1.Limited sampling strategy to estimate pharmacokinetic parameters of orally administered metformin hydrochloride.
Lifang CHEN ; Jianjie JIAO ; Caili ZHANG ; Jianshi LOU ; Changxiao LIU
Acta Pharmaceutica Sinica 2010;45(12):1533-6
The present study was to estimate pharmacokinetic parameters of metformin hydrochloride in 20 Chinese healthy volunteers with a limited sampling strategy (LSS), which will provide scientific data for bioequivalence and clinical application. A single dose of metformin was administrated to 20 healthy volunteers. The concentration of metformin in whole blood was determined by validated high performance liquid chromatography (HPLC) method. Multi-linear regression analysis was performed to establish a model to estimate AUC(0-24 h) and Cmax of metformin by LSS method. The LSS models were validated by the Jackknife method. The result indicated: the linearity relationship between AUC(0-24 h) or Cmax and single concentration point was poor. Several models for metformin AUC(0-24 h) or Cmax, estimation were better (r2 > 0.9, P < 0.05). Validation tests indicated that most informative sampling points (C2, C6 for AUC(0-24 h), C1.5, C2 for Cmax) provided accurate estimations of these parameters. So, a multi-linear regression model for estimation pharmacokinetic parameters of metformin by using LSS method is feasible.
2.Key Techniques and Application Progress of Molecular Pharmacognosy
Xuefeng XIAO ; Jing HU ; Haiyu XU ; Wenyuan GAO ; Tiejun ZHANG ; Changxiao LIU
Chinese Herbal Medicines 2011;03(2):106-116
At the boundary between pharmacognosy and molecular biology, molecular pharmacognosy has developed as a new borderline discipline. This paper reviews the methods, application, and prospect of molecular pharmacognosy. DNA marker is one of genetic markers and some molecular marker methods which have been successfully used for genetic diversity identification and new medicinal resources development. Recombinant DNA technology provides a powerful tool that enables scientists to engineer DNA sequences. Gene chip technique could be used in determination of gene expression profiles, analyses of polymorphisms, construction of genomic library, analysis of mapping, and sequencing by hybridization. Using the methods and theory of molecular biology and pharmacognosy, molecular pharmacognosy represents an extremely prospective branch of pharmacognosy and focuses on the study of systemic growth of medicinal plants, identification and evaluation of germplasm resources, plant metabolomics and production of active compounds. Furthermore, the great breakthrough of molecular pharmacognosy could be anticipated on DNA fingerprint analysis, cultivar improvement, DNA identification, and a global DNA barcoding system in the future.
3.Effects of Shenmai Injection on serum concentration and pharmacokinetics of digoxin in dogs with heart failure.
Jingyuan MAO ; Changxiao LIU ; Henghe WANG ; Guangli WEI ; Zhenpeng ZHANG ; Jie XING ; Xianliang WANG ; Yingfei BI
Journal of Integrative Medicine 2010;8(11):1070-4
To explore the effects of Shenmai Injection (SMI), a compound traditional Chinese herbal medicine, on pharmacokinetics and serum concentration of digoxin when applied together with digoxin.
4.Inhibition of berberine on organ anion transporters and its bidirectional trans-membrane transport
Weidang WU ; Xingyan ZHANG ; Zihong WEI ; Xiaoyan CI ; Lixin JIANG ; Jiangjie LU ; Changxiao LIU ; Xiulin YI
Drug Evaluation Research 2017;40(6):778-782
Objective To study the inhibition of berberine on organ anion transporters (OATs) and its bidirectional trans-membrane transport.Method The transgene cell lines of the organ anion transporters including OAT1,OAT2,OAT3,OAT4,OAT7,and URAT1 were constructed and selected by animal cell transgenic method mediated by transporter Lipo 3000.Wild type (WT) cells were used as control group,and activity of OATs was verified by adding their radiolabeled substrates and inhibitors.The inhibition of 100 μmol/L berberine on the transporters was investigated in vitro.The IC50 of berberine on URAT1 was also determined.The bidirectional transport of berberine was studied through the Caco-2 model.Result The results showed that 100 μmol/L berberine inhibited the activity of OAT1,OAT2,OAT3,OAT4,OAT7 and URAT1 to (70.48±4.23)%,(69.13±1.28)%,(72.12±3.28)%,(79.77±6.49)%,(69.51 ±5.99)% and (38.4 ± 2.67)% respectively,the IC50 of berberine to URAT 1 was 13.19 μmol/L,the Papp (A-B) of 50 μmol/L and 100 μmol/L berberine were separately 0.28 × 10-6 and 0.40 × 10-6 cm/s,and the effiux rates were separately 3.18 and 3.15.Conclusion Berberine shows a stronger inhibition to URAT1 compared to OAT1,OAT2,OAT3,OAT4 and OAT7.Berberine may be the substrate of some effiux transporters.This study provides theoretical basis for explaining the low bioavailability ofberberine and forecasting the possible drug-drug interaction.
