以提高布洛芬的生物利用度。

OBJECTIVE To investigate the pharmacokinetics of ibuprofen eugenol ester microemulsion（IEE-ME） in rats.METHODS The protective effect of IEE-ME and ibuprofen on ulcer was assessed pathologically in mice.Following the oral administration of IEE-ME or ibuprofen solution into rats,the blood samples were collected at 0.5,1,2,3,4,5,6,8,10 and 12 h and the plasma ibuprofen concentration was then quantified by HPLC.RESULTS The IEE-ME decreased the ulcerogenic percent obviously.The pharmacokintic parameters of the IEE-IEE and the solution were followed as：AUC0-12 were（270.31±58.32） and（55.07±39.77） mg·h·L^-1,ρmax（64.6±10.34） and（39.94±9.72） mg·L^-1,tmax 1 and 1 h,MRT0-12（3.69±0.06） and（3.62±0.54）h,respectively.CONCLUSION IEE-ME can decrease ulcerogenic probability induced by ibuprofen,and enhance the bioavailability of ibuprofen after oral IEE-ME.