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Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Table of Content

    Volume 14 Issue 4
    26 April 2009
    Novel anticoagulant, direct factor Xa inhibitor: Rivaroxaban
    KE Yong-sheng
    2009, 14(4):  361-367. 
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    Anticoagulants are recommended for the prevention and treatment of a wide variety of thromboembolic events.Although existing anticoagulants are effective , their usage is limited by parenteral administration or the requirement for frequent monitoring and subsequent dose adjustment.Therefore , there is an urgent need for novel , oral agents with a predictable anticoagulant action.Because of its key position in the coagulation cascade and its limited roles outside of coagulation, Factor Xa has presented as an attractive target for novel anticoagulants.As a result , the past decade has witnessed an explosion of research into small-molecule, oral , direct Factor Xa inhibitors , and some are now in clinical development.Rivaroxaban is currently furthest ahead in its developmental program, having entered phase III in 3 indications.It is hoped that , before long , these anticoagulants will allow us to enter an era of convenient , oral anticoagulation , without the need for regular monitoring or dose adjustment.
    Absorption kinetics of 20(R)-ginsenoside Rh2 in rat intestinal segments
    GU Yi, WANG Guang-ji, ZHANG Jing-wei, AI Hua, LV Hua, XIE Hai-tang, JIA Yuanwei, SUN Jian-guo
    2009, 14(4):  368-373. 
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    AIM: To establish a precise and reliable LC/MS assay for determining 20(R)-Ginsenoside Rh2 in rat plasma and to study the absorption kinetics of 20(R)-Ginsenoside Rh2 in different rat intestinal segments.METHODS: Different rat intestinal segments(duodenum , jejunum , ileum and colon)were isolated and ligated respectively , to form a closed intestinal loop model.20(R)-Rh2 was injected into the loop directly at a dose of 9 mg/kg.The blood was harvested at different time points after dosage.Concentrations of 20(R)-Ginsenoside Rh2 in plasma were determined by the LC/MS method.The parameters were calculated.RESULTS: 20(R)-Rh2 had a good linearity from 5 to 1000 ng mL(R2=0.9973)in the LC/MS method established in this paper.The within-day and inter-day precisions were within 15 %,and the accuracy was between 85 %-115 %.After administering in the intestinal loops , the AUC0-6 h were (207±88),(301±49),(157±93)and (172±68)ng·mL -1·h for duodenum , jejunum , ileum and colon respectively ,while the absorption rate constant Ka were (3.9±0.4),(1.6±0.4), (1.9±0.8)and (1.1±0.9)/h ,respectively.The peak time t max were(0.44±0.13),(1.75±0.50), (1.13±0.63)and (2.00±1.41) respectively , with the corresponding peak concentrations at (82±17), (110±11), (36±8)and (43±7)ng/mL.CONCLUSION: It is hard for 20(R)-Rh2 to be absorbed in rat intestine.Duodenum and jejunum are its main absorption sites.It is speculated that bad membrane permeability and intestinal efflux transporters are impact factors for its absorption.
    Electrophysiological study on arrhythmia induced by sulpiride
    YUAN Ting, SONG Hong-yan, YAN Dong, CHENG Lu-feng, ZOU Zhou, Parhat Kerram
    2009, 14(4):  374-380. 
