文献类型：期刊文献

英文题名：Pharmacokinetics of isoforskolin after administration via different routes in guinea pigs

作者：Feng, Tingting[1];Li, Yong[1];Chen, Jun[2];Chen, Yong[1];Huang, Jianming[2];Weng, Weiyu[1]

机构：[1]East China Univ Sci Technol, Sch Pharm, Dept Pharmaceut, Shanghai, Peoples R China;[2]Fudan Univ, Sch Pharm, 826 Zhangheng Rd, Shanghai 201203, Peoples R China

年份：2016

卷号：46

期号：7

起止页码：620

外文期刊名：XENOBIOTICA

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000373943100008)】；

基金：The authors report no conflicts of interest. Science and Technology Commission of Shanghai Municipality provided financial support (13401900502) to this study.

语种：英文

外文关键词：Bioavailability; guinea pigs; HPLC-ESI-MS; MS; isoforskolin; pharmacokinetics

摘要：1.The objective of this study was to characterize the pharmacokinetics of isoforskolin after oral, intraperitoneal and intravenous administration, as well as to compare bioavailability.2.Isoforskolin was administered to guinea pigs at a dose of 2mg/kg. Plasma concentrations were determined by high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (HPLC-ESI-MS/MS) method. The pharmacokinetic parameters were calculated by a noncompartmental method. A compartment model was also adopted to describe the pharmacokinetic profiles.3.The pharmacokinetic behavior of intravenously administered isoforskolin was characterized by rapid and extensive distribution (V-z=16.828.42L/kg) followed by rapid elimination from the body (Cl=9.63 +/- 4.21L/kg/h). After intraperitoneal administration, isoforskolin was absorbed rapidly (T-max=0.12 +/- 0.05h). The pharmacokinetic profiles of isoforskolin were similar after intraperitoneal and intravenous administration, except for the concentrations at the initial sampling times. Isoforskolin was also absorbed rapidly following oral dosing; however, the concentration-time data were best fit to a one-compartment model, which was different from that observed after intravenous and intraperitoneal administration. Following intraperitoneal and oral administration, the absolute bioavailability of isoforskolin was 64.12% and 49.25%, respectively.4.Isoforskolin is a good candidate for oral administration because of its good oral bioavailability.