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  1. Article: Pharmacokinetic comparison of sitagliptin and metformin HCl extended-release tablets versus JANUMET

    Que, Linling / Qin, Wei / Shi, Yunfei / Ding, Ying / Huang, Kai / Qian, Zhenzhong / Huang, Bingjie / Zhou, Peipei / He, Qing

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1105767

    Abstract: Background and Objectives: ...

    Abstract Background and Objectives:
    Language English
    Publishing date 2023-03-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1105767
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Corrigendum: Pharmacokinetics and bioequivalence study of esomeprazole magnesium enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions.

    Ding, Ying / Chu, Nannan / Que, Linling / Huang, Kai / Chen, Yuanxing / Qin, Wei / Qian, Zhenzhong / Shi, Yunfei / Xu, Zhen / He, Qing

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1217008

    Abstract: This corrects the article DOI: 10.3389/fphar.2023.1169103.]. ...

    Abstract [This corrects the article DOI: 10.3389/fphar.2023.1169103.].
    Language English
    Publishing date 2023-06-01
    Publishing country Switzerland
    Document type Published Erratum
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1217008
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  3. Article: Pharmacokinetics and bioequivalence study of esomeprazole magnesium enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions.

    Ding, Ying / Chu, Nannan / Que, Linling / Huang, Kai / Chen, Yuanxing / Qin, Wei / Qian, Zhenzhong / Shi, Yunfei / Xu, Zhen / He, Qing

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1169103

    Abstract: Objective: ...

    Abstract Objective:
    Language English
    Publishing date 2023-04-28
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1169103
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  4. Article: LZM008, a proposed tocilizumab biosimilar: Pharmacokinetics, safety, and immunogenicity profiles compared with ACTEMRA

    Cao, Guoying / Wang, Jingjing / He, Jinjie / Hu, Yingying / Yang, Haijing / Que, Linling / Gu, Xianghong / Yu, Jicheng / Wu, Xiaojie / Wu, Jufang / Fang, Wei / He, Qing / Zhang, Jing

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1111893

    Abstract: Background: ...

    Abstract Background:
    Language English
    Publishing date 2023-04-04
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1111893
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  5. Article ; Online: Evaluation of Acarbose Bioequivalence in Healthy Chinese Populations Using Novel Pharmacodynamic End Points.

    Que, Linling / Qian, Zhenzhong / Xiang, Xuemei / Ding, Ying / Huang, Kai / Bai, Yichuan / Zhao, Huanan / He, Qing

    Clinical pharmacology in drug development

    2024  Volume 13, Issue 3, Page(s) 233–239

    Abstract: Acarbose is a widely used α-glucosidase inhibitor for the management of postprandial hyperglycemia in patients with type 2 diabetes mellitus. Recent pilot studies on acarbose bioequivalence (BE) have successfully identified additional pharmacodynamic (PD) ...

    Abstract Acarbose is a widely used α-glucosidase inhibitor for the management of postprandial hyperglycemia in patients with type 2 diabetes mellitus. Recent pilot studies on acarbose bioequivalence (BE) have successfully identified additional pharmacodynamic (PD) parameters as valid end points. Nevertheless, there was a scarcity of published pivotal studies using novel PD parameters. The purpose of the study is to investigate the acarbose BE using the new PD parameters. The study was conducted with an open, randomized, 2-period crossover design. A total of 64 healthy Chinese volunteers received either the reference (R) or test (T) acarbose at a dose of 2×50 mg orally, followed by a 1-week washout period. After sucrose treatment (baseline) and sucrose/acarbose co-administration, serum glucose, and insulin concentrations were assessed. The rectifying approach yielded geometric mean ratios of 102.9% for maximum serum glucose concentration with deduction of glucose concentration at 0 hour and 105.3% for the area under the serum glucose concentration-time curve profile 0-2 hours after coadministration of sucrose and acarbose with deduction of baseline (AUC
    MeSH term(s) Humans ; Acarbose ; China ; Diabetes Mellitus, Type 2/drug therapy ; Glucose ; Sucrose ; Therapeutic Equivalency
    Chemical Substances Acarbose (T58MSI464G) ; Glucose (IY9XDZ35W2) ; Sucrose (57-50-1)
    Language English
    Publishing date 2024-01-10
    Publishing country United States
    Document type Randomized Controlled Trial ; Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2649010-9
    ISSN 2160-7648 ; 2160-763X
    ISSN (online) 2160-7648
    ISSN 2160-763X
    DOI 10.1002/cpdd.1362
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  6. Article ; Online: Clinical Significance of Peptidase M20 Domain Containing 1 Ii Patients with Carotid Atherosclerosis.

