大鼠口服右旋布洛芬及右旋布洛芬精氨酸盐后右旋布洛芬的药动学  

Pharmacokinetics of Dexibuprofen in Rats after Oral Administration of Dexibuprofen and Dexibuprofen Arginate

作　　者：韩静[1] 张丹[2] 肖雪[2] 张丽娜[2] 王晓琳[2] 刘会臣[1,2] 

机构地区：[1]辽宁医学院航天中心医院研究生培养基地,北京100049 [2]航天中心医院临床药理室,北京100049

出　　处：《中国药学杂志》2012年第17期1396-1399,共4页Chinese Pharmaceutical Journal

摘　　要：目的建立测定大鼠血浆中右旋布洛芬的LC-MS/MS方法,并用于研究大鼠口服右旋布洛芬和右旋布洛芬精氨酸盐后右旋布洛芬的药动学。方法大鼠单次口服右旋布洛芬和右旋布洛芬精氨酸盐,于给药后不同时间采集血样,血浆样本经沉淀蛋白后,以吲哚美辛为内标,LC-MS/MS测定血浆中右旋布洛芬的浓度。结果大鼠口服右旋布洛芬和右旋布洛芬精氨酸盐后右旋布洛芬均迅速吸收;大鼠口服右旋布洛芬精氨酸盐后血浆中右旋布洛芬的AUC,较其口服等剂量右旋布洛芬后的AUC明显增大。结论右旋布洛芬和精氨酸成盐后其生物利用度增加。OBJECTIVE To establish an HPLC-MS/MS method for the determination of dexibuprofen in rat plasma and to study the pharmacokinetic profiles of dexibuprofen in rats after oral administration of dexibuprofen suspention or dexibuprofeu arginate aqueous solution. METHODS Dexibuprofen suspention or dexibuprofen arginate aqueous solution was administered orally as a single dose to rats. Blood was collected at different time points and blood samples were prepared by protein precipitation. The concentration of dexibuprofen in plasma was determined by an HPLC-MS/MS method using indomethacin as internal standard. RESULTS The oral administration of both dexibuprofen suspention and dexibuprofen arginate aqueous solution resulted in rapid absorption of dexibuprofen. The AUC of dexibuprofen after oral administration of dexibuprofen arginate aqueous solution in rats was significantly higher than the AUC of dexibuprofen after administration of dexibuprofen suspention at equivalent dose. CONCLUSION Dexibuprofen will show an enhancement in oral bioavailability in the salt formulation as dexibuprofen arginate.

关 键 词：右旋布洛芬 右旋布洛芬精氨酸盐 药动学 液相色谱-质谱联用 

分 类 号：R969.1[医药卫生—药理学]