ObjectiveTo investigate the efficacy and side effects of telbivudine and lamivudine for treatment of chronic hepatitis B for 1 year. MethodsIn this random and control study,the efficacy of telbivudine and lamivudine treatments were compared in 120 patients who consisted of 60 cases with HBeAg-negative and 60 cases with HBeAg-positive chronic hepatitis B.The patients were randomly assigned to a daily 600mug telhivudine treatment group or daily 100mg lamivudine group for 52 weeks.The clinical efficacy and adverse reactions of the two groups were observed in control after 52 weeks of therapy,and dynamics of serum HBsAg,HBeAg levels were monitored and compared. ResultsAt week 52,mean reductions of serum HBV DNA from baseline and undetectable serum HBV DNA rates among patients with HBeAg-negative and HBeAg-positive chronic hepatitis B were significantly greater in the telbivudine-treated patients than in the lamivudine-treated group(all P＜0.05).Viral resistance and viral breakthrough was significant common in lamivudine compared with telbivudine(all P＜0.05).Among patients with HBeAg-positive chronic hepatitis B,telbivudine was significant superior to lamivudine with respect to loss of HBeAg(P＜0.05).There was no significant difference in side effects between patients treated with tebivudine and Iamivudine. ConclusionTelbivudine was more effective than lamivudine in treatment of patients with chronic hepatitis B,and the drug was well tolerated.

ObjectiveTo explore heart rate variability (HRV),cardiac troponin Ⅰ (cTnI),left ventricular ejection fraction (LVEF) and electrocardiogram (ECG) in order to clarify the function of cardiac autonomic nerve system and the incidence of potential myocardium injury in patients with severe brain injury.MethodsClinical data of 65 patients with severe brain injury admitted between June 2006 and June 2010 were reviewed.For the sake of comparison,patients were divided by different groupings as per different biomarkers or outcomes such as Glasgow coma scale (GCS) 6 - 8 group and GCS 3 - 5 group; cTnl ＞ 0.5 group,0.04 ＜ cTnl ＜ 0.5 group and CTnl ＜ 0.04 group; and survival group and death group.Another 30 healthy subjects were enrolled as control group.Heart rate variability (HRV) was analyzed with both timedomain and frequency domain methods based on data from 24-hour Holter monitoring.The level of serum cardiac troponin Ⅰ was detected. The left ventricular ejection fraction was measured by beside color ultrasonogram.The different relationships between HRV and GCS as well as prognosis,between cTnI and GCS as well as fatality,between cTnI and ECG,and between EF and GCS were analyzed.The computer statistical software SPSS version 13.0 was used for statistical analysis of data.ResultsAll of the 65 patents with severe brain injury were subjected to decrease in HRV.The patients of GCS 6 - 8 group and GCS 3 - 5 group showed significantly lowered HRV in comparison with control group ( P ＜ 0.05 ).The death group showed more obvious decrease in HRV than the survival group ( P ＜ 0.05 ).Fifty-one of the 65 patients had myocardial injury evidenced by increase in cardiac troponin Ⅰ.The patients of cTnl ＞0.5 group and 0.04 ＜cTnI ＜ 0.5 group showed significantly higher fatality compared with cTnI ＜ 0.04 group ( P ＜ 0.05 ).Compared with the GCS 6 ～ 8 group,more patients in the GCS 3 -5 group had abnormal serum CTnl level and lower EF.ConclusionsThere are cardiac autonomic nerve system disorders and different degrees of myocardial injury in patients with severe brain injury,and early intervention is essential to decrease the fatality of severe brain injury.

Objective To study whether bifendate (BFD) can decrease blood concentration of cyclosporine A (CsA) in the patients subject to renal transplantation. Methods In the 106 cases undergoing renal transplantation treated with CsA, Pred and Aza, 65 were administrated with BFD as experimental group and the remaining 41 cases without BFD as control group. Blood concentrations of CsA, and biochemistry indexes for liver and renal function were determined. Results Blood concentrations of CsA in the experimental group went down by 26. 5 % as compared with those before taking BFD and had a significant decrease as compared with control group (P

