LC-MS/MS法测定布洛芬颗粒剂的人体生物等效性研究

摘要

目的 研究布洛芬颗粒在健康人体内的药动学及其生物利用度,以评价其与布洛芬混悬液的生物等效性.方法 23例健康男性志愿受试者,采用随机、开放、单剂量、双周期自身交叉试验设计.分别口服布洛芬颗粒(受试制剂)与布洛芬混悬液(参比制剂)后,采用液相色谱-串联质谱(LC-MS/MS)法测定血浆中布洛芬的药物浓度.结果 受试制剂与参比制剂的Cmax分别为(17.438 6±5.304 0)、(18.557 7±4.641 7) mg/L,AUC0-24分别为(59.000 3±13.935 3)、(58.506 4±16.720 2) mg/(h·L),AUC0-∞分别为(59.718 0±14.020 0)、(59.227 8±16.815 8) mg/(h·L),Tmax分别为(1.478 3±0.922 9)、(1.021 7±0.822 0) h.结论 空腹口服布洛芬颗粒受试制剂与参比制剂具有生物等效性.%Objective To study the pharmacokinetics and bioavailability of ibuprofen granules in healthy volunteers in order to compare its bioequivalence with ibuprofen suspension.Methods Totally 23 healthy male volunteers were tested by random,open,single dose and double cycle self crossover design.The drug concentrations of plasma were determined by liquid chromatography tandem mass spectrometry (LC-MS/MS) method after oral administration of ibuprofen granules (test preparation) and ibuprofen suspension (reference preparation).Results The Cmax of test preparation and reference preparation was (17.438 6±5.304 0) and (18.557 7±4.641 7) mg/L respectively;AUC0-24 was (59.000 3±13.935 3) and (58.506 4±16.720 2) mg/(h·L);AUC0-∞ was (59.718 0±14.020 0) and (59.227 8±16.815 8) mg/(h·L);Tmax was (1.478 3±0.922 9) and (1.021 7±0.822 0) h.Conclusion The oral administration of ibuprofen granules has biological equivalence for the test preparation and reference preparation.