Pharmacokinetics of verproside after intravenous and oral administration in rats = rat에서 verproside의 경구 및 혈관투여 후 약동력학 연구

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Title
Pharmacokinetics of verproside after intravenous and oral administration in rats = rat에서 verproside의 경구 및 혈관투여 후 약동력학 연구
Author(s)
E J Park; H S Lee; Sei Ryang Oh; Hyeong Kyu Lee; H S Lee
Bibliographic Citation
Archives of Pharmacal Research, vol. 32, no. 4, pp. 559-564
Publication Year
2009
Abstract
Verproside, a catalpol derivative iridoid glucoside isolated from Pseudolysimachion longifolium, is a candidate for anti-asthmatic drug. The dose-dependency of the pharmacokinetics of verproside was evaluated in rats after intravenous and oral administration. After intravenous administration of verproside (2, 5 and 10 mg/kg doses), the systemic clearance (Cl) was significantly reduced and AUC was significantly increased at 10 mg/kg dose compared to 2 and 5 mg/kg doses. The volume of distribution at steady state (V ss) remained unchanged as the dose was increased. The extent of urinary excretion was low for both intravenous (3.3-6.2%) and oral (0.01-0.04%) doses. Isovanilloylcatalpol was identified as a metabolite after intravenous administration of verproside and showed the significant decreases in AUC and C max at 10 mg/kg verproside dose. The reduced systemic clearance of verproside at high doses appears to be due to the saturable metabolism. Upon oral administration of verproside (20, 50 and 100 mg/kg doses), C max was nonlinearly increased. The extent of verproside recovered from the gastrointestinal tract at 24 h after oral administration was 0.01-0.72% for all three doses studied. The absolute oral bioavailability (F) was 0.3 and 0.5% for 50 and 100 mg/kg doses, respectively. Low F appears to be due to first-pass metabolism.
Keyword
IsovanilloylcatalpolLC/MSPharmacokineticsRatsVerproside
ISSN
0253-6269
Publisher
Pharmaceutical Soc Korea
DOI
http://dx.doi.org/10.1007/s12272-009-1412-x
Type
Article
Appears in Collections:
Ochang Branch Institute > 1. Journal Articles
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