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

Abstract

A comparative pharmacokinetic study of berberine and palmatine after oral administration of Rhizoma Coptidis extract (96 mg/kg, containing berberine 22 mg/kg and palmatine 5 mg/kg based on body weight) was performed in normal and postinflammation irritable bowel syndrome (PI-IBS) rats, induced by intracolonic instillation of acetic acid and restraint stress. Quantification of berberine and palmatine in rat plasma was achieved by using a sensitive and rapid UPLC-MS/MS method. Plasma samples were collected at 13 different time points and the pharmacokinetic parameters were analyzed by WinNonlin software. The significant differences in the pharmacokinetic behaviors, such as C max⁡, AUC(0–t), V d/F, and CL/F, of berberine and palmatine were found between normal and PI-IBS model rats. The results indicated that PI-IBS pathological conditions in rats could alter the pharmacokinetic behavior of drug. Preclinical pharmacokinetic studies are usually carried out on healthy animals. However, we should pay more attention to the fact that the change of pharmacokinetic behavior plays an important role on efficacy. It is essential to investigate the pharmacokinetics of the drug in disease status.

Ameliorative effects of atractylodin on intestinal inflammation and co-occurring dysmotility in both constipation and diarrhea prominent rats

“…CP and DP rat models were used in preclinical studies [273637]. In the present study, whether CP and DP models were successfully established was confirmed by analysis of the following parameters: granules/moisture contents of feces, jejunal contractility, and jejunal inflammation.…”

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.…”

Artesunate-tinospora combination treatment decreases nuclear factor kappa-B and intercellular adhesion molecule-1 expression in mouse malarial models

“…(22) In a previous study, the in vivo antimalarial effect of T. crispa extract at a dose of 80 mg/kg/ day showed inhibitory activity on the growth of P.yoelii. (23) In another study, a methanolic extract of T. crispa stems had in vitro anti-plasmodial activity against P. falciparum strain 3D7 with IC 50 values between 0.27 mg/ml and 0.29 mg/ml, while the effective inhibitory dose was 2.0 mg/ml, at which dose the parasitemia decreased to 7.62% and 5.85% after 48 and 72 hours, respectively, resulting in a mean reduction of parasitemia degree by 47.12% and 56.83%, respectively.…”