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LC-MS/MS法测定人血浆中地氯雷他定与代谢物3-OH地氯雷他定浓度及其生物等效性研究
Determination of Desloratadine and Its Metabolite 3-OH Desloratadine in Human Plasma by LC-MS/MS
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摘要: 目的 建立液相色谱-串联质谱（LC-MS/MS）法测定人血浆中地氯雷他定及其代谢物3-OH地氯雷他定的浓度，并应用于两种地氯雷他定片的餐后人体生物等效性研究。方法 采用双周期随机交叉自身对照试验设计，24例健康男性受试者餐后分别单剂量口服两种地氯雷他定片5 mg，LC-MS/MS法测定血浆中地氯雷他定及其代谢物3-OH地氯雷他定的浓度，以Winnonlin6.3软件计算主要药动学参数，并评价两种地氯雷他定片的餐后生物等效性。结果 地氯雷他定和3-OH地氯雷他定标准曲线范围均为0.050～6.0 ng/mL，批内、批间相对标准偏差均在15%以内。地氯雷他定和3-OH地氯雷他定峰浓度（Cmax）、药时曲线下面积（AUC）0-t、AUC0-∞的90%置信区间均在80%~125%等效区间之内，达峰时间（tmax）经非参数秩和检验，不同制剂间差异无统计学意义（ P>0.05）。结论 所建立的LC-MS/MS方法适用于人血浆中地氯雷他定及其代谢物3-OH地氯雷他定浓度的同时测定，并可以用于地氯雷他定片生物等效性的评价。Abstract: Objective To develop a liquid chromatography-tandem mass spectrometry （LC-MS/MS） method for the simultaneous determination of desloratadine and its metabolite 3-OH desloratadine in human plasma. Methods 24 healthy male volunteers received a single oral dose of 5 mg desloratadine tablets in a randomized crossover bioequivalence study with two preparations of tablets. Serial plasma samples were taken and analyzed by the LC-MS/MS method. The pharmacokinetic parameters of the two preparations were calculated and compared statistically to evaluate their bioequivalence using Winnonlin 6.3. Results The calibration curves of desloratadine and 3-OH desloratadine were both linear over the concentration range of 0.050-6.0 ng/mL, with intra-batch and inter-batch relative standard deviations less than 15%. The 90% confidence intervals (CIs) of peak concentration （Cmax），area under the curve （AUC）0-t and AUC0-∞ of desloratadine and 3-OH desloratadine all resided within the bioequivalence limit 80%-125%. No significant difference in peak time (tmax) was demonstrated between the two preparations. Conclusion The LC-MS/MS method can be used for simultaneous determination of desloratadine and 3-OH desloratadine in human plasma, which has been successfully applied to a bioequivalence study.
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期刊类型引用(4)
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3. 刘璐，甄路路，任美娟，李蕊，刘畅，闫美兴. 地氯雷他定治疗荨麻疹的临床综合评价. 中国药房. 2022(10): 1240-1246 . 百度学术
4. 王梦颖，陈烨超，涂凤琴，侯靖，杨明，卢跃鹏，王煜红，杨总，陈丹. 超高效液相色谱-四极杆-飞行时间高分辨质谱用于乳液类化妆品中9种抗过敏违禁药物的筛查和定量分析. 色谱. 2020(12): 1423-1430 . 百度学术
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