Abstract
Context: Berberine is an active alkaloid isolated from Rhizoma coptidis [Coptis chinensis Franch. (Ranunculaceae)] that is widely used for the treatment of diabetes, hyperlipidemia and hypertension. However, the pharmacokinetics of berberine in normal rats and type 2 diabetes mellitus (T2DM) model rats are not clear.Objective: This study compares the pharmacokinetics of berberine between normal and T2DM model rats.Materials and methods: The T2DM model rats were fed with high fat diet for 4 weeks, induced by low-dose (30 mg/kg) streptozotocin for 72 h and validated by determining the peripheral blood glucose level. Rats were orally treated with berberine at a dose of 20 mg/kg and then berberine concentration in rat plasma was determined by employing a sensitive and rapid LC-MS/MS method.Results: The significantly different pharmacokinetic behaviour of berberine was observed between normal and T2DM model rats. When compared with the normal group, Cmax, t1/2 and AUC(0–t) of berberine were significantly increased in the model group (17.35 ± 3.24 vs 34.41 ± 4.25 μg/L; 3.95 ± 1.27 vs 9.29 ± 2.75 h; 151.21 ± 23.96 vs 283.81 ± 53.92 μg/h/L, respectively). In addition, oral clearance of berberine was significantly decreased in the model group (134.73 ± 32.15 vs 62.55 ± 16.34 L/h/kg).Discussion and conclusion: In T2DM model rats, the pharmacokinetic behaviour of berberine was significantly altered, which indicated that berberine dosage should be modified in T2DM patients.
Highlights
Diabetes mellitus is one kind of metabolic syndromes characterized by chronic hyperglycemia (Atkinson & Maclaren 1994; Ismail-Beigi 2012)
This study compares the pharmacokinetics of berberine between normal and type 2 diabetes mellitus (T2DM) model rats
Materials and methods: The T2DM model rats were fed with high fat diet for 4 weeks, induced by lowdose (30 mg/kg) streptozotocin for 72 h and validated by determining the peripheral blood glucose level
Summary
Diabetes mellitus is one kind of metabolic syndromes characterized by chronic hyperglycemia (Atkinson & Maclaren 1994; Ismail-Beigi 2012). Diabetes cases fall into two broad pathogenetic categories: type I and type II diabetes mellitus (T1DM and T2DM) (Tan & Cheah 1990; Hu 2011). T2DM, which is previously referred to as noninsulin-dependent diabetes mellitus, accounts for approximately 90% of the diabetes patients (AlAmer et al 2015; Tangvarasittichai 2015). One of the significant features of diabetes mellitus is lipid metabolism malfunction, which results in hyperlipidemia (Moest et al 2013). In the current clinical treatment, western medicines are extensively used to control hyperglycaemia, hyperlipidaemia and insulin resistance of type 2 diabetes mellitus, such as sulfonylurea, biguanides, thiazolidinediones and glycosidase inhibitors (Shankar et al 2015). The clinical efficacy of these drugs in T2DM treatment is limited and these drugs are very expensive
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