Pharmacokinetic performance of the nitrendipine intravenous submicron emulsion in rats

Abstract

To compare pharmacokinetic behaviors of nitrendipine submicron emulsion with nitrendipine solution following intravenous administration in rats. The plasma concentrations were analyzed by ultra-performance liquid chromatography coupled with tandem mass spectrometry detection (UPLC–MS/MS) through a new validated method. The pharmacokinetic parameters of the nitrendipine submicron emulsion and nitrendipine solution were as follows: AUC0–t 900.76 ± 186.59 versus 687.08 ± 66.24 ng h/ml, Cmax 854.54 ± 159.48 versus 610.59 ± 235.99 ng/ml, t1/2 2.37 ± 1.99 versus 2.80 ± 2.69 h. The relative bioavailability of nitrendipine submicron emulsion to nitrendipine solution was 131.4 ± 11.3%. The developed methods could meet the requirements of bioanalysis. Compared to the solution injection, intravenous submicron emulsion presents higher systematic exposure which can help to improve the therapeutic efficacy.

Keywords

• Nitrendipine
• Submicron emulsion
• Bioavailability
• Method validation