Abstract: AIM: To investigate the influence of isosorbide-5-mononitrate on pharmacokinetics of nisoldipine in rats.METHODS: Healthy male SD rats were administered with nisoldipine or in combination with isosorbide-5-mononitrate, and the plasma concentrations of nisoldipine were determined by LC-MS/MS.RESULTS: Maximum plasma concentration of nisoldipine alone was (8.67±3.97) μg/L compared with (9.21±5.02) μg/L for the combination. The elimination half-lives were (2.26±0.66) h and (3.17±1.41) h for nisoldipine alone and in combination, respectively. The area under the concentration-time curve of nisoldipine alone was (19.6±9.9) μg·h·L^-1 as opposed to (25.7±13.7) μg·h·L^-1 in combination. The statistic analysis showed there were no significant differences between two groups (P＞0.05).CONCLUSION: Isosorbide-5-mononitrate does not affect the pharmacokinetics of nisoldipine in SD rats, which providing experimental basis for clinical application of isosorbide-5-mononitrate and nisoldipine.

Key words: nisoldipine, isosorbide-5-mononitrate, pharmacokinetics, LC-MS/MS