摘要
目的：建立液相色谱-串联质谱联用法（liquid chromatography-tandem mass spectrum,LC-MS/MS）测定人血浆中头孢地尼的浓度,评价健康人餐后服用2种头孢地尼颗粒的生物等效性。方法：24例男性健康志愿者餐后随机交叉单剂量口服头孢地尼颗粒受试制剂或参比制剂,LC-MS/MS法测定头孢地尼体内血药浓度。采用药动学软件DAS对其药动学参数及等效性进行计算和评价。结果：头孢地尼在10.14-1 267.50 ng/ml质量浓度范围内线性良好（r〉0.999）,最低下限为10.14 ng/ml;日内、日间精密度RSD分别≤1.78%、3.75%。受试制剂和参比制剂的主要药动学参数包括：药-时曲线下面积（AUC）0-t分别为（4 284.81±1 150.02）和（4 479.97±1 333.70）μg·h/L,AUC0-∞分别为（4 425.56±1 173.44）和（4 632.83±1 369.83）μg·h/L,半衰期分别为（1.81±0.25）和（1.83±0.26）h,达峰时间分别为（3.70±0.71）和（3.73±0.51）h,峰浓度分别为（814.67±250.92）和（870.80±281.99）ng/ml。结论：该方法分析快速、灵敏、准确,适用于人血浆中头孢地尼浓度的测定,可成功用于头孢地尼颗粒生物等效性的评价。
OBJECTIVE：To establish a liquid chromatography-tandem mass spectrum（LC-MS/MS） method for deter-mination of cefdinir in human plasma, and to evaluate the bioequivalence after taking cefdinir granules in healthy volunteers.METHODS：A single dose of cefdinir granules of test or reference preparation were administered orally in 24 healthy male volunteers according to the randomized, two-way cross-over study.LC-MS/MS was adopted to determine the cefdinir concentration in human plasma.And the pharmacokinetic parameters and bioequivalence were calculated and evaluated with use of DAS software.RESULTS： The calibration curve was linear over the concentration ranges of 10.14-1 267.50 ng/ml （ r 〉0.999 ） , with the lower limit of quantitation （ LLOQ ） 10.14 ng/mL.RSD of within-day and between-day were lower than 1.78% and 3.75%.The main pharmacokinetic parameters of test and reference preparations were as follows：AUC0-t （ 4 284.81 ±1 150.02 ） μg· h/L and （4 479.97 ±1 333.70） μg· h/L, AUC0-∞（4 425.56 ±1 173.44） μg· h/L and （4 632.83 ±1 369.83） μg· h/L, t1/2 （1.81 ± 0.25） h and （1.83 ±0.26） h, tmax （3.70 ±0.71） h and （3.73 ±0.51） h, Cmax （814.67 ±250.92） ng/ml and （870.80 ± 281.99） ng/ml.CONCLUSIONS：The method is rapid, sensitive and accurate for the determination of cefdinir in human plasma, which had been successfully applied in the bioequivalence study of cefdinir granules in healthy volunteers.
出处
《中国医院用药评价与分析》
2016年第8期1014-1017,共4页
Evaluation and Analysis of Drug-use in Hospitals of China
基金
国家自然科学基金项目(No.81473287)