Objective To investigate the influence of deoxyschizandrin (Deo) on P-glycoprotein (P-gp).Methods The effect of P-gp on Deo (20,40,80 μg·mL-1) was studied in the Caco-2 cell model in vitro,and the apparent permeability coefficient (Papp) of Deo (20-160 μg·mL-1) on a P-gp substrate,rhodamine123 or cyclosporine A,was calculated.Healthy male Sprague-Dawley rats were randomly divided into five groups:blank control group,verapamil group,low-,medium-and high-dose Deo group (8 rats in each group).Rats in the low-,medium-and high-dose Deo group were intragastrically administered once daily with Deo at 8,16 and 32 mg·kg-1 for 3 consecutive days,while rats similarly received gavagewith verapamil (4 mg·kg-1) in the verapamil group and equal volume of purified water in the blank control group.Thirty minutes after the rats were treated with their respective drugs,rhodamine123 (5 mg· kg-1) was orally administrated.Then the pharmacokinetic profiles of rhodamine 123 were analyzed to evaluate the inhibitory ability of Deo on P-gp in vivo.Results The bidirectional transport rates of Deo (20,40,80 μg·mL-1) were similar,with non-selectivity.Deo (20-160 pg·mL-1)significantly inhibited the basolateral→apical(BL→AP) directional transports of rhodamine 123 and cyclosporine A in Caco-2 cell model (P ＜ 0.05) in a concentration-dependent manner.And Deo (8-32 mg· kg-1) also dose-dependently decreased the peak concentrations (Cm.) and the area under the plasma concentration-time curve (AUC0-t) of Rho123.Conclusion Deo can inhibit P-gp in vitro and in vivo,but it is not a P-gp substrate.

Tacrolimus is a novel immunosuppressant used in the treatment of a variety of autoimmune diseases.More and more studies have shown that tacrolimus has a certain therapeutic effect on myasthenia gravis (MG).This article reviews the mechanism,clinical researches,adverse reactions,dosage and clinical evaluation of tacrolimus in the treatment of MG.

Objective:To investigate the effects of schizandrin B on P- glycoprotein by a classical in vitro cell model. Methods:Caco-2 cell model was used as the carrier,and rhodamine 123 and cyclosporin A were employed as the P-gp substrates, the transmembrane transportation of schizandrin B,rodamine 123 and cyclosporin A were detected by HPLC and a liquid scintillation counting assay,and the apparent permeability coefficient and permeability directional ratio were calculated. Results:The bidirectional transportation rates of schizandrin B(20 μg·ml -1 ,40 μg·ml -1 and 80μg·ml-1 )were similar,and showed non-selective difference. Schizandrin B(20-160 μg ·ml -1 )significantly inhibited the BL → AP directional transportation of rhodamine 123 and cyclosporine A in Caco-2 cell model(P < 0. 05) in a concentration-dependent manner. Conclusion:Schizandrin B is a P-gp inhibitor,while it isn’t a P-gp substrate.

Objective:To explore value of plasma N terminal pro B type natriuretic peptide (NT-proBNP)assessing prognosis of patients With diastolic heart failure (DHF)complicated type 2 diabetes mellitus (T2DM).Methods:The folloW-up data of 206 inpatients With DHF and T2DM from our hospital Were retrospectively analyzed.Ac-cording outcome,they Were divided into no event group (n=108)and event group [n=98,With major adverse car-diovascular events (MACE)occurred].Levels of NT-proBNP,glycosylated hemoglobin (HbA1c),total cholesterol (TC)and loW density lipoprotein cholesterol (LDL-C),left ventricular end-diastolic dimension (LVEDd),left ventricular peak early diastolic velocity/peak late diastolic velocity (E/A)and left ventricular ejection fraction (LVEF)during admission Were measured and compared betWeen tWo groups. Results:Compared With no event group,there Were significant increase in NT-proBNP level and LVEDd,and significant decrease in LVEF and E/A in event group (P<0.05 all).Single factor linear analysis indicated that NT-proBNP,HbA1c,LVEDd and E/A Were positively correlated With MACE incidence rate (r=0.075~0.091,P<0.05 all).Mutivariate Logistic regres-sion analysis indicated that NT-proBNP Was an independent predictor for MACE (OR=1.003,P=0.009).Areaunder recieve operating characteristic curve (ROC)Was 0.803 for NT-proBNP predicting mortality of patients during admission (P <0.05),and survival rate of patientsWith plasma NT-proBNP≤4010pg/mlWas significantly higher than that of patients With NT-proBNP>4010 pg/ml (OR=5.028,P <0.05).Conclusion:Plasma NT-proBNP can independently predict prognosis of patients With diastolic heart failure complicated type 2 diabetes mellitus.

