Abstract
Objective:
To investigate the pharmacokinetical characteristics of a new neuroprotective drug
CXC195 after intraperitoneal injection in rats.
Method:
A single 10 mg · kg−1 of CXC195 was intraperitoneally injected to 8 rats after fasting overnight, respectively.
500 microliters of blood samples were collected at scheduled time before and after
administration. CXC195 in rats’ plasma was separated on a Diamonsil C18 column (150 mm×4.6 mm, 5 μm), eluted using methanol − 0.05 mM NaH2PO4 solution (86:14, v/v) as mobile phase, and detected by UV detector at wavelength
of 278 nm. The plasma concentration of CXC195 was determined by established HPLC method
after disposition and its pharmacokinetic parameters were analyzed and evaluated by
Drug and Statistic (version 2.0).
Results:
The Cmax, Tmax, t1/2, AUC0-8, AUC0-∞, MRT0-8, MRT0-∞, CL/F and V/F of CXC195 aftersingle dose intraperitoneal injection of 10 mg · kg−1 CXC195 were 12.37±5.35 μg · mL−1, 0.5±0.21 h,4.24±2.43 h, 24.89±8.32 μg · mL−1 · h, 28.57±9.66 μg · mL−1 · h, 2.00±0.53 h, 2.93±0.75 h, 1.4±0.73 L · h−1 and 1.16±0.68 L.
Conclusion:
The established HPLC method was sensitive, rapid, and suitable for CXC195 pharmacokinetic
study. The procedure of CXC195 in rat was fit to double-compartmental model with lag
time of 0.13 h.
Key words
CXC195 - tetramethylpyrazine - pharmacokinetics - HPLC