    Huang, Xincheng / He, Peiyuan / Wu, Linling

    Arquivos brasileiros de cardiologia

    2022  Volume 119, Issue 3, Page(s) 372–379

    Abstract: Background: Atherosclerosis is the main cause for most cardiovascular diseases, and new biomarkers for this condition are always needed. Peptidase M20 domain containing 1 (PM20D1) is associated with both lipid metabolism and obesity. However, no study ... ...

    Title translation Significado Clínico do Domínio da Peptidase M20 Contendo 1 em Pacientes com Aterosclerose Carotídea.
    Abstract Background: Atherosclerosis is the main cause for most cardiovascular diseases, and new biomarkers for this condition are always needed. Peptidase M20 domain containing 1 (PM20D1) is associated with both lipid metabolism and obesity. However, no study focuses on the role of PM20D1 in carotid atherosclerosis.
    Objective: The present study aimed to investigate the role of PM20D1 in carotid atherosclerosis patients.
    Methods: The present prospective observational study contained a total of 231 carotid atherosclerosis patients, who went to our department between July 2018 and December 2019. Blood samples and medical characteristics were also obtained from 231 healthy individuals with the same body mass index distribution of carotid atherosclerosis patients. Serum PM20D1 was determined using enzyme-linked immunosorbent assay. Clinical and demographic characteristics of all patients were collected, including age, sex, body mass index and medical history. Levels of C-reactive protein, tumor necrosis factor, homocysteine, as well as total cholesterol, triglyceride, high-density leptin cholesterol and low-density leptin cholesterol were recorded. Statistical analysis was conducted using the SPSS software, with p<0.05 as statistically different.
    Results: Serum PM20D1 levels were markedly lower in carotid atherosclerosis patients when compared to the healthy control, which were significantly lower in severe carotid atherosclerosis patients and carotid atherosclerosis/stroke patients. Patients with unstable plaques showed markedly lower PM20D1 when compared to patients with stable plaques. No significant difference was found among carotid atherosclerosis patients with different body mass index. Patients with higher PM20D1 levels showed significantly lower expression of C-reactive protein, tumor necrosis factor, homocysteine, triglyceride, total cholesterol and low-density leptin cholesterol. PM20D1 was negatively correlated with C-reactive protein, tumor necrosis factor, homocysteine, total cholesterol and low-density leptin cholesterol in carotid atherosclerosis patients, and could be used as a biomarker for severe carotid atherosclerosis patients or carotid atherosclerosis patients with stroke. Sex, tumor necrosis factor, homocysteine and PM20D1 were risk factors for carotid atherosclerosis.
    Conclusion: PM20D1 was decreased in carotid atherosclerosis patients and was associated with severity, plaque stability, and levels of C-reactive protein, tumor necrosis factor, homocysteine, triglyceride, total cholesterol and low-density leptin cholesterol in carotid atherosclerosis patients.
    MeSH term(s) Amidohydrolases ; Biomarkers ; C-Reactive Protein ; Carotid Artery Diseases ; Cholesterol ; Homocysteine ; Humans ; Leptin ; Peptide Hydrolases ; Plaque, Atherosclerotic ; Risk Factors ; Stroke/complications ; Triglycerides ; Tumor Necrosis Factors
    Chemical Substances Biomarkers ; Leptin ; Triglycerides ; Tumor Necrosis Factors ; Homocysteine (0LVT1QZ0BA) ; C-Reactive Protein (9007-41-4) ; Cholesterol (97C5T2UQ7J) ; Peptide Hydrolases (EC 3.4.-) ; Amidohydrolases (EC 3.5.-) ; PM20D1 protein, human (EC 3.5.-)
    Language Portuguese
    Publishing date 2022-09-21
    Publishing country Brazil
    Document type Journal Article ; Observational Study
    ZDB-ID 730261-7
    ISSN 1678-4170 ; 0066-782X
    ISSN (online) 1678-4170
    ISSN 0066-782X
    DOI 10.36660/abc.20210799
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  7. Article ; Online: Targeting the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual screening and pharmacological evaluation.