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    AIM: To observe the effects of different concentrations of sulpiride (1,3,10,30,100μmol/L) on action potentials of rabbit cardiac purkinje fibers under ischemic conditions, and the effects of sulpiride on fast sodium current (INa) of ventricular myocytes in guinea pigs.METHODS: By standard microelectrode technique, the effects of different concentrations (1 -100 μmol/L) sulpiride on action potential parameters (APA ) , the depolarization velocity (Vmax) , effective refractory period (ERP) and 90 % action potential duration (APD90) of rabbit cardiac purkinje fibers were observed, in which tissues were perfused by simulated ischemic fluid.Single ventricular myocytes in guinea pigs were isolated with enzymatic dissociation method and the effects of sulpiride on INa of ventricular myocytes were recorded using whole-cell patch clamp technique.RESULTS: The effects of different concentrations of sulpiride on the ischemic cardiac purkinje fibers APA, APD90 had no statistical difference, but the Vmax was decreased.Sulpiride (3 -300μmol/L) inhibited INa in a concentration dependent manner (IC50=10.79 μmol/L, the test potential was-35 mV).Sulpiride (10 μmol/L) reduced the maximum conductance(gmax ) of INa, and the activation and inactivation voltage of INa were decreased by 1.91mV,5.22 mV (P<0.01) , respectively, the coincidnece time constant was increased, while the maximum activated current of INa recovered to that before administration.CONCLUSION: Sulpiride could lightly reverse the shortening of action potential in cardiac purkinje fibers induced by ischemia reperfusion.Sulpiride also inhibits INa in a concentration dependent manner.Sulpiride probably affects the inactivated-state of sodium channels.
    Cardiac protective effects of noninvasive delayed limb ischemic preconditioning against ischemia-reperfusion injury in diabetic rats
    ZHU Xue-hui, LOU Jian-shi, LI Yu-mei, YUAN Heng-jie, WU Yan-na, KANG Yi, JIAO Jian-jie
    2009, 14(4):  381-385. 
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    AIM: To study the effects of noninvasive delayed limb ischemic preconditioning (NDLIP) on myocardium ischemia-reperfusion injury in diabetic rats.METHODS: The acute diabetic rat models were induced by injecting streptozotocin(STZ) through vena caudalis.The diabetic rats were randomly divided into ischemia-reperfusion (IR) group, cardiac ischemic preconditioning (CIP) group and NDLIP group.Rats in NDLIP group subjected to NDLIP left hind limb for 3 days, and at the fourth day, all rats were subjected to myocardial ischemia reperfusion injury.Rats in CIP group were myocardial ischemic preconditioning before ischemia.Blood pressure and electrocardiogram were monitored continuously.The effects of myocardial electrophysiology function, myocardial infarction size and myocardial enzyme were observed in the diabetic rats with NDLIP after myocardium ischemia-reperfusion injury , and the superoxide dismutase(SOD) , the activities of glutathion peroxidase(GSH-Px) , the content of malonaldehyde in rats muscular tissues were detected.RESULTS: The levels of blood glucose were increased and the body weights were decreased in diabetic model rats(P<0.01).Compared with I R group, the elevation extent of ST segment in NDLIP and CIP group were degraded, the emergence time of ventricular premature contraction and ventricular tachycardia were delayed and the duration of both was shortened, and the incidence of ventricular arrhythmia was decreased (P<0.05) , the myocardial infarct size was reduced (P<0.01) , the releases of cadiocyte lactate dehydrogenase (LDH) , creatine kinase (CK ) , and creatine kinase isozyme were decreased (P<0.05, P<0.01) , the activities of SOD and GSH-Px in rats muscular tissues were increased (P<0.01) and the content of MDA was decreased in CIP and NDLIP groups(P<0.05, P<0.01).CONCLUSION: NDLIP can relieve cadiocyte damage induced by I R injury in the diabetic rats and the leakage of cardiac muscle enzyme is decreased , and the physiologic function of heart is improved, the cardiac protective effects of NDLIP group and CIP group are considerable.The effects are associated with the regulation of the equilibrium between oxidation and antioxidation system in myocardium.
    Effects of Mailuoning injection on rat activities of CYP1A2, CYP2E1 and CYP3A4 using a three-drug Cocktail approach
    CHEN Wei-kao, JU Wen-zheng, XU Li-jun, LIU Shi-jia, TAN Heng-shan
    2009, 14(4):  386-390. 
