Preclinical pharmacokinetics, tissue distribution and excretion studies of a potential analgesics – corydaline using an ultra performance liquid chromatography–tandem mass spectrometry

• The PK, tissue distribution and excretion of corydaline was investigated.
• Corydaline was quickly absorbed and eliminated.
• Rapid and wide distribution into tissues and BBB penetration ability of corydaline.
• Few of corydaline were excreted unchangingly.

A rapid resolution ultra performance liquid chromatography (UPLC) coupled with electrospray ionization (ESI) mass spectrometry method was developed and validated for the quantitative analysis of corydaline in rats’ plasma and various tissues for pharmacokinetic, tissue distribution and excretion studies of corydaline. The analytes were separated on an Acquity UPLC BEH C18 column (2.1 mm × 100 mm, 1.7 μm) and detected with a triple quadrupole mass spectrometer using positive ion ESI in the multiple reaction monitoring (MRM) mode. The MS/MS ion transitions monitored were m/z 370.0 → 192.0 for corydaline and 354.1 → 188.0 for IS, respectively. Calibration curves (1/x2 weighted) offered satisfactory linearity (r2 > 0.9984) within 1–1000 ng/mL. The accuracy and precision ranged from −7.4% to 8.5% and 3.4% to 12.8%, respectively. The absolute matrix effect (94.2–119.2%), relative matrix effect (1.7–9.6%) and recoveries (81.4–93.7%) were satisfactory in all the biological matrices examined. The assay was successfully applied to the plasma pharmacokinetics, tissue distribution and excretion studies of corydaline in rats. The pharmacokinetic parameters such as half-life (t1/2), mean residence time (MRT) and maximum concentration (Cmax) were determined. These preclinical data of corydaline would be useful for the clinical reference.