Study of pharmacokinetics and bioavailability of scicinib in rats

Abstract

Abstract: AIM: To investigate the pharmacokinetic properties of scicinib and its absolute bioavailability in vivo in rats.METHODS: With the LC/MS/MS method for the quantification of scicinib in biosamples, the concentration of scicinib in rat plasma was determined after administrated (i.g.) scicinib at the dose of 5, 10, 20, 40 mg/kg and intravenous injected scicinib at the dose of 5 mg/kg. Main pharmacokinetic parameters were estimated by non-compartmental analysis using 3P97 software. Experimental data was calculated by t-test and then the absolute bioavailability was determined.RESULTS: The pharmacokinetic property of scicinib fitted two compartment model after scicinib was given to rats at a single dose (5, 10, 20 and 40 mg/kg). The AUC_0-T was linearly increased with the increase of dosage in rats, while t_1/2 was not varied,the t_1/2 was (6.26±1.26),(5.80±4.44),(7.16±4.40),(7.38±3.24) h, respectively. The absolute bioavailability of scicinib after administration (i.g.) at the dose of 5 mg/kg was 20.4%.CONCLUSION: The pharmacokinetic behavior of scicinib showes the first-order kinetics characteristics after the dosage of 5-40 mg/kg, and the absolute bioavailability was well accepted.

Key words: scicinib, LC/MS/MS, pharmacokinetic, bioavailability

CLC Number:

R965.2

ZOU Quan-fei, LU Rong, FAN Hui-rong, ZHAO Guang-rong, ZHANG Tie-jun, SI Duan-yun. Study of pharmacokinetics and bioavailability of scicinib in rats[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(3): 254-259.

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