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    AIM: To investigate the effects of Mailuoning injection on rat activities of CYP1A2, CYP2E1 and CYP3A4.METHODS: 14 rats were randomly and equally divided into two groups, i.e.clinicallyequivalent-dose group and higher-dose group.Two group rats underwent 2-cycle pharmacokinetic experiments before and after being treated with two doses of Mailuoning injection for 14 days, in which the rats were concomitantly administered Theophylline (30mg/kg) , Chlorzoxazone (50 mg/kg) and Dapsone (20 mg/kg) by gastrogavage, followed by blood-withdrawing from orbital bleeding at different intervals within 24 hours.High-performance liquid chromatography (HPLC ) was utilized to simultaneously quantitate 3 probe compounds in rat plasma, and DAS 2.0 Software was used to fit plasma concentration-time curve and calculate their corresponding principal pharmacokinetic parameters, among which the statistical differences were evaluated by Pariedt-test.RESULTS: In the 14-day administration period, the 2-cycle pharmacokinetic parameters of 3 probes for the clinically-equivalent-dose group rats exhibited insignificant differences(P>0.05) , meanwhile, after being treated with higher-dose Mailuoning injection, there were no significant differences for theophylline pharmacokinetics in rats, but AUC0-24 h of dapsone and chlorzoxazone after treatment were 1.27 and 1.44 times larger than those before treatment, respectively and chlorzoxazone CLF became smaller.CONCLUSION: Clinically- equivalent- dose Mailuoning injection did not affect the activities of rat CYP1A2, CYP2E1 and CYP3A4 ;higher dose Mailuoning injection could not insignificantly change CYP1A2 activity, but could weakly inhibit activities of CYP2E1 and CYP3A4.
    Protective effect of preparation of nanometer tanshinone ⅡA against global cerebral ischemia-reperfusion injury in rats
    CHEN Feng, YE Long-bin, XIN Zhong-suai, XI Tao
    2009, 14(4):  391-396. 
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    AIM: To investigate the protection effect of preparation of nanometer Tanshinone ⅡA against brain injury in rats undergone global cerebral ischemia reperfusion.METHODS: The rats were intragastrically administrated with the preparation of nanometer Tanshinone ⅡA , then the global cerebral ischemia-reperfusion model of rat was made by clipping and releasing three arteries.The content of MDA and the activity of SOD and Na+-K+-ATPase in homogenate of the cerebral tissues were measured.The sections of pathology and ultrastructure of mitochondrion in cortex had been observed.RESULTS: Tanshinone ⅡA (25 mg/kg ) could obviously decrease the content of MDA (P<0.01)and increase the activity of SOD(P<0.05) and Na+-K+-ATPase(P<0.05)in rats brain tissue.The observation of pathology and ultrastructure showed that the injury of cell and mitochondrion had been restrained in these of rat brain.CONCLUSION: Preparation of nanometer Tanshinone ⅡA has protective effect against global cerebra injury caused by global cerebral ischemia-reperfusion injury in rats.
    Comparion between therapeutic effects of rhein and pioglitazone on experimental nonalcoholic steatosis hepatitis rats
    YING Wei-xing, ZHU Chou-wen,LI Rong-zhou
    2009, 14(4):  397-400. 
