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Planta Med 2021; 87(05): 395-403
DOI: 10.1055/a-1271-7092
Pharmacokinetic Investigations
Original Papers

Comparative Pharmacokinetics of Puerarin Alone and in Pueraria mirifica Extract in Female Cynomolgus Monkeys

Sureerat Namken
1   Department of Biology, Faculty of Science, Chulalongkorn University, Bangkok, Thailand
,
Phanit Songvut
2   Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand
3   Translational Research Unit, Chulabhorn Research Institute, Bangkok, Thailand
,
Nitra Nuengchamnong
4   Science Laboratory Centre, Faculty of Science, Naresuan University, Phitsanulok, Thailand
,
Taratorn Kemthong
5   National Primate Research Center of Thailand-Chulalongkorn University, Saraburi, Thailand
,
Phisit Khemawoot
6   Preclinical Pharmacokinetics and Interspecies Scaling for Drug Development Research Unit, Chulalongkorn University, Bangkok, Thailand
7   Chakri Naruebodindra Medical Institute, Faculty of Medicine Ramathibodi Hospital, Mahidol University, Samutprakarn, Thailand
,
Suchinda Malaivijitnond
1   Department of Biology, Faculty of Science, Chulalongkorn University, Bangkok, Thailand
5   National Primate Research Center of Thailand-Chulalongkorn University, Saraburi, Thailand
6   Preclinical Pharmacokinetics and Interspecies Scaling for Drug Development Research Unit, Chulalongkorn University, Bangkok, Thailand
› Author AffiliationsSupported by: 90th Anniversary Chulalongkorn University Fund (Ratchadaphiseksomphot Endowment Fund)
Supported by: Chulalongkorn University Research Unit Grant
Supported by: Scholarship from the Graduate School, Chulalongkorn University to commemorate the 72nd Anniversary of his Majesty King Bhumibol Adulyadej
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Abstract

Pueraria mirifica is an endemic Thai plant that has been used for rejuvenation and in the relief of various aging diseases. Puerarin is one of the major isoflavones found in this plant and shows several pharmacological activities in relation to the Thai traditional use of P. mirifica. Therefore, comparative pharmacokinetics of pure puerarin alone and that in a P. mirifica extract in cynomolgus monkeys were conducted in order to investigate the pharmacokinetic profiles of the 2 preparations. To this end, puerarin and P. mirifica extract, at an equivalent dose of 10 mg/kg of puerarin, were orally dosed to adult female monkeys for 7 consecutive days. A single intravenous injection of puerarin at a dose of 1 mg/kg was also peformed. Serial blood samples and excreta were collected from 0 – 24 h and 0 – 48 h after dosing. Determination of the puerarin levels and its metabolites in biological samples was conducted by liquid chromatography tandem mass spectrometry. Plasma levels of aspartate aminotransferase, alanine aminotransferase, and creatinine fluctuated in the normal range, with no abnormal physical signs in the animal. The absolute oral bioavailability of puerarin was approximately 1% in both preparations. Accumulation of puerarin was found after oral dosing for 7 consecutive days in both groups. Major metabolites of puerarin found in monkeys were hydroxylation and deglycosylation products. A negligible amount of unchanged puerarin was detected in urine and feces. Pharmacokinetic profiles obtained from this study could help to design the prescribed remedy of puerarin and P. mirifica extract phytopharmaceutical products for human use.

Key words

bioavailability - Fabaceae - Macaca fascicularis - pharmacokinetics - Pueraria mirifica - puerarin


Publication History

Received: 05 May 2020

Accepted after revision: 21 September 2020

Article published online:
15 October 2020

© 2020. Thieme. All rights reserved.

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