摘要
目的建立一种简便、灵敏的测定人血浆中格列吡嗪血药浓度的高效液相色谱-串联质谱(HPLC-MS/MS)方法,计算两种制剂在中国健康受试者的药动学参数并评价生物等效性。方法采用双周期、随机、自身交叉试验设计,24名受试者分别服用受试制剂或参比制剂5 mg,采用高效液相色谱-串联质谱法(HPLC-MS/MS)测定其血药浓度。计算受试制剂和参比制剂的药动学参数并评价其生物等效性。结果受试者口服受试制剂和参比制剂5 mg后格列吡嗪的平均ρmax分别为(251.25±61.94)和(240.13±52.43)μg·L-1,t1/2分别为(4.85±1.39)和(5.08±1.76)h,tmax分别为(3.35±1.22)和(3.38±1.35)h,AUC0-tn分别为(1 561.44±475.73)和(1 588.82±507.40)μg·h·L-1。结论建立的HPLC-MS/MS法灵敏,简单,可用于血浆中格列吡嗪血药浓度的测定;受试者服药后血药浓度结果经统计学分析,表明两种制剂所含的格列吡嗪生物等效。
ObjectiveTo establish a simple and sensitive method of high performance liquid chromatography - tandem mass spectrometry （HPLC-MS/MS） for the determination of glipizide in human plasma and to calculate the pharmacokinetic parameters and evaluate the bioequivalence of two glipizide preparations in healthy Chinese volunteers. Methods A two-periods, randomized, crossover trial design was used. Twenty-four subjects took the test and reference preparations at the dose of 5 mg , and glipizide plasma concentration was determined by HPLC-MS/MS. Pharmacokinetic parameters were calculated and bioequivalence was evaluated. Results The mean pharmacokinetic parameters of glipizide after adminstration of 5 mg of test or reference preparations were as follows： ρmax were （251.25±61.94） and （240.13±52.43） μg·L-1, t1 / 2 were （4.85±1.39） and （5.08±1.76） h, tmax were （3.35±1.22） and （3.38±1.35） h, and AUC0-tn were （1 561.44±475.73） and （1 588.82±507.40） μg·h·L-1, respectively. Conclusion The HPLC-MS/MS method is sensitive and simple, and can be used for the determination of glipizide plasma concentration. Statistical analysis of the pharmacokinetic parameters in heathy subjects indicated that the two preparations of glipizide are bioequivalent.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2013年第14期1204-1208,共5页
Chinese Pharmaceutical Journal