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    AIM: To approach the therapeutic effect of rhein and pioglitazone respectively on nonalcoholic steatosis hepatitis(NASH)rats and the possible mechanism.METHODS: 52 male SD rats were randomly divided into 4 groups :control group (n=14), model group (n=14), rhein group (n=12), piogli-tazone group (n=12), the body weight were 140 -160 g.Control group were fed with normal diet for 20 weeks (2 rats for 12 weeks and then were executed).Model group were fed with high-fat and high-cholesterol diet consisting of normal diet , 10 %lard and 2 %cholesterol , for 20 weeks (2 rats for 12 weeks and then were executed).Drugs were given after 12 weeks fed with high-fat and high-cholesterol diet.Rhein (5 g/L suspension)was prepared with normal saline , intragastric administration(100 mg/kg-1?d-1) every day in fixation time.Pioglitazone group (8 mg/kg-1 ?d-1)were intragastric administered.All rats were executed after 20 weeks , and the body weight , liver humid weight were determined , the liver index number was calculated.The levels of fasting blood glucose(FBG), aminopherase and blood fat were determined.The fasting insulin (FINS)and TNF-αwere measured by radio-immunoassay , the insulin resistance index was calculated.The levels of malonaldehyde(MDA), glutathione peroxidase(GSH-Px)in hepatic tissue bomogenate were measured using enzymic method , the liver histopathologic slides were dyed with HE dyeing.RESULTS: Compared with model group , the levels of ALT , AST , blood glucose , insuline , insulin resistance index , TNF-α, MDA were obviously decreased in drug groups.Compared with pioglitazone group , the hepatic steatosis in rhein was obvious(P<0.05), but the inflammation in liver was lower grade.CONCLUSION: Rehin and pioglitazone have therapeutical effects on NASH rats.However , they are different in the aspects of improving hepatocyte steatosis and inflammatory.
    Simvastatin inhibits migration of nasopharyngeal carcinoma -2( CNE2)cells
    TU Yong-sheng, WANG Hong-yan, XU Ji-de, LI Jian-hua, PENG Miao-ru, LIU Xiao-ai
    2009, 14(4):  401-404. 
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    AIM: To study the effect of simvastatin on cells migration of nasopharyngeal carcinoma cell line CNE2 in vitro.METHODS: The depressive effects of simvastatin on CNE2 cells migration were observed by scratch wound healing assay and transwell migration assay.RESULTS: The experimental result of scratch wound healing assay showed that simvastatin inhibited migration of nasopharyngeal carcinoma CNE2 cells in a time-and dose-dependent manner.With 2.5 μmol/L simvastatin treatment for 24 hs, the migration lenth was 50.1 % of that in control group.Transwell experimental result indicated that with 2.5 μmol/L simvastatin treatment for 24 hs, the migrating cell population was 69.2 % of that in control group.CONCLUSION: Simvastatin can inhibits CNE2 cells migration in a time-and dose-dependent manner, which can provide rational clues for clinical research of simvastatin.
    Experimental study of the relationship between Smad2/3 and Smad7 proteins expressions in blood polymorphonuclear leucocyte and the asthma exacerbation
    TONG Xia-sheng, LUO Dong-jiao, FANG Hui-ying, FANG Li, WANG En-zhi, CHEN Hao, YE Hui
    2009, 14(4):  405-409. 
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    AIM: To observe the expressions of Smad2/3 and Smad7 proteins at blood polymorphonuclear leukocyte (PMN) in rats asthma.And to determine whether PMN participate in airway inflammation of asthma via Smads ysterm.METHODS: Rat asthma model was induced by ovalbumin, twenty male Sprague-Danley rats were randomly divided into two groups on average, including asthma group and control group.Blood PMNs were isolated and purified.The expressions of Smad2 3 and Smad7 proteins were detected by immunocytochemical method at blood PMN.RESULTS: The expressions of Smad2 3 protein were significantly higher in asthma group (0.142±0.021, optical density ) than those in control group(0.081±0.011, optical density, P<0.01).But the expressions of Smad7 protein were significantly lower in asthma group(0.125±0.024, optical density) than those in control group(0.257±0.047, optical density, P<0.01).There were significant statistical negtive correlation between the expression of Smad2 3 and Smad7 (n=19, r= -0.891, P<0.01 ).CONCLUSION: Smads system is in imbalanced state in asthma exacerbation.Receptor-regulated Smads is predomination.The synthesis function of PMN about Smad2/3 and Smad7 protein are increased in asthma exacerbation.PMN participated in airway inflammation of asthma may be via Smads systerm.
    Expression of matrix metalloprotease2/9 and tissue inhibitor of metalloproteinase- 2 in the liver tissue of rats with vibrio vulnificus sepsis and the effects of antibacterial agents on these genes
    LI Jing-rong, XIONG Shu-dao, LIANG Huan, LU Zhong-qiu
    2009, 14(4):  410-415. 
