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    药物研究
  • 药物研究
    LI Lei;WANG Chang-yuan;CAI Yun;GAO Peng-cheng;TIAN Yan;LIU Ke-xin
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    Objective To prepare JBP 485loaded oral microemulsion, and to study the shape characteristics,in vitro stability,and its pharmacokinetics in rats. Methods Pseudo ternary phase diagram was adopted to optimize the formula of JBP 485 microemulsion.Drug loading capability, stability and viscosity were used as the indexes for the assessment of the best formula.Rats were used in the study to compare the oral bioavailability of JBP 485 solution and JBP 485 microemulsion. Results Glycerol trioleate/ODO-L/EtOH/H2O (Km= 1:1) was selected as the delivery system of JBP 485.The prepared JBP 485 microemulsion was stable in thermodynamic assessment.The particle diameter was 60-120 nm and the drugloading capability was 35 μg.mL-1.The relative bioavailability of the prepared JBP 485 microemulsion reached 191.3% compared with the JBP 485 solution. Conclusion The prepared JBP 485 microemulsion is stable, of low toxity, and can prolong the circulation time in vivo and improve the bioavailability.
  • 药物研究
    CAI Jin-yan;ZHU En;ZHAO lin;ZHANG Tie;ZHU Chen-chen
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    Objective To investigate the hypoglycemic effect of 3 different extracts from Anoectiochilus in diabetic rats induced by high lipid diet plus streptozotocin (STZ). Methods The total EtOH extracts were prepared from A.lanceolatus, A.moulmeinensis and A.elwesii, yielding 3 extracts.Blood glucose (BG), insulin sensitivity index (ISI) and antioxidant activity was assayed.Morphological examination of the pancreas was performed. Results The total extract from A.elwesii showed the best profile in hypoglycemic effect and improving insulin sensitivity with a fall of BG from 19.3 to 8.5 mmol.L-1 (P<0.05).A significant raise in SOD activity and a reduction in plasma NO were observed after the treatment of 3 extracts from Anoectochilus. Conclusion The total extract from A.elwesii shows a good activity in improving glucose metabolism, which may be attributed to increased insulin sensitivity and SOD activity and reduced plasma NO level.
  • 药物研究
    YUAN Rong-gao;YANG Liu-cai;LIU De-jun;LI Shi-hong;XU Hong-tao
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    Objective To study the effects of the polysaccharides of Ganoderma lucidum on the kidneys of diabetes mellitus (DM) rats and the related molecular mechanism. Methods The DM rat model was established.The DM rats were divided into control group, model group and treatment group.The treatment group was treated by Ganoderma lucidum polysaccharides for 8 weeks.The rat renal function profile, oxidation and anti-oxidation index were determined.TUNEL assay method was used for the detection of renal cell apoptosis.The expression levels of Bcl-2, TGF-β1 and Bax in the kidney were determined by Western blotting. Results After treatment with Ganoderma lucidum polysaccharide, renal function profile in the treatment group was significantly better than that in the model group, and worse than that in the control group (both P<0.05).Renal cortical MDA of treatment group was significantly lower than that of model group, and higher than that of the control group (both P<0.05).SOD of the treatment group was significantly higher than that of the model group, and lower than that of the control group (both P<0.05).Renal cell apoptosis rate of the treatment group was significantly lower than that of the model group, and higher than that of the control group (both P<0.05).Renal cortical Bcl-2 expression level of the treatment group was significantly higher than that of model group, and lower than that of the control group (both P<0.05).The expression levels of BAX and TGF-β1 protein of the treatment group were significantly lower than those in the model group, and higher than those of the control group (both P<0.05). Conclusion Ganoderma lucidum polysaccharides may improve oxidative stress and inhibit renal apoptosis of renal cells to protect the renal function of DM rats.
  • 药物研究
    WEI Wen;GAO Ting-ting;TAN Yong;WU Zheng-hua;
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    Objective To study in vitro antibacterial activity of extracts from different parts of purple perilla. Methods The antibacterial activity of perilla seed oil, perilla leaves and seed peel against Escherichia coli, Bacillus subtilis, Sarcina and Staphylococcus aureus was studied by the disk diffusion susceptibility test (KirbyBauer).The minimum inhibitory concentration (MIC) was determined by tube double dilution method. Results Extracts of perilla leaves and seed peel by water immersion extraction exerted the best antibacterial effect on Bacillus subtilis, with the MIC of 62.5 and 125 mg.mL-1, respectively. Conclusion The extracts of perilla leaf and perilla peel by water immersion, water decoction and alcohol extraction have distinct antibacterial effects against four kinds of bacteria.The extracts by water immersion exert stronger antibacterial effects, especially to Bacillus subtilis.
