𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Pharmacokinetics and bioavailability of the flavonoid 7,8-benzoflavone in rats

✍ Scribed by Xiaodong Wang; Marilyn E. Morris

Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
164 KB
Volume
97
Category
Article
ISSN
0022-3549

No coin nor oath required. For personal study only.

✦ Synopsis

The flavonoid 7,8-benzoflavone was recently identified as one of the most potent inhibitors of breast cancer resistance protein (BCRP); however, little is known of the in vivo disposition of 7,8-benzoflavone. The objective of this study was to investigate the pharmacokinetics and bioavailability of 7,8-benzoflavone in rats. Three intravenous (5, 10, and 25 mg/kg) and three oral (12.5, 25, and 50 mg/kg) doses were administered to female Sprague-Dawley rats. Plasma samples were analyzed by high-performance liquid chromatography. Pharmacokinetic analysis was conducted by WinNonlin and ADAPT II. The dose-normalized plasma concentration versus time curves did not superimpose with each other, indicating the nonlinear pharmacokinetics of 7,8-benzoflavone. 7,8-benzoflavone exhibited a large volume of distribution (V(ss) approximately 1.5 L/kg) and rapid oral absorption (t(max) < 30 min). The bioavailability of 7,8-benzoflavone was low (0.61-13.2%) and dose-dependent. A pharmacokinetic model with dose-dependent bioavailability, linear absorption and nonlinear elimination best described the pharmacokinetic profiles of 7,8-benzoflavone. Using a 50 mg/kg oral dose of 7,8-benzoflavone, we could significantly increase the AUC for the BCRP substrate nitrofurantoin, demonstrating the potential for BCRP-mediated drug interactions.

📜 SIMILAR VOLUMES

Pharmacokinetics and bioavailability of
Pharmacokinetics and bioavailability of methocarbamol in rats
✍ R. Obach; J. Pruñonosa; A. Menargues; M. Nomen; J. Vallès 📂 Article 📅 1988 🏛 John Wiley and Sons 🌐 English ⚖ 467 KB 👁 1 views

In a pharmacokinetic study, 15, 30, 60, and 150 mg kg-' intravenous and oral doses of methocarbamol were administered to rats. Differences observed in plasma clearance values, i.e. 0~0203,0~0156,0~0123, and 0-0085 1 kg-' min-' for 15,30,60, and 150 mg kg-', respectively, suggested a dosedependent ph

Bioavailability and pharmacokinetic mode
Bioavailability and pharmacokinetic model for ritonavir in the rat
✍ R. Lledó-García; A. Nácher; L. Prats-García; V.G. Casabó; M. Merino-Sanjuán 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 English ⚖ 216 KB

The aim of this study is to investigate in vivo the oral bioavailability of ritonavir and to evaluate the pharmacokinetic model that best describes the plasma concentration behavior after oral and intravenous administration. Male Wistar rats were intravenously administered at 3 mg dose of pure riton

Metabolism, oral bioavailability and pha
Metabolism, oral bioavailability and pharmacokinetics of chemopreventive kaempferol in rats
✍ Avantika Barve; Chi Chen; Vidya Hebbar; Joseph Desiderio; Constance Lay-Lay Saw; 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 English ⚖ 155 KB 👁 2 views

## Abstract The purpose of this study was to compare the hepatic and small intestinal metabolism, and to examine bioavailability and gastro‐intestinal first‐pass effects, of kaempferol in rats. Liver and small intestinal microsomes fortified with either NADPH or UDPGA were incubated with varying co

The bioavailability and nonlinear pharma
The bioavailability and nonlinear pharmacokinetics of MK-679 in humans
✍ Haiyung Cheng; Jules I. Schwartz; Charles Lin; Raju D. Amin; James R. Seibold; K 📂 Article 📅 1994 🏛 John Wiley and Sons 🌐 English ⚖ 451 KB 👁 2 views

## Abstract MK‐679 (R(−)‐3‐((3‐(2‐(7‐chloro‐2‐quinolinyl)ethenyl)phenyl)(3‐(dimethylamino)‐3‐oxopropyl)thio)methyl)thio(propanoic acid) is a potent and specific LTD~4~‐receptor antagonist. The disposition of MK‐679 was investigated in a three‐way crossover study in 12 healthy males receiving single