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    AIM: To observe the gene expression of matrix metalloprotease 2/9 (MMP-2/9) and tissue inhibitor of metalloproteinase-2 (TIMP-2) in the liver tissues of rats with vibrio vulnificus sepsis and the effects of cefoperazone godium in combination of levofloxacin on the expression of gene MMP2 9 and TIMP-2.METHODS: 110 depuratory grade Sprague-Dawley male rats were randomly divided into three groups, normal control group (CN group, n=10) , vibrio vulnificus sepsis model groups (VV group, n=50) and vibrio vulnificus sepsis model treated with cefoperazone godium in combination of levof loxacin (AA groups, n=50).The ethological changes were observed in all group rats.The expression of MMP2 9 and TIMP2 mRNA were detected by reverse transcriptive polymerase chain reaction (RT-PCR).RESULTS: The levels of gene expression of MMP2 9 were markedly up-regulated and TIMP-2 were down-regulated at early time in all VV groups (via CN group, P<0.05).However, the levels of gene expression of MMP2 9 were down-regulated and TIMP-2 were up-regulated after interruption by antibiotics (via VV group, P<0.05).CONCLUSION: The up-regulation of MMP-2 9 and down-regulation of TIMP-2 are associated with the pathophysiological processes of vibrio vulnificus sepsis, the treatment with cefoperazone sodium in combination with levofloxacin may down-regulate the expressions of MMP-2 9 and up-regulate TIMP-2 gene expression in the liver tissue of rats with vibrio vulnificus sepsis, and relieve the clinical symptoms.
    Effects of salvianolic acid capsule on acute myocardial ischemia in Beagle dogs
    ZHANG Shan-fei, CHEN Min-li, CHAI Jian-guo, PAN Yong-ming, YING Hua-zhong, CHEN Liang, XU Jian-qin, ZHU Ke-yan, YE Hong
    2009, 14(4):  416-420. 
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    AIM: To observe the effect of salvianolic acid capsule on acute myocardial ischemia in Beagle dogs.METHODS: 56 Beagle dogs weighting (12±2) kg were randomly divided into 7 groups, which including sham operation group, model control group, salvianolic acid capsule group(25, 50, 100 mg/kg) , salvia tablets group(275 mg/kg) , Diaoxinxuekang capsule group (100 mg/kg ).The acute myocardial ischemia model in Beagle dogs were established by ligating anterior descending coronary artery after duodenal administration.The degree of myocardial ischemia was detected by epicardial electro gram mapping and the area of myocardial infarction was determined by NBT immunohistochemistry.The levels of serum CK and LDH were detected.The heart muscle ischemia protection of salvianolic acid capsule were observed.RESULTS: The salvianolic acid capsule could degrade the extent of heart muscle ischemia (Σ-ST) , decrease the range of heart muscle ischemia(N-ST) , deflate the myocardial infarction size (MIS) , relieve the levels of serum CK and LDH significantly, and relieve the injury degree of cadiocyte.CONCLUSION: Salvianolic acid capsule has remarkable protective effect on acute myocardial ischemia in Beagle dogs.
    Protective effects of crocetin on cerebral ischemia-reperfusion injury in mice
    GAO Cong , PENG Fei-cheng ,QIAN Zhi-yu
    2009, 14(4):  421-425. 
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    AIM: To research the protective effects of crocetin on cerebral ischemia-reperfusion (CIR)injury in mice.METHODS: The effects of crocetin on brain edema , brain capillary permeability , the activities of lactate dehydrogenase (LDH), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) in brains and the contents of malondialdehyde (MDA)and nitric oxide(NO)in CIR model mice were observed.RESULTS: Compared with the CIR group , crocetin (50 ,100 mg/kg for 5 d )decreased the content of water , Evans blue , MDA and NO in mice brain tissue , and increased LDH 、SOD and GSH-Px activity in brains of CIR mice , with statistical significance.CONCLUSION: Crocetin has protective effects on cerebral ischemia-reperfusion injury in mice , the mechanism may be related to its anti-oxidative activity and inhibition of NO overproduction.
