UPLC-MS/MS法测定人血浆中丙卡特罗的浓度  

Determination of procaterol in human plasma by UPLC-MS/MS

作　　者：赵想 杨亚楠 许杨 李玮 陶春蕾 ZHAO Xiang;YANG Ya-nan;XU Yang;LI Wei;TAO Chun-lei(School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;Anhui Wanbang Pharmaceutical Technology Co.,Ltd.,Heifei 230011;Anhui Provincial Institute for Food and Drug Control,Heifei 230051)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]安徽万邦医药科技股份有限公司,合肥230011 [3]安徽省食品药品检验研究院,合肥230051

出　　处：《中南药学》2023年第1期68-74,共7页Central South Pharmacy

摘　　要：目的建立超高效液相色谱串联质谱(UPLC-MS/MS)法测定人血浆中丙卡特罗的浓度,并研究丙卡特罗与原研制剂的人体生物等效性。方法采用固相萃取法处理血浆样品,内标为替硝唑,色谱柱为Hypersil GOLD C18(100 mm×2.1 mm,1.9μm),流动相为0.02%乙酸水溶液(含5 mmol·L^(-1)甲酸铵)-80%甲醇水溶液(含5 mmol·L^(-1)甲酸铵),流速为0.30 mL·min^(-1),柱温为40℃,进样量为5μL。32例健康受试者参加空腹试验,32例健康受试者参加餐后试验,均采用自身两交叉试验设计。采用WinNonlin 8.1软件计算得到药代动力学参数,并进行统计分析。结果丙卡特罗质量浓度在2.00~500 pg·mL^(-1)与测定值线性关系较好。空腹给药后参比制剂与受试制剂的C_(max)分别为(154±50.0)和(157±53.1)pg·mL^(-1),t_(max)分别为(1.01±0.38)和(1.17±0.54)h,t_(1/2)分别为(7.07±2.07)和(7.53±2.06)h,AUC_(0~t)分别为(719±194)和(724±168)pg·h·mL^(-1)。餐后给药后参比制剂与受试制剂的Cmax分别为(54.0±17.6)和(52.3±16.2)pg·mL^(-1),t_(max)分别为(1.73±0.97)和(1.94±1.01)h,t_(1/2)分别为(5.26±1.42)和(5.48±1.28)h,AUC_(0~t)分别为(295±76.9)和(307±74.3)pg·h·mL^(-1)。结论本方法可用于测定人血浆中丙卡特罗的浓度,两种片剂在空腹和餐后条件下均生物等效。Objective To establish an ultra-high performance liquid chromatography-mass spectrometry tandem(UPLC-MS/MS)method for the determination of the concentration of procaterol in human plasma,and to study the bioequivalence of procaterol and the original preparation meptin-mini.Methods The plasma samples were processed by solid phase extraction method.The internal standard was tinidazole,the column was Hypersil GOLD C18(100 mm×2.1 mm,1.9μm),and the mobile phase was 0.02%acetic acid aqueous solution(containing 5 mmol·L^(-1) ammonium formate)-80%methanol aqueous solution(containing 5 mmol·L^(-1) ammonium formate).The flow rate was 0.30 mL·min^(-1),the column temperature was 40℃,and the injection volume was 5μL.Totally 32 healthy subjects participated in the fasting test,and another 32 healthy subjects participated in the postprandial test.Both groups adopted their own two-crossover experimental design.Pharmacokinetic parameters were analyzed by WinNonlin 8.1 software.Results The standard curve of procaterol was good at 2.00~500 pg·mL^(-1).The pharmacokinetic parameters for procaterol of reference and test preparation under fasting condition were as follows:C_(max) was(154±50.0)and(157±53.1)pg·mL^(-1),t_(max) was(1.01±0.38)and(1.17±0.54)h,t_(1/2) was(7.07±2.07)and(7.53±2.06)h,and AUC_(0~t) was(719±194)and(724±168)pg·h·mL^(-1).The pharmacokinetic parameters for procaterol of reference and test preparation under postprandial condition were as follow:C_(max) was(54.0±17.6)and(52.3±16.2)pg·mL^(-1),tmax was(1.73±0.97)and(1.94±1.01)h,t_(1/2) was(5.26±1.42)and(5.48±1.28)h,and AUC_(0~t) was(295±76.9)and(307±74.3)pg·h·mL^(-1).Conclusion This method can be used to determine the concentration of procaterol in human plasma,and both tablets are bioequivalent under fasting and postprandial condition.

关 键 词：UPLC-MS/MS 丙卡特罗 固相萃取 生物等效性 

分 类 号：R96[医药卫生—药理学]