5.Simultaneous Analysis of Thirteen Bioactive Components in Evodia rutaecarpa and Its Varieties by HPLC-DAD-MS
Haiyu XU ; Tiejun ZHANG ; Xuefeng XIAO ; Ping ZHAO ; Changxiao LIU ; Jun XU
Chinese Herbal Medicines 2010;02(2):112-117,131
Objective To control the quality of Evodia rutaecarpa better. Methods An HPLC-DAD-MS/MS method was established for the rapid and efficient identification of bioactive constituents and for simultaneous quantitative analysis of four bioactive ingredients including evodiamine, rutaecarpine, dehydroevodiamine, and evodin in E.rutaecarpa, which was applied to evaluating eight samples of E. rutaecarpa and its varieties from different areas.Results Thirteen potentially bioactive constituents including one flavonoid glycoside, one limonin, four indoloquinazoline alkaloids, and seven quinolone alkaloids were identified in all samples and the contents of dehydroevodiamine, evodine, evodiamine, and rutaecarpine varied widely from 0.10% to 0.51%, 0.49% to 3.12%,0.07% to 1.56%, and 0.10% to 0.69%, respectively. Conclusion This method is found to be convenient, fast,accurate, and it is facilitated to improve the quality control standard of E. rutaecarpa and related products.
6.Medical data quality analysis and governance countermeasures
Chen ZHANG ; Hong JI ; Changxiao JIN
Chinese Journal of Hospital Administration 2020;36(9):747-750
With the increasing maturity of big data technology, data as an objective indicator of hospital decision-making, its effective application has been paid more and more attention. Data quality will affect the accuracy, pertinence and effectiveness of hospital decision-making. Based on the quality and evaluation of medical data, the authors analyzed the problems existing in data quality, and put forward countermeasures to improve data quality, including improving management system to improve data integrity and standardization, establishing statistical platform system to improve data consistency, establishing data center to improve data integration and governance ability.
7.Five cases of breast reconstruction with pedicled greater omentum metastasis after mastectomy
Guangxu HAO ; Qing ZHONG ; Changxiao ZHAO ; Li DONG ; Yi REN ; Jing ZHANG
Chinese Journal of Endocrine Surgery 2021;15(2):211-214
Immediate breast reconstruction with pedicle great omentum metasasis is safe,easy to perform, and has extensive clinical indications, less postoperative complications. The shape of reconstructed breast is plump and symmetrical, which is the optimal choice for reconstruction surgery with small and medium-sized breast at present. The surgical methods and effects of breast reconstruction with pedicle great omentum metastasis in 5 patients are reported in this article. Combined with the previous literature, the feasibility and safety of surgery is discussed, which provide a reference to clinicians.
8.Early predictors of Mycoplasma pneumoniae necrotizing pneumonia in children
Shuaishuai LIU ; Jing MA ; Zhongxiao ZHANG ; Changxiao LI ; Linlin HAN ; Chen MENG
Chinese Journal of Applied Clinical Pediatrics 2021;36(8):601-604
Objective:To study the early predictors of Mycoplasma pneumoniae necrotizing pneumonia in children.Methods:Clinical data of 291 children with lobar pneumonia caused by Mycoplasma pneumoniae who were hospitalized in Department of Respiratory Intervention, Qilu Children′s Hospital of Shandong University from August 2016 to September 2018, were retrospectively analyzed.The patients were divided into necrotizing pneumonia group (154 cases) and non-necrotizing pneumonia group (137 cases). After comparing clinical characteristics, laboratory tests, and bronchoscopy findings, multivariate logistic regression analysis was carried out on the indicators with statistical significance to obtain the independent predictive indicators of Mycoplasma pneumoniae necrotizing pneumonia, and then the cutoff value with the maximum diagnostic value of each indicator was found through receiver operating characteristic (ROC) curve analysis.Results:There were no significant differences in gender and age distribution, duration before admission, and platelet count between the 2 groups(all P>0.05). Necrotizing pneumonia group manifested with 11.0(8.3-14.4)×10 