  • 药物研究
    LI Fan-Fan;LI Jie;WANG Jia-ling;XIAO Jun-hua
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    Objective To study the effects of diazepam on myocardial physiological properties and action potential in rats. Methods The spontaneous beats, contractile force, functional refractory period and excitability of isolated atrial muscles were recorded according to the regular Methods .Standard microelectrode intracellular recording technique was used to record the action potential of ventricular papillary muscles. Results Diazepam (0.017 5-5.25 μmol.L-1) did not markedly affect spontaneous beats of the right atrium.Diazepam (17.5-175.0 μmol.L-1) reduced the frequency of spontaneous beats in a concentrationdependent manner.Diazepam at the low dose (0.175 μmol.L-1) extended the functional refractory period of the isolated left atrium.Diazepam at the high dose (17.5 μmol.L-1) decreased the excitability of left atrium and significantly reduce the action potential amplitude. Conclusion Diazepam exerts direct effects on myocardial spontaneous beats, contractile force, functional refractory period, excitability and action potential.
  • 药物研究
    ZHAO Shi-yin;QIU Hua;HE Qin;LI De-mei;TAN Hua-bing
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    Objective To investigate the effect of gepenoside (GPS) on hepatic fibrosis of rats with type 2 diabetes mellitus (T2DM) and nonalcoholic fatty liver disease (NAFLD). Methods T2DM and NAFLD model (group M) and NAFLD model (group NM) were established by feeding the rats with highfat diet and injection of streptozotocin.The T2DM and NAFLD model was administered with GPS (1 g.kg-1.d-1) (group JH) or GPS (0.5 g.kg-1.d-1) (group JL).αSMA in the liver tissues was determinied by quantified PCR.Blood glucose, triacylglycerol (TG), total cholesterol (TC) and hyaluronic acid were examined.Laminin (LN) expression in liver tissues was detected by immunohistocheministry. Results αSMA expression in the liver tissues was as follows:the amplification of αSMA in group N was regarded as 1, and that in group M was 3.17, with significant difference (P<0.01); The amplification of αSMA in group NM was 2.37 (P<0.01 vs.group N); That was 2.26 in group JH (P<0.01 vs.group M); That was 2.63 in group JL (P<0.05 vs.group JH).LN expression levels were as follows:greatest in group M, middle in group JL and MN, lowest in group JH.HA was significantly increased in groups M, NM, JH, and JL (P<0.01 vs.group N).There were significant differences in HA between group JH, JL and group M (P<0.01).There were significant differences in blood glucose levels, TG and TC between group JH [(10.86±3.46) , (1.41±0.10) and (1.83±0.56) mmol.L-1], group JL [(14.78±3.39) , (1.49±0.20) and (2.82±0.66) mmol.L-1] and group M [(18.84±4.24) , (1.85±0.12) and (3.97±0.64) mmol.L-1] (P<0.01).Significant differences in blood glucose and TG were also found between group JH and group JL (P<0.05, P<0.01). Conclusion GPS can alleviate hepatic fibrosis of rats with T2DM and NAFLD.
