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Pharmacokinetic plasma behaviors of intravenous and oral bioavailability of thymoquinone in a rabbit model.

Abstract：

:Thymoquinone (THQ), the active constituent of Nigella sativa seeds, has demonstrated some potential pharmacological activities. The present study was designed to investigate the pharmacokinetic behavior of THQ following intravenous (IV) and oral (PO) administration using an animal model. THQ was given vascularly (5 mg/kg IV) and extravascularly (20 mg/kg PO) to Vole rabbits, and blood samples were collected at predetermined time points. The concentrations of THQ in plasma were measured by a high-performance liquid chromatography, and the pharmacokinetic parameters were determined using both compartmental and non-compartmental analyses. The calculated clearance (CL) following IV administration was 7.19 ± 0.83 ml/kg/min, and the estimated volume of distribution at steady state (V ss) was 700.90 ± 55.01 ml/kg. Whereas with PO dosing, apparent CL/F value was 12.30 ± 0.30 ml/min/kg and V ss/F was 5,109.46 ± 196.08 ml/kg. These parameters were associated with an elimination half-life (T 1/2) of 63.43 ± 10.69 and 274.61 ± 8.48 min with IV and PO dosing, respectively. The calculated absorption T 1/2 was about 217 min. Compartmental analysis revealed T 1/2α of ~8.9 min and T 1/2β of ~86.6 min. The calculated absolute bioavailability of THQ was ~58 % with a lag time of ~23 min. The estimated THQ protein binding was >99 %. Therefore, THQ represents a compound with rapid elimination and relatively slower absorption following PO administration.

journal_name

Eur J Drug Metab Pharmacokinet

journal_title

European journal of drug metabolism and pharmacokinetics

authors

Alkharfy KM,Ahmad A,Khan RM,Al-Shagha WM

doi

10.1007/s13318-014-0207-8

subject

Has Abstract

pub_date

2015-09-01 00:00:00

pages

319-23

issue

3

eissn

0378-7966

issn

2107-0180

journal_volume

40

pub_type

杂志文章

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