Pharmacokinetics in rats and tissue distribution in mouse of berberrubine by UPLC-MS/MS

Wang, Xianqin; Wang, Shuanghu; Ma, Jianshe; Ye, Tao; Lü, Min; Fan, Min; Deng, Mingjie; Hu, Lufeng; Gao, Zhimou

doi:10.1016/j.jpba.2015.07.031

Cited by 49 publications

(19 citation statements)

References 20 publications

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“…A variety of sample preparation techniques have been applied in a bioanalytical method such as protein precipitation, liquid-liquid extraction, and solid-phase extraction [32]. Among these, the most widely used are protein precipitation and liquid-liquid extraction followed by solid-phase extraction which are used in different category such as antibiotic [33][34][35][36][37][38][39][40], anticancer [36,[41][42][43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58][59][60][61][62], antiviral [63][64][65][66][67], antifungal [68][69][70][71][72], cardiovascular [73][74][75][76][77]…”

Section: Application Of Uhplc-ms/msmentioning

confidence: 99%

Ultra-high performance liquid chromatography-MS/MS (UHPLC-MS/MS) in practice: analysis of drugs and pharmaceutical formulations

et al. 2019

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Background: UHPLC-MS/MS is connected in various research facilities for the qualitative and quantitative investigation of a pharmaceutical substance, pharmaceutical items, and biological specimen. Main body: The commence review article is an endeavor to offer pervasive awareness around assorted aspects and details about the UHPLC-MS/MS and related techniques with the aim on practice to an estimation of medicinal active agents in the last 10 years. The article also focused on isolation, separation, and characterization of present impurity in drug and biological samples. Conclusion: Review article compiles a general overview of medicinally important drugs and their analysis with UHPLC-MS/MS. It gives fundamental thought regarding applications of UHPLC-MS/MS for the study on safety limit. The summary of developed UHPLC-MS/MS methods gives a contribution to the future trend and limitations in this area of research.

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Section: Application Of Uhplc-ms/msmentioning

confidence: 99%

Ultra-high performance liquid chromatography-MS/MS (UHPLC-MS/MS) in practice: analysis of drugs and pharmaceutical formulations

et al. 2019

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“…In fact, BRB showed good antibiosis [7] , anti-inflammatory effects [8] , in addition to antioxidant effect on human fibrosarcoma cells [9] and the scavenging effect of reactive oxidative species (ROS) [10] . Pharmacokinetics studies also indicated that BRB had more efficient intestinal absorption and bioavailability than BBR [11] . Glucuronidation is the one of the most common Phase II conjugation reactions in the drug metabolizing system [12] .…”

Section: Introductionmentioning

confidence: 99%

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

et al. 2017

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Berberrubine (BRB) is the primary metabolite of berberine (BBR) that has shown a stronger glucose-lowering effect than BBR in vivo. On the other hand, BRB is quickly and extensively metabolized into berberrubine-9-O-β-D-glucuronide (BRBG) in rats after oral administration. In this study we compared the pharmacokinetic properties of BRB and BRBG in rats, and explored the mechanisms underlying their glucose-lowering activities. C57BL/6 mice with HFD-induced hyperglycemia were administered BRB (50 mg· kg -1 ·d -1 , ig) for 6 weeks, which caused greater reduction in the plasma glucose levels than those caused by BBR (120 mg· kg -1 ·d -1 ) or BRB (25 mg· kg -1 ·d -1 ). In addition, BRB dose-dependently decreased the activity of α-glucosidase in gut of the mice. After oral administration of BRB in rats, the exposures of BRBG in plasma at 3 different dosages (10, 40, 80 mg/kg) and in urine at different time intervals (0-4, 4-10, 10-24 h) were dramatically greater than those of BRB. In order to determine the effectiveness of BRBG in reducing glucose levels, we prepared BRBG from the urine pool of rats, and identified and confirmed it through LC-MS-IT-TOF and NMR spectra. In human normal liver cell line L-O2 in vitro, treatment with BRB or BRBG (5, 20, 50 μmol/L) increased glucose consumption, enhanced glycogenesis, stimulated the uptake of the glucose analog 2-NBDG, and modulated the mRNA levels of glucose-6-phosphatase and hexokinase. However, both BBR and BRB improved 2-NBDG uptake in insulin-resistant L-O2 cells, while BRBG has no effect. In conclusion, BRB exerts a stronger glucose-lowering effect than BBR in HFD-induced hyperglycemia mice. Although BRB significantly stimulated the insulin sensitivity and glycolysis in vitro, BRBG may have a greater contribution to the glucose-lowering effect because it has much greater system exposure than BRB after oral administration of BRB. The results suggest that BRBG is a potential agent for reducing glucose levels.

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“…The pharmacokinetic parameters, including maximal plasma concentration (C max ), the time to peak plasma concentration (T max ), the area under the plasma concentration-time curve (AUC), the elimination half-life (t 1/2 ) and the mean residence time (MRT), were analyzed using DAS (Drug and Statistics) software (Version 3.2.8, The People's Hospital of Lishui, China). [12][13][14] All the pharmacokinetic parameters are expressed as the mean ± SD. The GraphPad (version 7.0; GraphPad Software Inc., San Diego, CA, USA) was applied to calculate IC 50 values and plot plasma concentration-time curves.…”

Section: Discussionmentioning

confidence: 99%

Effects of avitinib on the pharmacokinetics of osimertinib in vitro and in vivo in rats

Jiang

Wang

et al. 2020

Thoracic Cancer

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Background: Avitinib is one type of the third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) for the treatment of nonsmall cell lung cancer (NSCLC) with EGFR mutations. The purpose of this study was to investigate the effect of avitinib on the pharmacokinetics of osimertinib, one FDA approved third-generation TIKI, both in vitro and in vivo. Methods: The in vitro metabolic stability and inhibitory effect of avitinib on osimertinib were assessed with rat liver microsomes (RLM) to determine its IC 50 values. For the in vivo study, 18 Sprague-Dawley rats were randomly divided into three groups: the avitinib multiple dose group (30 mg/kg avitinib once daily for seven days), the avitinib single dose group (PEG200 once daily for six days and a dose of 30 mg/kg avitinib in PEG200 on day 7) and the control group (equal amounts of PEG200 once daily for seven days). Next, all rats were given osimertinib at a dosage of 10 mg/kg. UPLC/MS-MS was used for the determination of the concentration of osimertinib in plasma. Results: In vitro analysis revealed that the IC 50 value of osimertinib in rat liver microsomes was 27.6 μM. When rats were pretreated with avitinib, the values of AUC and MRT of the osimertinib were increased, and its C max and T max were significantly extended, whereas the values of CLz/F were significantly decreased (P < 0.05). Conclusions: Both in vitro and in vivo results demonstrated that a drug-drug interaction between avitinib and osimertinib occurred and more attention should be paid when avitinib and osimertinib are synchronously administered in clinic.

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Pharmacokinetics in rats and tissue distribution in mouse of berberrubine by UPLC-MS/MS

Cited by 49 publications

References 20 publications

Ultra-high performance liquid chromatography-MS/MS (UHPLC-MS/MS) in practice: analysis of drugs and pharmaceutical formulations

Ultra-high performance liquid chromatography-MS/MS (UHPLC-MS/MS) in practice: analysis of drugs and pharmaceutical formulations

In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine

Effects of avitinib on the pharmacokinetics of osimertinib in vitro and in vivo in rats

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