9/L of white blood cell count, 0.740±0.115 of neutrophil, 44.2(21.2-72.0) mg/L of C-reactive protein(CRP), 55(35-80) mm/1 h of erythrocyte sedimentation rate, 0.19(0.08-0.60) ng/L of procalcitonin, 2.63(1.62-3.79) mg/L of plasma D-dimer, 456(340-665) U/L of serum lactate dehydrogenase, (35.6±4.3) g/L of serum albumin, 121 cases(78.6%)of bronchoscopic mucosal erosion, 75 cases(48.7%)of purulent lavage, 119 cases(77.3%)of massive secretions embolism; non-necrotizing pneumonia group manifested with 8.7(6.9-11.6)×10 9/L of white blood cell count, 0.660±0.127 of neutrophil percentage, 15.9(7.5-34.3) mg/L of CRP, 45(30-60) mm/1 h of erythrocyte sedimentation rate, 0.10(0.06-0.20) ng/L of procalcitonin, 0.69(0.46-1.24) mg/L of plasma D-dimer, 314(250-419) U/L of serum lactate dehydrogenase, (38.9±3.7) g/L of serum albumin, 53 cases(38.7%)of bronchoscopic mucosal erosion, 20 cases(14.6%)of purulent lavage, and 76 cases(55.5%)of massive secretions embolism.All the above indicators had statistical differences between the 2 groups.Erythrocyte sedimentation rate, serum lactate dehydrogenase, D-dimer, and bronchoscopic mucosal erosion were independent predictors of Mycoplasma necrotizing pneumonia.The area under the ROC curve were 0.643, 0.749, 0.858 and 0.699, respectively, with the cut off point of 53 mm/1 h, 335 U/L, and 1.36 mg/L, respectively. Conclusions:Erythrocyte sedimentation rate≥53 mm/1 h, serum lactate dehydrogenase≥335 U/L, D-dimer≥1.36 mg/L, and bronchoscopic mucosal erosion are early independent predictors of Mycoplasma necrotizing pneumonia in children, among which D-dimer has the highest value.
9.Transport mechanism of swertiamain metabolite across Caco-2 model.
Cheng TANG ; Yanjun ZHANG ; Tiejun ZHANG ; Chengwang TIAN ; Changxiao LIU
China Journal of Chinese Materia Medica 2009;34(17):2258-2260
OBJECTIVETo investigate the intestinal absorption mechanism of swertiamain metabolite {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c]pyridine-1-one, EHPO}.
METHODThe time depended hi-directional transport of EHPO in Caco-2 monolayer model was investigated with the factors of concentration, pH and verapamil. EHPO concentration was measured by HPLC assay and the apparent permeability coefficients (Papp) were calculated.
RESULTIn the this cell model, EHPO could be absorbed through Caco-2 soon. The P(app AP-BL) was equal to the P(app BL-AP), and Papp keep almost constant with the selected concentration investigated. But the Papp could be influenced by pH and verapamil (100 mg x L(-1)).
CONCLUSIONThe absorption of EHPO in Caco-2 cell model is a passive one. And absorption of EHPO in the intestines is quite good.
Biological Transport ; Caco-2 Cells ; Cell Membrane Permeability ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Humans ; Models, Biological
10.Inhibition of berberine on organ cation transporters
Weidang WU ; Tao CUI ; Xingyan ZHANG ; Zihong WEI ; Xiaoyan CI ; Jiangjie LU ; Lixin JIANG ; Changxiao LIU ; Xiulin YI
Drug Evaluation Research 2017;40(5):633-637
Objective To study the inhibitory effects ofberberine on human organic cation transporter (OCTs) including OCT1,OCT2,OCT3,OCTN1 and OCTN2.Methods Using animal cell transgenic method mediated by transporter Lipo 3000,the drug transporters over expression cell lines S2-OCT1,S2-OCT2,S2-OCT3,S2-OCTN1 and S2-OCTN2 were obtained by selective medium culture.The OCTs evaluation model was established by detecting the trans-membrane transport of radioactive substrate in vitro.Wild type (WT) cells were used as control group,activity of OCTs was verified by adding its inhibitor.The inhibition of berberine on the transporters was investigated in vitro.The IC50 of inhibitory effect of berberine on various drug transporters was also calculated.Result The transport activity of transporter cell lines was increased by more than 5 times compared to the WT cell line respectively,what's more,their transport activity decreased significantly by their corresponding inhibitor.The ICs0 of berberine to OCT1,OCT2,OCT3,OCTN1 and OCTN2 were respectively 7.63,6.80,2.25,4.66 and 210.34 μmol/L.Conclusion Berberine significant inhibition to OCT1,OCT2,OCT3,OCTN1 and OCTN2.The inhibition on OCT1,OCT2,OCT3,OCTN1 is stronger compared to OCTN2.