Comparison of the pharmacokinetics of levetiracetam injection and levetiracetam tablets in human

Abstract

Abstract:

AIM: To compare the pharmacokinetic parameters of levetiracetam with those of levetiracetam tablets in fasting condition, and to observe the safety and tolerability of them in healthy subjects. METHODS: The concentrations of levetiracetam in plasma samples of healthy subjects before and after two cycles of administration were determined using established high performance liquid chromatography-mass spectrometry (HPLC-MS/MS) analysis. RESULTS: The main pharmacokinetic parameters of levetiracetam after intravenous injection and oral administration of levetiracetam were as follows:t1/2 were (7.70±0.85), (7.81±0.88) h;Tmax were（0.70±0.10) , (0.90±0.80）h, Cmax were (51.64±9.59) , (40.83±9.13) ng/mL and AUC0-t were (385.69±65.45) , (394.24±64.68) ng·mL-1·h, and AUC0-∞ was (390.85±66.40), (400.13±65.89) ng·mL-1·h, respectively. The average relative bioavailability of the test preparation was (98.1±9.4)% with levetiracetam AUC0-t. No severe adverse events were observed during the trial. CONCLUSION: The pharmacokinetic parameters of levetiracetam and levetiracetam tablets are not significantly different, and the safety is better in healthy subjects.

Key words: levetiracetam, antiepileptic drugs, HPLC-MS/MS, pharmacokinetic, safety evaluation

CLC Number:

R969.1

LIU Shijia, CHEN Du, YIN Jungang, CHU Jihong, XU Meijuan, LIU Fang, DAI Guoliang, XIONG Ningning, JU Wenzheng. Comparison of the pharmacokinetics of levetiracetam injection and levetiracetam tablets in human[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2017, 22(3): 294-298.

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