title: Comparative pharmacokinetics of active alkaloids after oral administration of Rhizoma Coptidis extract and Wuji Wan formulas in rat using a UPLC-MS/MS method.
abstract: Wuji Wan (WJW), containing Rhizoma Coptidis (Huanglian in Chinese, HL), Frutus Evodiae Rutaecarpae (Wuzhuyu, WZY) and Radix Paeoniae Alba (Baishao, BS), is a classical traditional Chinese medical formula employed in treating intestinal disorders. Berberine (BBR) and palmatine (PMT) are the major active alkaloids in HL and have analgesic and anti-microbial effects. A sensitive, specific and validated ultra-performance liquid chromatography-tandem mass spectrometric method was developed to investigate the pharmacokinetic profiles of BBR and PMT in rat plasma and in situ intestinal perfusion solution. In comparison with the pharmacokinetic parameters of BBR and PMT, t(1/2), C(max), T(max), AUC, CL and MRT after intragastric (i.g.) administration with HL extract alone, those remarkably changed after i.g. administration with WJW formulas 1 and 2 (herb proportions are 12:2:3 and 12:1:12). Particularly, the oral bioavailability of PMT in WJW formula 1 was significantly increased. In rat intestinal perfusion experiments, the apparent permeability coefficient value of PMT was (1.45 ± 0.72) × 10(-5) cm/s when perfusion with HL was performed, and the value was significantly increased to (3.92 ± 0.52) × 10(-5) cm/s on perfusion with WJW formula 1. These results indicate that the pharmacokinetic parameters and absorption of BBR and PMT are affected by the other herbs or ingredients from WJW formulas.
authors.affiliation: Department of Pharmacokinetics of Chinese Materia Medica, Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, No. 16, Dongzhimen Nei Nanxiao Road, Dongcheng District, Beijing, 100700, People's Republic of China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Yuejie
authors.initials: Y
authors.lastname: Li
authors.forename: Yajie
authors.initials: Y
authors.lastname: Wang
authors.forename: Qing
authors.initials: Q
authors.lastname: Yang
authors.forename: Yu
authors.initials: Y
authors.lastname: Dong
authors.forename: Xiaogang
authors.initials: X
authors.lastname: Weng
authors.forename: Xiaoxin
authors.initials: X
authors.lastname: Zhu
authors.forename: Yiwei
authors.initials: Y
authors.lastname: Wang
authors.forename: Zipeng
authors.initials: Z
authors.lastname: Gong
authors.forename: Ruijie
authors.initials: R
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001599:Berberine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001600:Berberine Alkaloids / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D002853:Chromatography, Liquid / Q000379:methods*; D000089042:Coptis chinensis; D004347:Drug Interactions; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D007408:Intestinal Absorption / Q000187:drug effects; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D008297:Male; D008657:Metabolic Clearance Rate; D008517:Phytotherapy; D010946:Plants, Medicinal; D051381:Rats; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry
chemical_list: D001600:Berberine Alkaloids; D004365:Drugs, Chinese Herbal; C000601111:wuji wan formula; D001599:Berberine; C107393:Coptidis rhizoma extract; C005413:palmatine