摘要
目的:建立人血浆中的氯氮平的高效液相色谱-质谱测定方法,用于研究氯氮平口腔崩解片的人体药动学和生物等效性。方法:24名男性健康志愿者随机交叉给药,分别单剂量口服国产的氯氮平口腔崩解片(受试制剂)及氯氮平片(参比制剂),采用高效液相色谱-质普法,电喷雾电离源选择性正离子检测受试者血浆中氯氮平的浓度。用BAPP2.2软件计算药动学参数及相对生物利用度。结果:计算两者主要药动学参数:Cmax分别为(56.8±19.7)μg·L-1和(51.9±10.6)μg·L-1,tmax为(1.9±0.9)h和(1.5±0.5)h,AUC0-24分别为(713±261)h·μg·L-1和(616±132)h·μg·L-1。结论:受试制剂对参比制剂的相对生物利用度为(96.5±36.2)%,两制剂在人体内具有生物等效性。
OBJECTIVE To determine clozapine in human plasma by an HPLC-MS method,and to study the pharmaeokinetics and bioequivalenee of clozapine orally disintegrating tablets in human. METHODS 24 healthy male vol.unteer s were orally administered with a randomized and single crossover dose of elozapine orally disintegrating tablets （ test sample ） and clozapine Tablets （ reference sample ） . The plasma elozapine was quantified by LC-MS （ SIM＋ ） . The pharmacokinetic parameters and relative bioavailability were calculated using BAPP 2. 2. RESULTS The main pharmacokinetic parameters of elozapine test and reference tablets were as follows ： Cmax was （56. 8 ± 19. 7）μg·L^-1 and （51.9 ± 10. 6）μg·L^-1 , t was （ 1.9 ± 0. 9） h and （ 1.5 ± 0. 5）h,AUC0-24 （713 ± 261 ）h·μg·L^-1and（ 616 ± 132） h·μg·L^-1 respectively. CONCLUSION The relative bioavailability of test sample was （96. 5 ± 36.2） % ,The two formulations were bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第19期1644-1648,共5页
Chinese Journal of Hospital Pharmacy