    Distribution of inosine triphosphate pyrophosphohydrolase activity in Han Chinese
    LI Wei-liang, XING Hua-wen, WU Xiao-chun, LI Qing, XIONG Lei
    2009, 14(4):  426-431. 
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    AIM: To study the distribution of inosine triphosphate pyrophosphatase (ITPA) activity in Han Chinese.METHODS: The erythrocyte ITPA activity was detected in healthy Han Chinese by HPLC assay (n=402).RESULTS: There was no significant difference in the mean ITPA activity between male and female of Han Chinese or among different blood types(P>0.05) , a bimodal distribution of ITPA activity was found and the frequency of the ITPA deficiency was 27.6 % in Han Chinese.Furthermore, 6cases with ITPA activity deficiency were found, accounting for 1.47 % of total healthy recipients.CONCLUSION: The distribution of erythrocyte ITPA activity shows a bimodal distribution in Han Chinese.
    Determination of terfenadine concentration in human plasma by LCMS
    LI Li-min, HAO Bin
    2009, 14(4):  432-435. 
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    AIM: To establish a highly sensitive method for the quantitation of terfenadine in human plasma by using high performance liquid chromatogramelectrospray ionization-mass spectrometry (LC-ESIMS).METHODS: Flunarizine was chosen as the internal standard (I.S.) , the plasma was extracted by ethyl acetate after alkalized with 2 mol L sodium hydroxide, and the Phenomenex C18 chromatographic column(250 mm ×4.6 mm, 5 μm) was used, the column temperature was 25 ℃, the mobile phase was methanol-water(80∶20) including 1 %glacial acetic acid and 0.5 % triethylamine.The flow rate was 1 mL/min.Analytes were quantitated using positive electrospray ionization in a quadrupole spectrometer.The selected ion monitoring(SIM) mode was detected , terfenadine m z was 472 and flunarizine m z was 203.RESULTS: The linear range was 0.1 -20 ng mL, the lowest detectable limit was 0.05 ng mL (S N >3) , The intra and inter-assay precision of terfenadine was 2.54 %-9.28 %.The recovery of terfenadine in plasma was 88.62 % -91.67 %.CONCLUSION: The method has strong specificity and high sensitivity and can be used for clinical experiment of terfenadine pharmacokinetic study.
    Effects of atorvastatin on recession of coronary plaque and its components
    XIE Xiang-rong, WANG Ming, ZHANG Hou-jun, SHAN Shou-jie, LIU Zhi-zhong, CHEN Shao-liang
    2009, 14(4):  438-442. 
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    AIM: To evaluate the effects of medium dosage atorvastatin on coronary plaque recession and its components using IVUS gray-scale and virtual histology analysis.METHODS: 22 patients who had been preliminarily clinically diagnosed as coronary heart disease were performed coronary angiography.The selected patients must have at least one major coronary branch whose stenosis extent was 20 %-50 % by CAG examination with eye-measurement.The grayscale and virtual histology after selecting the stenosis aeteria coronaria as target vessel were recorded and the target blood vessel were examined by IVUS.All selected patients were treated with 20 mg atorvastatin lasting for 6 months after the performance and after 6 months the reexamination of the vessel by CAG and IVUS were performed.The LDL-C levels of patients before and after the treatment were compared ;meanwhile the target vessel MLD and DS variation using quantitative coronary angiography were analyzed.The plaque volume and composition variation using IVUS were also analyzed.RESULTS: After 6 months, the LDL-C level was decreased significantly from (3.48±0.49 )mmol/L to (2.25±0.32) mmol/L.The mean decreasing level was 1.23 mmol L and the level diminished 35.3 %(P<0.05) compared with the baseline.The volume of plaque was decreased from (362±167) mm3 to (314±136) mm3.It was decreased by 48.2 mm3 and compared with the baseline it diminished 13.3 % (P<0.05).The proportion of fiber was increased from 66.7 %±5.8 % to 69.8 %±4.4 % (P< 0.05) , and the proportion of necrosis core was decreased from 12.9 %±5.8 %to 9.8 %±4.2 % (P<0.05).The decreasing level of plaque volume was related to the LDL-C decreasing level (r=0.54, P<0.05) , not the proportion of necrosis core ecreasing level was related to the LDL-C decreasing level (r=0.07,P>0.05).CONCLUSION: Patients with mild coronary artery lesions were treated with medium dosage of atorvastatin for 6 months, the plaque recessed, the proportion of fiber increased and the proportion of necrosis core decreased, moreover, the plaque volume decreasing level was related to the LDL-C decreasing level.
