关键词: 硝苯地平缓释片, 硝苯地平缓释片, 硝苯地平缓释片, 液相色谱/质谱联用, 液相色谱/质谱联用, 液相色谱/质谱联用, 药动学, 药动学, 药动学, 生物等效性, 生物等效性, 生物等效性

Abstract:

Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4.6 mm × 150 mm) column and a mobile phase of methanol: 0.01 mol·L^-1 ammonium acetate (60:40, V/V) were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization (AP-ESI) mode and ion mass spectrum (m/z) of 314.9[M+H]+ for nifedipine, and 320.8 [M+H]+ for lorazepam (Internal Standard, IS). Results The linear range of nifedipine was 0.3 – 80 ng·mL^-1 ( r = 0.9997), and the limit of quantitation (LOQ) was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test (T) or reference (R) were as the followings, t1/2 (6.73 ± 2.00) h and (7.04 ± 2.18) h, Tmax (4.28 ± 0.70) h and (4.48 ± 0.70) h, Cmax (39.66 ± 10.58) ng·mL^-1 and (40.19 ± 10.97) ng·mL^-1, AUC0-36 (391.63 ± 108.55) ng·mL^-1·h and (387.57 ± 121.51) ng·mL^-1·h, and AUC0-∞ (408.28 ± 121.16) ng·mL^-1·h and (406.15 ± 133.13) ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets (test) was (103.02 ± 13.93) %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.

Key words: Nifedipine sustained-release tablets, Nifedipine sustained-release tablets, LC-MS, LC-MS, Pharmacokinetics, Pharmacokinetics, Bioequivalence, Bioequivalence