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刊物信息

期刊名称:药物分析杂志
主管单位:中国科学技术协会
主办单位:中国药学会
承办:中国食品药品检定研究院
主编:金少鸿
地址:北京天坛西里2号
邮政编码:100050
电话:010-67012819,67058427
电子邮箱:ywfx@nifdc.org.cn
国际标准刊号:ISSN 0254-1793
国内统一刊号:CN 11-2224/R
邮发代号:2-237
 

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LC-MS/MS法研究阿普唑仑胃漂浮片恒河猴生物等效性

Bioequiavailability study of intragastric floating tablets of alprazolam in rhesus monkeys by LC-MS/MS

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出版年·卷·期(页码):2014,34 (3):0-0
DOI: 10.16155/j.0254-1793.2017.01.01
-----摘要:-------------------------------------------------------------------------------------------

目的:建立LC-MS/MS法测定恒河猴血浆中阿普唑仑的浓度,并用于阿普唑仑胃漂浮片的生物等效性分析。方法:采用随机、双周期、自身交叉试验设计,6只恒河猴单剂量口服受试制剂或参比制剂(1.2 mg),不同时间点采集的血浆样本经提取,液相色谱-串联质谱法测定血浆样本中阿普唑仑的浓度,并使用DAS2.1软件计算药代动力学参数,评价制剂的生物等效性。结果:阿普唑仑的线性范围为0.4~100 ng·mL-1,定量下限为0.4 ng·mL-1,日内、日间精密度(RSD)均小于15%,准确度(RE)在±15%以内。恒河猴单剂量口服受试制剂和参比制剂Cmax分别为(64.75±8.78)、(78.87±6.06)ng·mL-1Tmax分别为(4.50±1.22)、(2.17±0.52)h,t1/2分别为(3.51±1.72)、(3.51±1.52)h,AUC0-t分别为(719.93±114.74)、(326.93±66.20)h·ng·mL-1,相对生物利用度为(233.18±86.82)%。结论:LC-MS/MS方法适用于阿普唑仑制剂生物等效性研究。受试制剂与参比制剂比较生物利用度显著提高,Tmax显著推迟,具有缓释的效果。

-----英文摘要:---------------------------------------------------------------------------------------

Objective: To establish a method of high performance liquid chromatography tandem mass spectrometry(HPLC-MS/MS)for the determination of alprazolam in plasma of rhesus monkeys and the bioequivalence analysis of intragastric floating alprazolam tablets. Methods: In a randomized,double-period,self-crossover study,6 rhesus monkeys were given a single oral dose of test or reference tablets containing 1.2 mg alprazolam. Then the plasma concentration was determined by HPLC-MS/MS method after extraction of alprazolam. The pharmacokinetic parameters were calculated by DAS 2.1 program and the bioequivalence of two formulations was evaluated. Results: The calibration curve of alprazolam was linear in the range of 0.4-100 ng·mL-1. The lower limit of quantitation was 0.4 ng·mL-1. Intra-day and inter-day RSDs were both less than 15% and the relative error(RE)was within ±15%. The pharmacokinetic parameters for test tablets vs reference tablets were as follows: Cmax of(64.75±8.78)and(78.87±6.06)ng·mL-1,Tmax of(4.50±1.22)and(2.17±0.52)h,t1/2 of(3.51±1.72)and(3.51±1.52)h,AUC0-t of(719.93±114.74)and(326.93±66.20)h·ng·ml-1,the relative bioavailability was(233.18±86.82)%. Conclusion: The LC-MS/MS method is suitable for the bioequivalence study of alprazolam preparations. The statistic data showed that Tmax for test tablets was significantly delayed comparded with reference tablets,indicating that test tablets had sustained-release effect.

-----参考文献:---------------------------------------------------------------------------------------

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