<abstract xmlns="http://www.w3.org/1999/xhtml">Fructose-1,6-diphosphate (FDP), a glycolytic metabolite, has been reported to protect susceptible organs during hypoxia or ischemia. However, there is paucity of human data on its pharmacokinetics after being exogenously administered. In the current study, the preliminary pharmacokinetics of FDP given orally to humans was investigated, and no typical peak was observed in the serum drug-time curve. Then, the pharmacokinetic studies were performed following multiple doses of FDP in rats, and the Caco-2 monolayer model was used to study the absorption of FDP in vitro. The results suggested that plasma FDP concentration was significantly increased after oral multiple doses of 180 mg kg-1 but not 90 mg kg-1 of FDP, and FDP was partly depleted during the absorption, which was supposed to be consumed by the intestinal epithelium cells. Thus, we conclude that a high dose of FDP should be orally administered in order to get an effective plasma level. </abstract>

Fructose-1,6-diphosphate (FDP), a glycolytic metabolite, has been reported to protect susceptible organs during hypoxia or ischemia. However, there is paucity of human data on its pharmacokinetics after being exogenously administered. In the current study, the preliminary pharmacokinetics of FDP given orally to humans was investigated, and no typical peak was observed in the serum drug-time curve. Then, the pharmacokinetic studies were performed following multiple doses of FDP in rats, and the Caco-2 monolayer model was used to study the absorption of FDP in vitro. The results suggested that plasma FDP concentration was significantly increased after oral multiple doses of 180 mg kg-1 but not 90 mg kg-1 of FDP, and FDP was partly depleted during the absorption, which was supposed to be consumed by the intestinal epithelium cells. Thus, we conclude that a high dose of FDP should be orally administered in order to get an effective plasma level.

Rational application of fructose-1,6-diphosphate: From the perspective of pharmacokinetics

Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education, West China School of Pharmacy, Sichuan University Chengdu, China 2 Pharmacy Department of People’s Hospital of Xishuangbanna Dai Autonomous Prefecture, Jinghong China

Pharmacy Department of People’s Hospital of Xishuangbanna Dai Autonomous Prefecture, Jinghong China

Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education, West China School of Pharmacy, Sichuan University Chengdu, China

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Fructose-1,6-diphosphate (FDP), a glycolytic metabolite, has been reported to protect susceptible organs during hypoxia or ischemia. However, there is paucity...

Rational application of fructose-1,6-diphosphate: From the perspective of pharmacokinetics

Publié en ligne: 23 mai 2015

Pages: 147 - 157

Accepté: 22 déc. 2014

DOI: https://doi.org/10.1515/acph-2015-0020

© by Xue-Hua Jiang

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.