Pharmacokinetics and Tissue Distribution Kinetics of Puerarin in Rats Using Indirect Competitive ELISA

Abstract

Puerarin (PUE) is a compound isolated from the roots of Pueraria lobata. We studied the pharmacokinetics and tissue distribution kinetics of PUE in Sprague-Dawley rats following intraperitoneal administration of three concentrations. Indirect competitive ELISA based on an anti-PUE monoclonal antibody was used to determine the concentration of PUE in the blood, heart, liver, spleen, lung, kidney, hippocampus, cerebral cortex, and striatum. The plasma and tissue distribution kinetic characteristics following a single injection of PUE (20, 40, and 80 mg/kg) were calculated using a non-compartment model. In the high-dose (80 mg/kg) and medium-dose (40 mg/kg) groups, the kinetic profile of PUE in blood and kidney samples showed two absorption peaks, while that of the other tissues showed only one peak. In the low-dose (20 mg/kg) group, there was only one peak, irrespective of the sample type. Pharmacokinetic parameters such as the area under the curve, Cmax, and Tmax varied according to the administered dose. AUC and Cmax values increased dose-dependently. PUE was widely distributed in areas of the brain such as the hippocampus, cerebral cortex, and striatum, providing a foundation for guiding the use of PUE in the treatment of cerebral ischaemic stroke and neurodegenerative diseases.

Protective effects and mechanism of puerarin targeting PI3K/Akt signal pathway on neurological diseases

“…Also, puerarin can be quickly eliminated. Puerarin also crosses the blood-brain barrier and is widely distributed in the hippocampus, cerebral cortex, striatum, and other regions of the brain, but at low levels (Kong et al, 2017). The gastrointestinal absorption and bioavailability of puerarin are poor.…”

Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine

“…After intravenous injection, puerarin was detected in most organs, including the hippocampus, heart, lung, stomach, liver, mammary gland, kidney, spleen, tibia, and femur (Anukunwithaya et al., 2018). Puerarin could cross the blood-brain barrier, then widely distribute in areas of the brain such as hippocampus, cerebral cortex, and the striatum (Kong et al., 2017). The excretion of puerarin into the bile in the form of unconjugated puerarin was also detected (Prasain et al., 2009).…”