PHARMACEUTICAL RESEARCH
·
2025
·
IF 4.3
Bai Wanting,Li Yang,You Feng,Duan Xiaoyan,Hu Jiahuan,Wu Jinjin,Sun Tao,Wang Xing,Lan Pei,Hu Jinping
Objective Bicyclol, a hepatoprotective agent, is often used in combination with other drugs for liver diseases, including drug-induced liver injury (DILI), raising concerns about potential drug-drug interactions (DDIs). This study investigates the interaction between bicyclol and key transporters (OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, MATE2-K, P-gp, BCRP, BSEP) to predict transporter-related DDI risks. Methods Transporter interaction studies were conducted using cell lines or membrane vesicles overexpressing human uptake and efflux transporters. The substrate and inhibitory potential of bicyclol were systematically evaluated through transport and inhibition assays. The static model and criteria were applied to assess the risk of transporter-related DDIs in vivo . Results Bicyclol was not a substrate of above-mentioned transporters. Regarding inhibition, it was not an inhibitor of OATP1B1, OATP1B3, OAT1, OAT3, MATE1, MATE2-K, or BSEP (IC 50 s > 100 μM). However, it was a marginal inhibitor of OCT2 (IC 50 = 76.2 μM), a weak inhibitor of P-gp (IC 50 = 123 μM), and a strong inhibitor of BCRP (IC 50 = 8.5 μM). The static model predicted that only BCRP would be inhibited in vivo by bicyclol, suggesting dose optimization might be required for BCRP substrates. Conclusions Here, we systematically elucidated the substrate and inhibition potential of bicyclol on major human drug transporters for the first time, which may provide the basis for rational co-administration of bicyclol, potentially broadening its clinical application.
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Analytical Methods
·
2026
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IF 2.6
lidi Gao,Jiawen Yu,Dongsheng Zhao,Xinyu Liang,Jun Wang,Fuquan Zhao,Ming Zhao,Hongtao Chu,Shili Qin
In this work, a novel Ti-based MOF (NH2-MIL-125) bonded open-tubular (OT) column was firstly prepared via one-step in-situ growth method for capillary electrochromatography (CEC). The stationary phase was characterized by Fourier transform-infrared spectroscopy, scanning electron microscopy, X-ray diffraction spectroscopy, and nitrogen adsorption-desorption measurements. The results showed that the stationary phase exhibited a large specific surface area (1247.57 m²/g) with microporous and mesoporous structure and no obvious changes in the morphology/size inside and outside the column. Baseline separation of three β-adrenergic receptor blockers (Prop, Sot, and Lab), three β-adrenergic receptor agonists, and four sulfonamide antibiotics were obtained under the optimized CEC conditions with the shortest analysis time of 2.52 min and a maximum resolution of 11.52. The separation mechanisms were mainly attributed to polarity and electrophoretic mobility of the analytes, as well as π-π interactions and hydrogen bonding interaction between the stationary phase and the analytes. A quantitative detection method of three β-adrenergic receptor blockers in pork samples was established using the NH2-MIL-125 bonded OT column. Good linearity (R² > 0.999) was obtained over the concentration range of 0.01-1.00 mg/mL with limits of detection of 0.0044-0.0084 mg/mL and recoveries of 90.27-106.74%. Thus, the developed method was simple, rapid and high efficiency, and could be applied for the simultaneous separation and detection of the three β-adrenergic receptor blockers in real samples.
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Analytical Methods
·
2019
·Vol. 12
·期 2
·141-148
·
IF 2.378
Xue Ren,Man He,Beibei Chen,Bin Hu
Herein, magnetic porous organic polymers (MOPs) prepared via an azo coupling reaction in water under mild conditions are evaluated for the extraction of seven cardiovascular drugs, including xylocaine, metoprolol, mexiletine, labetalol, propranolol, carvedilol and propafenone, from human urine samples for the first time. The extraction mechanisms are assumed to be electrostatic interaction and π–π stacking. The MOPs exhibited fast adsorption/desorption time (13 min) and high enrichment factors (315–365-fold) for target analytes. Based on this, a method coupling magnetic solid phase extraction with HPLC-UV detection was developed for the analysis of cardiovascular drugs. Under the optimized conditions, the LODs (S/N = 3) were in the range of 0.06–0.57 μg L−1 with an RSD (n = 5) of 4.3–8.6%, and the linear range was 0.2–200 μg L−1 for propranolol, 2–200 μg L−1 for metoprolol, and 0.5–200 μg L−1 for the other five analytes. The developed method was applied for the analysis of cardiovascular drugs in urine samples with recoveries of 89.0–112%. In order to further evaluate the application potential of this method, real-time monitoring of metoprolol in urine samples collected from volunteers treated with metoprolol tablets was performed. The proposed method is simple, fast, and sensitive and has good potential in the monitoring of cardiovascular drugs in competitive sports and clinical analysis.
