KMID : 0043320100330091395
|
|
Archives of Pharmacal Research 2010 Volume.33 No. 9 p.1395 ~ p.1400
|
|
Effects of prednisolone on the pharmacokinetics of loratadine after oral and intravenous administration of loratadine in rats
|
|
Li Cheng
Kim Min-Hee Choi Jun-Shik
|
|
Abstract
|
|
|
The present study aims to investigate the effects of prednisolone on the pharmacokinetics of orally and intravenously administered loratadine in rats. A single dose of loratadine was administered orally (4 mg/kg) and intravenously (1 mg/kg) in the presence or absence of prednisolone (0.2 or 0.8 mg/kg). Compared to the oral control group, prednisolone (0.2 mg/kg, p < 0.05; 0.8 mg/kg, p < 0.01) significantly increased the area under the plasma concentrationtime curve of orally administered loratadine by 54.0?96.4%. After oral administration, the peak plasma concentration of loratadine was significantly (0.2 mg/kg, p < 0.05; 0.8 mg/kg, p < 0.01) increased by 20.9?65.3% in the presence of prednisolone. Consequently, the relative bioavailability of loratadine was increased by 1.54- to 1.96-fold. Compared to the intravenous control group, the presence of prednisolone significantly (0.8 mg/kg, p < 0.05) increased the area under the plasma concentration-time curve of loratadine. Prednisolone enhanced the oral bioavailability of loratadine in this study. The enhanced bioavailability of loratadine may be due to inhibition both cytochrome P450 3A4-mediated metabolism and the efflux pump P-glycoprotein (P-gp) in the intestine and/or liver by the presence of prednisolone.
|
|
KEYWORD
|
|
Prednisolone, Loratadine, Pharmacokinetics, Bioavailability, CYP3A4, P-gp, Rats
|
|
FullTexts / Linksout information
|
|
|
|
Listed journal information
|
|
|
|