论文部分内容阅读
利用手性高效液相色谱法研究大鼠注射及口服布洛芬精氨酸之后布洛芬对映体的药代动力学。布洛芬精氨酸注射及口服给药后,布洛芬对映体的药代动力学呈现立体选择性,且口服给药后立体选择性程度更高。与系统前转化相比,R-布洛芬至S-布洛芬的系统转化在口服给药后立体选择性药代动力学中起更重要的作用。布洛芬精氨酸口服给药后,优势对映体S-布洛芬迅速吸收,S-布洛芬与R-布洛芬的绝对生物利用度分别为100%和80%。基于研究发现的S-布洛芬体内系统性暴露,可以推断布洛芬精氨酸注射及口服给药后的药理作用相似,仅在作用的起始阶段存在差异。
Pharmacokinetics of ibuprofen enantiomers in rats injected with ibuprofen arginine by chiral high performance liquid chromatography. After ibuprofen arginine injection and oral administration, the pharmacokinetics of the ibuprofen enantiomer showed stereoselectivity, and the degree of stereoselectivity after oral administration was higher. Systemic transformation of R-ibuprofen to S-ibuprofen plays a more important role in stereoselective pharmacokinetics after oral administration compared to pre-systemic conversion. After oral administration of ibuprofen arginine, the dominant enantiomer S-ibuprofen was rapidly absorbed and the absolute bioavailabilities of S-ibuprofen and R-ibuprofen were 100% and 80%, respectively. Based on the systemic systemic exposure of S-ibuprofen found in the study, one can infer that the pharmacological effects after ibuprofen arginine injection and oral administration are similar, with differences only in the initial stages of action.