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Drug Res (Stuttg) 2013; 63(07): 342-345
DOI: 10.1055/s-0033-1341423
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetics of a New Tetramethylpyrazine Analogue CXC195 in Rats

C. Wei   *
1   Department of Pharmacology, School of Medicine, Shandong University
2   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Shandong University
,
L. Kong   *
1   Department of Pharmacology, School of Medicine, Shandong University
,
X. Wei
1   Department of Pharmacology, School of Medicine, Shandong University
,
L. Chen
1   Department of Pharmacology, School of Medicine, Shandong University
,
X. Liu
1   Department of Pharmacology, School of Medicine, Shandong University
,
X. Zhang
1   Department of Pharmacology, School of Medicine, Shandong University
,
X. Liu
3   Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University
,
H. Liu
1   Department of Pharmacology, School of Medicine, Shandong University
› Author Affiliations
Further Information

Publication History

received 16 January 2013

accepted 27 February 2013

Publication Date:
28 March 2013 (online)

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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
*

* These authors contributed equally to this work.


 

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