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.

Wuji Wan Formula Ameliorates Diarrhea and Disordered Colonic Motility in Post-inflammation Irritable Bowel Syndrome Rats by Modulating the Gut Microbiota

“…The Wuji Wan extract was a mixture of the above three extracts and was stored in a light-resistant container at 4°C before use. The qualitative chemical profile of this extract was analyzed by LC–MS as previously described ( Gong et al, 2014 ; Chen et al, 2015 ). PB tablets were obtained from Abbott Healthcare SAS (Abbott, Chatillon Sur Chalaronne, France).…”

Pharmacokinetics of Two Alkaloids after Oral Administration of Rhizoma Coptidis Extract in Normal Rats and Irritable Bowel Syndrome Rats

“…The qualitative chemical profile of these extracts was analyzed by UPLC-MS/MS as previously described [21]. And the content of berberine and palmatine in the ethanol extract of RC was 23.03% and 5.52%.…”

Metabolic profile of Rhizoma coptidis in human plasma determined using ultra‐high‐performance liquid chromatography coupled with high‐resolution mass spectrometry

“…As we know, the in vivo processes of Chinese herbs are difficult to clarify due to their varied compositions and complex metabolic pathways. Based on the assumption that only the constituents absorbed into the blood have the opportunity to exhibit pharmacological effects, detailed pharmacokinetic studies of the alkaloids, including berberine, coptisine and palmatine, after oral administration of Rhizoma coptidis extract in rat plasma, rabbit plasma and the pharmacokinetic behavior of berberine in the plasma of healthy male volunteers were conducted. However, to the best of our knowledge, few efforts have been made to investigate the metabolic profile of the whole extract of Rhizoma coptidis in human plasma.…”