    Gan, Linling / Yang, Ying / Liang, Zizhen / Zhang, Maojie / He, Yun / Zhang, Shao-Lin

    European journal of medicinal chemistry

    2023  Volume 264, Page(s) 116008

    Abstract: Proliferating cancer cells are characterized by the Warburg effect, a metabolic alteration in which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation. The pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/ ... ...

    Abstract Proliferating cancer cells are characterized by the Warburg effect, a metabolic alteration in which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation. The pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis plays a crucial role in this effect and has been identified as a potential target for anticancer drug development. Herein, we present the discovery and pharmacological evaluation of potent PDK inhibitors targeting the PDK/PDC axis. We successfully identified 6 compounds from a small molecule library through a structure-based virtual screening campaign and evaluated their enzymatic inhibitory potencies for PDK1-4. Our results indicated that compound 1 exhibited submicromolar inhibitory activities against PDK1-3 (IC
    MeSH term(s) Pyruvate Dehydrogenase Acetyl-Transferring Kinase/metabolism ; Protein Serine-Threonine Kinases ; Pyruvate Dehydrogenase Complex/metabolism ; Oxidative Phosphorylation ; Cell Division
    Chemical Substances Pyruvate Dehydrogenase Acetyl-Transferring Kinase ; Protein Serine-Threonine Kinases (EC 2.7.11.1) ; Pyruvate Dehydrogenase Complex
    Language English
    Publishing date 2023-12-03
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.116008
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  8. Article ; Online: Insight into the fracture energy dissipation mechanism in elastomer composites

    He, Dongyi / Cheng, Xiaxia / Wong, Chunyu / Zeng, Xiangliang / Li, Linling / Teng, Chao / Du, Guoping / Zhang, Chenxu / Ren, Linlin / Zeng, Xiaoliang / Sun, Rong

    Physical chemistry chemical physics : PCCP

    2024  Volume 26, Issue 5, Page(s) 4429–4436

    Abstract: Most tough elastomer composites are reinforced by introducing sacrificial structures and fillers. Understanding the contribution of fillers and sacrificial bonds in elastomer composites to the energy dissipation is critical for the design of high- ... ...

    Abstract Most tough elastomer composites are reinforced by introducing sacrificial structures and fillers. Understanding the contribution of fillers and sacrificial bonds in elastomer composites to the energy dissipation is critical for the design of high-toughness materials. However, the energy dissipation mechanism in elastomer composites remains elusive. In this study, using a tearing test and time-temperature superposition, we investigate the effect of fillers and sacrificial bonds on the energy dissipation of elastomer composites consisting of poly(lipoic acid)/silver-coated Al fillers. We found that the fillers and sacrificial bonds mutually enhance both the intrinsic fracture energy and the bulk energy dissipation, and moreover the sacrificial bonds play a more important role in enhancing fracture toughness than the fillers. It is unreasonable to rely solely on the loss factor for bulk energy dissipation. The addition of sacrificial bonds results in a chain segment experiencing greater binding force compared to the addition of fillers. This suggests that the chain segment consumes more energy during its movement. By calculating the length of the Kuhn chain segment and the Kuhn number, it is evident that the addition of sacrificial bonds results in a greater binding force for the chain segment than the addition of fillers, and this enhanced binding force increases the energy consumption during the motion of the chain segment.
    Language English
    Publishing date 2024-01-31
    Publishing country England
    Document type Journal Article
    ZDB-ID 1476244-4
    ISSN 1463-9084 ; 1463-9076
    ISSN (online) 1463-9084
    ISSN 1463-9076
    DOI 10.1039/d3cp04695h
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  9. Article: The effect of food on the pharmacokinetics of WXFL10203614, a potential selective JAK1 inhibitor, in healthy Chinese subjects.

