A Method of Effectively Improved alpha-Mangostin Bioavailability

作者:Zhao, Yan*; Tang, Guosheng; Tang, Qiang; Zhang, Jing; Hou, Yingying; Cai, Enbo; Liu, Shuangli; Lei, Daihong; Zhang, Lianxue*; Wang, Shijie
来源:European Journal of Drug Metabolism and Pharmacokinetics, 2016, 41(5): 605-613.
DOI:10.1007/s13318-015-0283-4

摘要

alpha-Mangostin, a major xanthone isolated from the pericarp of Garcinia mangostana, exhibits anti-inflammatory and antitumor effects. Its absolute bioavailability is low, with minimal oral absorption. In this article, a soft capsule, with vegetable oil as the dispersion matrix, was prepared to improve the bioavailability of alpha-mangostin. Its pharmacokinetics and tissue distribution were determined in rats. An HPLC assay was established to determine the concentration of alpha-mangostin in biological samples. The validated method was used successfully to support pharmacokinetic and tissue distribution studies of alpha-mangostin in rats after intravenous (i.v.) and oral administration. The pharmacokinetic study found the absolute bioavailabilities of low, medium and high doses were 61.1, 51.5 and 42.5 %, respectively, indicating that the absolute bioavailability was effectively improved.