    Study on the clinical therapeutic effect of Heshouwu granula on type 2 diabetic hyperlipemia
    DING Ping, ZHU Jian-ping
    2009, 14(4):  443-447. 
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    AIM: To evaluate the clinical therapeutic effect of Heshouwu granula on type 2 diabetic hyperlipemia.METHODS: 106 cases with type 2 diabetic hyperlipemia were divided into two groups :52 in test group and 54 in control group.In addition of their conventional treatment of hypoglycemic agents and diabetic diet and exercise, Heshouwu granulas were used in test group, the dosage was 3 g (one pouch) once per day.Simvastatin of 10 mg once per day was used in control group.Both groups were treated for consecutive 45 days.RESULTS: The symptoms in test group were improved, the scores of the symptoms were lowered significantly compared with both that before treatment (P<0.05) and that of compare group (P<0.01) ;in test group, the blood glucose was significantly lowered compared with that before treatment and that in control group(P<0.05, P<0.01).The 2-hour postprandial glucose in control group was decreased significantly compared with that in control group(P<0.05).The urine glucose was decreased significantly than that before treatment (P<0.05).The cholesterol and triglyceride in test group were decreased significantly compared with those before treatment (P<0.05) but not significantly compared with those in control group(P>0.05).There were 12 cases with market effect and 29 with effectiveness in test group, the total effective rate was 78.85 %, which was significantly effective than that in control group(P<0.05).CONCLUSION: Heshouwu granula is effective for treating type 2 diabetic hyperlipemia, and the efficiacy is better than simvastatin.
    Role of transporters in the drug excretion and its significance in new drug development
    WANG Lei , LI Ning , CHEN Xi-jing
    2009, 14(4):  448-454. 
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    This review is mainly concerned about the effects of drug transporters on drug excretion and the possibility in the development and clinical application of new drugs.The understanding of the properties of transporters enables us to develop novel drugs , which can increase the site-directional drug delivery , or avoid the distribution to other organs , thereby increase the therapeutic effects and reduce the chance of toxic effects.Furthermore , the research of drug transporter- mediated drug-drug interactions and enterohepatic cycle , is able to guide us a more reasonable , safe and effective clinical medication.It is well accepted in recent years that the pharmacokinetic properties of a new drug should be studied in its early stage of development.Additionally , high-through screening system established on transporters is bound to be an effective tool to accelerate the development of new drugs.
    Effects and mechanisms of hepatic stellate cells (HSC)activation and proliferation-related signal transduction pathway in liver fibrosis
    BAO Jia-chun, YUAN Feng-lai, LU Wei-guo, LI Xia, WU Fan-rong, CHEN Fei-hu
    2009, 14(4):  455-459. 
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    The activation and proliferation of hepatic stellate cell(HSC)have been considered to play an important role in hepatic fibrosis.The manipulation of the activation and proliferation of hepatic stellate cells and the process of liver fibrosis inversion are the key in anti-liver-fibrosis researches.This paper briefly reviews the hepatic stellate cells (HSC)activation and proliferation-related signal transduction pathway and explores the role in the pathogenesis of liver fibrosis.It is a new way to study the pathogenesis and therapy of liver fibrosis through intervention of HSC activation and proliferation-related signal transduction pathway.
