盐酸吡格列酮片的血药浓度测定及其健康人体内的药动学研究  

Determination of Pioglitazone in Human Plasma by HPLC and Study on its Pharmacokinetics

作　　者：于翠霞[1] 樊宏伟[1] 朱余兵[1] 邹健军[1] 胡云芳[1] 

机构地区：[1]南京医科大学附属南京第一医院国家药品临床研究基地,南京210006

出　　处：《中国药师》2010年第4期480-482,共3页China Pharmacist

摘　　要：目的:测定人血浆中盐酸吡格列酮片的血药浓度并研究其在健康人体内的药物动力学。方法:健康受试者单次(15mg,30 mg)或多次(15 mg,qd,连续服药6 d)口服盐酸吡咯列酮片,用HPLC法测定血浆中的吡咯列酮浓度,DAS2.0计算药动学参数。结果:15 mg单剂量给药的主要药物动力学参数:t_(1/2)=(8.02±1.16)h;t_(max)=(2.24±0.56)h,C_(max)=(0.82±0.13)mg·L^(-1),V/F=(21.72±6.14)L,CL/F=(1.84±0.29)L·h^(-1),AUC_((0-36))=(7.99±1.34)mg·L^(-1)·h,MRT_((0-36))=(9.73±1.01)h。30 mg单剂量给药的主要药物动力学参数:t_(1/2)=(7.81±1.03)h;t_(max)=(2.42±0.63)h,C_(max)=(1.12±0.45)mg·L^(-1),V/F=(33.19±12.26)L,CL/F=(2.92±0.87)L·h^(-1),AUC_((0-36))=(10.85±3.97)mg·L^(-1)·h,MRT_((0-36))=(10.10±0.91)h。多剂量给药的主要药物动力学参数:t_(max)=(2.36±0.69)h,C_(max)=(0.95±0.10)mg·L^(-1),V/F=(21.76±8.52)L,AUC_((0-36))=(8.29±1.87)mg·L^(-1)·h,MRT_((0-36))=(9.58±0.99)h。多次口服给药4 d后,吡格列酮血药浓度达稳态,C_(av)=(0.31±0.07)mg·L^(-1),DF=2.88±0.85,AUC_(55)=(7.50±1.66)mg·L^(-1)·h。结论:口服盐酸吡格列酮片吸收达峰速度较快,消除较慢,且与给药量无关。Objective： To determination the concentration and pharmacokineties of pioglitazone hydroebloride tablets in Chinese healthy volunteers. Method： The single does design was used,the volunteers were received a single does of 15 mg or 30 mg pioglita- zone. In the multiple does design ,the volunteers were received 15 mg pioglitazone one time a day for six consecutive days. The plasma samples were assayed by HPLC and the pharmaeokiuetics were calculated by DAS 2. 0. Result： The pharmacokinetie parameters were obtained as follows ： the single does of 15 nag： tmax was （ 8.02±1.16） h, tmax was （2.24 ± 0. 56） h, Cmax was （0.82 ±0. 13 ） rag. L - ~, V/F was （21.72 _± 6.14） L, CL/F was （ 1.84 ± 0. 29 ） L- h-1, AUC（o_36） was （7.99 ± 1.34） mg. h. L-1, MRT（0_36） was （ 9. 73 ± 1.01） h. The single does of 30 mg：t1/2 was （7.81 ±1.03） h;tmax was （2.42 ±0.63） h,Cmax was （1.12 ±0.45） mg.L-1V/F was （33.19 ± 12.26） L,CL/F was （2. 92 ±0. 87） L.h-1 ,AUCmax was （ 10. 85 ± 3.97） mg.L-1 -h,MRT（0-36） was （ 10. 10 ±0. 91） h. The multiple does：tmax was （2. 36 ±0. 69） h,Cmax was （0. 95 ±0. 10） mg.L-1 ,V/F was （21.76 ± 8. 52） L,AUC（0.36） was （8.29 ± 1.87） mg-L-1.h,MRT（0.36） was （9. 58 ±0. 99） h. The multi-does pharmacokinetic parameters of pioglitazone were obtained as follows ： Cav was （0. 31 ±0. 07） mg.L -1 ,DF was 2. 88 ±0. 85 ,AUC,s was （7. 50 ± 1.66 ） mg.L -1 -h. Conclusion： The pharmaeokinetic parameters of pioglitazone of simple does and multiple does have not significent differences.

关 键 词：吡咯列酮 药物动力学 HPLC 

分 类 号：R969.1[医药卫生—药理学]