摘要
目的:研究那格列奈在健康受试者体内的药代动力学特征及生物转化过程中的消旋化。方法:8名健康受试者单剂量口服那格列奈90mg,用RP-HPLC法同时测定血浆和尿液中那格列奈对映体的浓度,矩量法计算药代动力学参数。结果:那格列奈的Cmax为7.51±2.83mg·L-1,tmax为1.25±0.26h,t1/2为1.18±0.33h,AUC（0-24h）为17.97±4.34mg·h·L-1,CL/F（s）为5.30±1.46L·h-1,12h内原型药物排出率为6.23％±0.86％,血浆和尿液中均未见L-异构体。结论:那格列奈在人体内快速吸收和消除,在肝脏生物转换过程中不存在对映体的消旋化。
OBJECTIVE: To study pharmacokinetics of nateglinide and its racemization during biotransformation in 8 Healthy Volunteers. METHODS: each volunteer was orally given 90mg. Drug concentrations in plasma and urine were assayed by RP-HPLC method. Pharmacokinetic parameter were calculated on the basis of noncompartment model. RESULTS: After a single oral dose(90mg),Cmax was 7.51±2.83mg·L-1at 1.25±0.26h, t1/2 was 1.18±0.33h, AUC(0-t) was 17.97 ±4.34mg·h·L-1, Cl/F (s) was 5.30±1.46L.h-1, original drug percentage in urine within 12 hours was 6.23%±0.86%·L-enantiomer was not detected in both plasma and urine. CONCLUTION: Nateglinide has a rapid absorption and exclusion. The racemization of D-enantiomer in vivo was not observed.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第3期195-199,共5页
The Chinese Journal of Clinical Pharmacology