    DPHDevelopment of the genetic polymorphism study on organic cation transporters
    HAN Lin-zhi, ZHOU Hong-hao
    2009, 14(4):  460-464. 
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    Various kinds of transporters exist in human organs, such as liver, kidney and intestine.The transport of cationic substrates which include endogenous metabolites, exotic substance, and drugs was mainly executed by different organic cation transporters (OCTs).In this article the genetic polymorphisms and their influences on OCTs funtions were mainly reviewed.Meanwhile, the recent findings of OCTs polymorphism influences on pharmacodynamics and pharmacokinetics value of several clinical widely used drugs were also included in this review.
    Application of gene diagnosis in treatment of phenytoin for epilepsy
    LIU Yang, SONG Ya-juan, DING Guo-hua
    2009, 14(4):  465-470. 
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    To analyze in vivo the metabolic process of phenytoin and the basic theories of gene diagnosis, and introduce the examples of successful application of gene diagnosis in clinical phenytoin usage , and thoroughly expound the theoretical basis , clinical relevance, specific methods , and fields of application of using gene diagnosis to improve the usage of phenytoin ,using recently published literature as a basis.The genetic polymorphism is an important factor that affects the pharmacodynamics , pharmacokinetics , and drug adverse reaction of phenytoin.Gene diagnosis may become an effective way of improving usage of phenytoin and should be used widely in treating epilepsy with phenytoin.
    Research progress on the treatment of compensatory Congestive Heart Failure with recombinant human brain natriuretic peptide
    ZHONG Mai-ye, JI Qiu-he
    2009, 14(4):  471-474. 
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    Recombinant human brain natriuretic peptide(rhBNP) is a synthetic peptide, its role is similar to endogenous brain natriuretic peptide, with effects on expanding blood vessel, diuretic, natriuretic, antisympathetic nervous system, decreasing plasma aldosterone and endothelin, also with characteristic of depress urization while neither speeding up the heart rate, nor activating the renin-angiotensin-aldosterone system.A number of studies had confirmed that recombinant human brain natriuretic peptide was effective in the treatment of Congestive Heart Failure(CHF) , it could effectively improve the cardiac function, reduce the cardiac load and reverse left ventricular remodeling.It is now put on to market and applied in clinical treatment of Congestive Heart Failure.The article introduces rh-BNP pharmacologic action, the relationship with CHF, and the research progress on the treatment of CHF.
    Application of imaging new techniques in experimental porcine pulmonary embolism model
    QIAN Bo-chu, SHI Hong, ZHENG Xiao-liang
    2009, 14(4):  475-480. 
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    Pulmonary embolism is a common acute cardiovascular disease with pulmonary artery and its embranchment blocked by endogenous or extraneous embolus.Usually, pulmonary embolism happens suddenly and has a high mutilation rate, so it is a big threat to human health, but the clinical and basic researches on pulmonary embolism are very limited.Imaging new techniques such as noninvasive spiral CT angiography (CTA ) , magnetic resonance angiography (MRA) , magnetic resonance (MR) perfusion, ventilation imaging , and real-time magnetic resonance imaging are developed recently and widely applied in porcine pulmonary embolism model.This paper briefly introduced the application of MR imaging in porcine pulmonary embolism model, including magnetic resonance imaging of fibrin-specific contrast agent in porcine pulmonary embolism model induced by human thromb, the comparision of CTA, MRA, real time magnetic resonance imaging in porcine pulmonary embolism model, the feasibility for the assessment of lung function in porcine pulmonary embolism model combining with MR perfusion, angiography and 3He ventilation imaging, the comparision on pulmonary ventilation perfusion CT and planar imaging in porcine pulmonary embolism model.The above-mentioned methods are useful to carry out the research of pulmonary embolism base drug and antipulmonary embolism drug.