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JOURNAL OF CHROMATOGRAPHY A
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2016
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IF 3.926
Wenying Fan,Man He,Linna You,Xuewei Zhu,Beibei Chen,Bin Hu
Due to the high selectivity and stability, molecularly imprinted polymers (MIPs) have been successfully applied in stir bar sorptive extraction (SBSE) as a special coating to improve the selective extraction capability for target analytes. However, traditional MIPs usually suffer from incompatibility in aqueous media and low adsorption capacity, which limit the application of MIP coated stir bar in aqueous samples. To solve these problems, a water-compatible graphene oxides (GO)/MIP composite coated stir bar was prepared in this work by in situ polymerization. The prepared water-compatible GO/MIP coated stir bar presented good mechanical strength and chemical stability, and its recognition ability in aqueous samples was improved due to the polymerization of MIP in water environment, the adsorption capacity for target analytes was also increased by the addition of GO in MIP pre-polymer solution. Based on it, a method of water-compatible GO/MIP coated stir bar sorptive extraction combined with high performance liquid chromatography-ultraviolet detector (HPLV-UV) was proposed for the analysis of propranolol (PRO) in aqueous solution. The influencing factors of SBSE, such as sample pH, salt effect, stirring rate, extraction time, desorption solvent and desorption time, were optimized, and the analytical performance of the developed SBSE-HPLC-UV method was evaluated under the optimized conditions. The limit of detection (LOD) of the proposed method for PRO was about 0.37 μg L −1 , and the enrichment factor (EF) was 59.7-fold (theoretical EF was 100-fold). The reproducibility was also investigated at concentrations of 5 μg L −1 and the relative standard deviation (RSD) was found to be 7.3% (n = 7). The proposed method of GO/MIP coating-SBSE-HPLC-UV was successfully applied for the assay of the interested PRO drug in urine samples, and further extended to the investigation of the excretion of the drugs by monitoring the variation of the concentration of PRO in urine within 10 h after drug-taking.
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2024
·
IF 4.3
Yuxin He,Hanting Wang,Yuting Yan,Xinhui Jiang,Hecun Zou,Zhengwei Zhang
Gefitinib, a highly significant antitumor drug, is now commonly employed in clinical settings as a first-line treatment for patients with advanced or metastatic non-small cell lung cancer, colon cancer, and breast cancer. Herein, a convenient, rapid, and accurate fluorescence method based on nitrogen-doped carbon dots (NCDs) was designed for ultrasensitive detection of gefitinib. The NCDs were easily synthesized through one-pot hydrothermal process using p -phenylenediamine and D-glutamic acid as the precursors. The sensing strategy relied on the fluorescence of NCDs at 345 nm, which was selectively reduced by gefitinib based on the inner filter effect (IFE). With a broad linear range of 0.025–30 μg/mL and a low limit of detection of 5.5 ng/mL, the probe was successfully applied to the detection of gefitinib in human serum samples, demonstrating strong practicality, affordability, and high accuracy. The proposed sensor is simple in design, fast in detection and cost-effective, and exhibits promising application in drug real-time analysis.
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CHROMATOGRAPHIA
·
2024
·
IF 1.2
Xiang Yuqian,Huang Yu,Yan Xiaohui,Zhu Zhipeng,Wu Dapeng,Gao Peng,Li Jiulong
In this work, in order to investigate retention and selectivity mechanism on hydrophilic interaction liquid chromatography (HILIC), one of the most common hydrophilic stationary phases, polyethylene glycols (PEG) of different molecular weights (200, 400, 800 and 2000 Dalton) were covalently bonded to porous silica spheres via isocyanate silane. The PEG stationary phase was then characterized in detail by infrared spectroscopy, scanning electron microscope, nitrogen adsorption–desorption isotherms, and thermogravimetric analysis, and the PEG bonding density was determined as 2.7, 2.3, 1.4, 0.26 μmol m −2 , respectively. The HILIC retention mechanism was systematically conducted by quantitative evaluation of the effect of partitioning and adsorption, hydrogen bonding and hydrophilicity, and temperature on the retention of nucleosides and nucleobases. It was found that the retention was highly relevant on the partitioning, hydrogen bonding between solutes and PEG, and strong electrostatic interactions (attractive/repulsive) between solutes and silica. To further assess the separation performance, three kinds of polar compounds (nucleosides and nucleobases, organic acids and β-blockers) were chosen as probe compounds. Among the four PEG stationary phases, it was found that the higher PEG ligand density generally resulted into more superior separation performance to these polar compounds, that is, PEG200-bonded stationary phase with highest ligand density of 2.7 μmol m −2 generated better resolution. Furthermore, higher ligand bonding mass would increase the retention of nucleosides, nucleobases and organic acids except β-blockers. Generally, the HILIC stationary phase with continuous and dense hydrophilic layer is beneficial to the separation of polar analytes. Graphical Abstract
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危险品化学品经营许可证（带存储）