    Huang, Kai / Shi, Yunfei / Chu, Nannan / Que, Linling / Ding, Ying / Qian, Zhenzhong / Qin, Wei / Gu, Xianghong / Wang, Jiakun / Zhang, Zhiwei / Xu, Jianguo / He, Qing

    Frontiers in pharmacology

    2022  Volume 13, Page(s) 1066895

    Abstract: Objective: ...

    Abstract Objective:
    Language English
    Publishing date 2022-11-24
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2022.1066895
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  10. Article ; Online: No apparent pharmacokinetic interactions were found between henagliflozin: A novel sodium-glucose co-transporter 2 inhibitor and glimepiride in healthy Chinese male subjects.

    Que, Linling / Huang, Kai / Xiang, Xuemei / Ding, Ying / Chu, Nannan / He, Qing

    Journal of clinical pharmacy and therapeutics

    2022  Volume 47, Issue 8, Page(s) 1225–1231

    Abstract: What is known and objective: Henagliflozin is a novel selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with similar inhibitory effect to ertugliflozin. Glimepiride is widely used to treat type 2 diabetes mellitus (T2DM) with few ... ...

    Abstract What is known and objective: Henagliflozin is a novel selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with similar inhibitory effect to ertugliflozin. Glimepiride is widely used to treat type 2 diabetes mellitus (T2DM) with few cardiovascular side effects. In the present study, we aimed at evaluating the pharmacokinetic (PK) interactions between henagliflozin and glimepiride.
    Methods: An open-label, single-centre, single-arm, 3-period, 3-treatment, self-control study was conducted in twelve healthy Chinese male subjects. During each study period, subjects received a single oral dose of glimepiride 2 mg, multiple oral doses of henagliflozin 10 mg or a combination of the two drugs. Serial blood samples were collected 24 h post-dosing for PK analyses. Finger-tip blood glucose was also tested for safety evaluation.
    Results and discussion: Co-administration of henagliflozin with glimepiride did not affect their plasma PK profiles. For henagliflozin, the 90% confidence intervals for the geometric mean ratio (GMR) for the maximum plasma concentrations at steady-state (C
    What is new and conclusion: Multiple doses of henagliflozin did not exert a significant change on glimepiride PK profiles and a single dose of glimepiride had little effect on henagliflozin blood concentration. Thus, henagliflozin can be co-administered with glimepiride without dose adjustment of either drug.
    MeSH term(s) Blood Glucose ; Bridged Bicyclo Compounds, Heterocyclic/pharmacokinetics ; China ; Drug Interactions ; Healthy Volunteers ; Humans ; Male ; Sodium-Glucose Transporter 2 Inhibitors/pharmacokinetics ; Sulfonylurea Compounds/pharmacokinetics
    Chemical Substances Blood Glucose ; Bridged Bicyclo Compounds, Heterocyclic ; Sodium-Glucose Transporter 2 Inhibitors ; Sulfonylurea Compounds ; henagliflozin (21P2M98388) ; glimepiride (6KY687524K)
    Language English
    Publishing date 2022-03-31
    Publishing country England
    Document type Clinical Study ; Journal Article
    ZDB-ID 639006-7
    ISSN 1365-2710 ; 0269-4727
    ISSN (online) 1365-2710
    ISSN 0269-4727
    DOI 10.1111/jcpt.13659
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