OBJECTIVE:To evaluate the efficacy and safety of Fluvastatin vs. Xuezhikang for hyperlipidemia in patients after renal transplantation. METHODS: 56 hyperlipidemia patients after renal transplantation were enrolled: 32 were assigned to receive Fluvastatin (40～80 mg) po qd for 8 weeks and 24 to receive Xuezhikang (0.6 g) po bid for 8 weeks. Total cholesterol (TC),triglyceride (TG),low-density lipoprotein-cholesterol (LDL),high-density lipoprotein-cholesterol (HDL),liver function and renal function in two groups were measured before and after treatment. RESULTS: In Fluvastatin-treated group,the TC decreased from(7.39?1.98)mmol?L-1 to(5.62?0.93)mmol?L-1,LDL reduced from(3.68?1.13)mmol?L-1 to (2.86?0.83)mmol?L-1;in Xuezhikang-treated group,TC decreased from(6.82?1.29)mmol?L-1 to (5.56?1.19) mmol?L-1 and LDL decreased from (3.26?0.73) mmol?L-1 to (2.78?0.80) mmol?L-1,all showing significant differences as compared with before treatment(P 0.05). No obvious adverse effect was noted in either group during treatment. CONCLUSION: Both Fluvastatin and Xuezhikang are safe and effective for hyperlipidemia in patients after renal transplantation.

Objective: To establish an HPLC-fluoremetry method for determination of the plasma concentration of mycophenolic acid ( MPA) in renal transplantation patients. Methods:The sample was subjected to precipitate proteins using acetonitrile, and the supernatant (20 μl) was used for the sample injection and determination on a Hypersil BDS C18 (250 mm × 4. 6 mm, 5 μm) column with temperature at 25℃. The mobile phase consisted of acetonitrile-methanol-0. 2 mol·L-1 dipotassium hydrogen phosphate buffer (pH=9. 0)( 18∶2∶80)with the flow rate of 1. 0 ml·min-1. The excitation wavelength (Ex) was 342 nm and the emission wave-length ( Em) was 425 nm. Results:The endogenous plasma impurities and drug combinations had no interference with the determina-tion. The calibration curve was linear over the range of 0. 25-50. 00 mg·L-1(r=0. 999 7), and the lower limit of quantification was 0. 25 mg·L-1 . The mean methodological recovery was 99. 12% and the mean extraction recovery was 93. 27%, the intra-day RSD was less than 2% and the inter-day RSD was less than 6%. Totally 10 cases of renal transplantation patients were with mycophenolate mofetil at the dose of 0. 5-1. 75 g·d-1 , and MPA in plasma was within the range of 0. 43-21. 58 mg·L-1 . Conclusion:The method is rapid, sensitive, accurate and convenient, which can be used in the quantitative determination of plasma concentration of MPA in re-nal transplantation patients.

Aim To investigate effects of berberine (Ber) on the transport of P-gp substrates including cyclosporine A (CsA) and digoxin across Caco-2 and L-MDR cell monolayers. Methods Permeability coefficients and transport rates of digoxin and CsA across Caco-2 and L-MDR1 monolayers were measured in the presence of Ber(50 ?mol?L-1~5 mmol?L-1). Results The inhibition studies for digoxin transport showed a dose-dependent decrease in basal-to-apical direction across Caco-2 and L-MDR1 monolayers in the presence of Ber (50 ?mol?L-1~5 mmol?L-1). Both a dose-dependent decrease in basal-to-apical direction and an increase in apical-to-basal direction were observed for CsA transport across Caco-2 monolayers with different concentrations of Ber. The IC50 values calculated for Ber-induced inhibition of digoxin transport are 1.44 mmol?L-1 in Caco-2 cells and 1.24 mmol?L-1 in L-MDR1 cells, respectively. The IC50 value for Ber-induced inhibition of CsA transport is 607 ?mol?L-1 in Caco-2 cells. Conclusion It was suggested that the inhibition and saturation of P-gp transport activity might be involved in interactions between Ber and CsA.