ABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Radix astragali (RA) was the most frequently used traditional Chinese medicine (TCM) according to the statistics on 52 anti-diabetic formulas recorded in New National Traditional Chinese Medicine; it was employed in 34 out of the 52 formulas. The aim of this study was to elucidate potential pharmacokinetic interaction between RA and pioglitazone, and to provide guidance for clinical medicine safety. MATERIALS AND METHODS: A specific and rapid UPLC-MS/MS method was established to quantify pioglitazone in rat plasma. Then healthy and type 2 diabetes mellitus (T2DM) rats were each divided into control and RA decoction (RAD) administration groups-healthy, healthy-RAD, T2DM, T2DM-RAD; pharmacokinetics of pioglitazone was carried out after RAD was administrated to rats for 7 days. RESULTS: The established UPLC-MS/MS method was rapid, specific, and precise. Between healthy and healthy-RAD groups, half-life (T(1/2)), area under the curve (AUC (0-t)), Vz/F, and Cl/F showed mild yet statistically significant differences; no significant difference for any above parameter was detected between T2DM and T2DM-RAD groups. CONCLUSION: RAD co-administration did not affect the pharmacokinetics of pioglitazone especially in diabetic groups; RA and pioglitazone might be feasible herb-drug co-effectiveness.
Subject(s)
Drugs, Chinese Herbal/pharmacology , Herb-Drug Interactions , Hypoglycemic Agents/pharmacokinetics , Thiazolidinediones/pharmacokinetics , Animals , Astragalus Plant , Astragalus propinquus , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 2/metabolism , Male , Pioglitazone , Rats , Rats, WistarABSTRACT
BACKGROUND: Dahuang Huanglian Xiexin Decoction (DHXD) is a classical formula in traditional Chinese medicines. In this study, a novel UPLC-MS/MS method was developed for the simultaneous quantification of rhein, emodin, berberine and baicalin, the major bioactive compounds of DHXD in rat plasma. RESULTS: The method possessed high sensitivity and ultrashort analysis time (7 min). Linearity, accuracy, precision and extraction recovery of four analytes were all satisfactory. The method was then successfully applied in a pharmacokinetic study of four bioactive components after a single oral administration of DHXD extract to rats. CONCLUSION: The method was applicable for simultaneous bioanalysis of rhein, emodin, berberine and baicalin.
Subject(s)
Anthraquinones/blood , Berberine/blood , Chromatography, High Pressure Liquid/methods , Emodin/blood , Flavonoids/blood , Tandem Mass Spectrometry/methods , Animals , Anthraquinones/pharmacokinetics , Berberine/pharmacokinetics , Colonic Diseases, Functional/drug therapy , Drugs, Chinese Herbal/pharmacokinetics , Emodin/pharmacokinetics , Flavonoids/pharmacokinetics , Medicine, Chinese Traditional , Plasma/chemistry , Rats , Reproducibility of Results , Sensitivity and Specificity , Statistics, NonparametricABSTRACT
A novel, simple and rapid ultraperformance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) assay was established for quantification of saxagliptin in rat plasma. Plasma samples were processed by liquid-liquid extraction with ethyl acetate and chromatographed on a C18 column (2.1 × 50 mm i.d., 1.7 µm). The mobile phase consisted of methanol and 0.1% formic acid (40:60, v/v). Multiple reaction monitoring transitions were performed for detection in positive-ion mode with an electrospray ionization source. The calibration curve was linear over the concentration range of 0.5-100 ng/mL (R² > 0.99). All accuracy values were between 90.62 and 105.60% relative error and the intra- and inter-day precisions were less than 9.66% relative standard deviation. Extraction recovery was more than 81.01% and the matrix effect ranged from 90.27 to 109.15%. After validation, the method was applied to a pharmacokinetic study where healthy rats were orally given 0.5 mg/kg saxagliptin.
