HPLC测定血浆中那格列奈及其人体药动学和相对生物利用度研究  

Determination of Nateglinide by HPLC and Its Application of Its Pharmacokinetics and Relative Bioavailability

作　　者：朱南平[1] 徐平声[2] 

机构地区：[1]中南大学湘雅二医院临床药学研究室,长沙410011 [2]中南大学湘雅医院药剂科,长沙410008

出　　处：《中国药学杂志》2006年第13期1013-1015,共3页Chinese Pharmaceutical Journal

基　　金：湖南省卫生厅课题资助项目(Y02-046)

摘　　要：目的 建立HPLC测定血浆中那格列奈，并研究其药动学及相对生物利用度。方法 18名受试者随机等分成2组，先后单剂量po受试制剂或参比制剂后，采用HPLC测定血药浓度，计算药动学参数并进行方差分析，以双单侧t检验进行生物等效性判定。结果 单次服用60mg受试制剂或参比制剂后的药动学参数AuC0～10，AuC0-∞，ρmax，tmax及t1／2分别为（6．84±3．51）和（7．24±3．51）mg·h·L^-1，（6．95±3．45）和（7．38±3．58）mg·h·L^-1，（4．35±2.45）和（4.20±2.13）mg·L^-1，（1.02±0.48）和（1．16±0．51）h，（2．20±0.78）和（2.04±0．65）h。受试制剂对参比制剂的相对生物利用度为（94．5±13）％。2种制剂的药动学参数无明显差异。结论 HPLC能快速、准确测定人血浆中的那格列奈．受试制剂与参比制剂具有生物等效性。OBJECTIVE To determine the concentration of nateglinide in human plasma by HPLC method, and study its pharmacokinetics, relative bioavailability. METHODS Eighteen volunteers were randomized into 2 groups. The subjects in group one firstly received the test preparation of nateglinide tablets, followed by the reference preparation. The subjects in group two received the reference preparation firstly, followed by the test preparation. The plasma concentration of nateglinide was measured by high performance liquid chromatography （HPLC） method. ANOVA was used to check the difference of the means of the pharmacokinetic parameters between the two preparations. Bioequivalence was determined by student t-tests. RESULTS The pharmacokinetie parameters of the volunteers after a single dose of 60 mg of the test preparation or the reference preparation were as follows： AUC0 - 10 （ 6.84±3.51 ） and （7.24±3.51 ） mg·h·L^-1, AUC0 -∞ （6.95±3.45） and （7.38±3.58） mg·h·L^-1,ρmax（4.35±2.45） and （4.20±2.13） mg·L^-1,tmax（1.02±0.48） and （1.16±0.51） h, t1/2（2.20±0.78） and （2.04 ± 0.65） h, respectively. The relative bioavailability was（94.5 ± 13）%. No significant differences were found among the main pharmacokinetic parameters. CONCLUSION The method can determine gemflbrozil in the human body quickly and correctly. The two preparations are equivalent.

关 键 词：那格列奈 高效液相色谱法 药动学 生物利用度 

分 类 号：R969[医药卫生—药理学]