  • 药物研究
    XU Biao;ZENG Kun;XIAO Zheng
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    Objective To investigate the effect and mechanism of atorvastatin on the inhibition of chronic heart failure after acute myocardial infarction. Methods Fortyfive male rats with acute myocardial infarction were divided into high dose atorvastatin group, low dose atorvastatin group and acute myocardial infarction group (n=15).Another 10 rats served as sham operation group.High and low dose atorvastatin group received atorvastatin with 20 mg.kg-1.d-1 and 10 mg.kg-1.d-1 by gavage for 6 weeks after acute myocardial infarction.The sham operation group and the control group received no treatment.At the 6th week, the changes of left ventricular morphology and function of rats in every group were detected with ultrasonic heartbeat graph.Left ventricular hypertrophy index (LVHI) was determined in every group.The left ventricle free wall myocardium in the sham operation group and the infarction and border zone myocardium in myocardial infarction groups were preserved to detect myocardial interleukin6 (IL-6) by immunofluorescence confocal microscopy and Western blot. Results Compared to the the sham operation group, there were higher value of left ventricular enddiastolic dimension (LVEDD), left ventricular endsystole dimension (LVESD), enddiastolic volume (EDV), endsystole volume (ESV), LVHI, higher expression levels of myocardial IL-6, as well as lower valuers of left ventricular ejection fraction (LVEF) in the model group, the groups with high or low dose atorvastatin (P<0.05 or P<0.01).Compared to the model group, there were lower values of LVEDD, LVESD, EDV, ESV, LVHI, lower expression levels of myocardial IL-6, as well as higher values of LVEF in the groups with high or low dose atorvastatin (P<0.05 or P<0.01).Compared to the the low dose atorvastatin group, there were lower value of LVEDD, LVESD, EDV, ESV, LVHI, lower expression level of myocardial IL-6, as well as higher value of LVEF in the high dose atorvastatin group (P<0.05). Conclusion Atorvastatin may supress ventricular remodeling by inhibiting the overexpression of myocardial IL-6 after acute myocardial infarction.The effect is dose dependent.
  • 药物研究
    LU Hua;CHENG Dao-hai;LEI Xiao-guang;HE Yun-yan;WAN Rui-rong;SU Ming;WU Ke-jie;LUO Jian-ming
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    Objective To establish a high performance liquid chromatography (HPLC) method for the determination of deferiprone in human plasma. Methods The analytical column was a Kromasil C18 column (4.6 mm×200 mm, 5 μm).The mobile phase was a mixture of acetonitrile and buffer of 50 mmol.L-1 potassium dihydrogen phosphate (containing 5 mmol.L-1 sodium heptanesulfonate and 1% triethylamine) (11:89, pH adjusted to 1.3 with phosphoric acid).Detection wavelength was set at 278 nm.The column temperature was 25 ℃.The injected volume was 20 μL.Flow rate was 1 mL.min-1. Results The calibration curve of deferiprone were linear in the range of 0.5-80.0 mg.L-1 (r=0.996 5), and the lower limit of detection was 0.5 mg.L-1.The absolute recoveries of deferiprone at low, medium and high concentrations were more than 85.6%, and the method recoveries were more than 89.9%.The intraday coefficients of variation were 1.61%-3.70%, and the interday coefficients of variation were 1.84%-4.81%. Conclusion The method is simple, quick, accurate, sensitive, and specific, and can be used in detecting deferiprone concentration in human plasma.
  • 药物研究
    YUE Wen-wei;ZHANG Xin;CHEN Bo;LIU Qiang
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    Objective To investigate the effects of aliskiren on ventricular remodeling in rats with acute myocardial infarction (AMI) and the related mechanism. Methods Sixty male Wistar rats were randomly assigned into four groups (n=15):sham group, control group, perindopril group and aliskiren group.After ligation of the anterior descending coronary artery, the rats in perindopril group and aliskiren group were given perindopril or aliskiren for 8 weeks, respectively.The concentration of hs-CRP in serum was assayed by ELISA.The expression of MMP-2, MMP-9, TIMP-1 and TGF-β was detected by immunehistochemistry.The mRNA expression of MMP-2, MMP-9, TIMP-1, TGF-β, Collagen Ⅰand Ⅲ was determined by RTPCR.Protein expression of MMP-2, MMP-9, TIMP-1 and TGF-β was determined by Western blotting. Results The concentration of hs-CRP was significantly lower in perindopril group and aliskiren group than in the control group (P<0.05).The mRNA and protein expression of MMP-2, MMP-9, TGF-β, Collagen Ⅰand Ⅲ were significantly downregulated in perindopril group and aliskiren group as compared to the sham group (P<0.05).Meanwhile, the mRNA and protein expression levels of TIMP-1 were significantly upregulated in perindopril group and aliskiren group as compared to those in sham operated group (P<0.05). Conclusion Aliskiren can downregulate the expression of MMP-2, MMP-9, TGF-β, Collagen Ⅰand Ⅲ and hs-CRP, upregulate TIMP-1.There is no significant difference between perindopril and aliskiren in ventricular remodeling in rats with AMI.

  • 药物研究
    LI Li;LUO Ze-ping;ZHOU Huan-di;YANG Xiu-fen
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    Objective To study the effect of butyl alcohol extract of Melastoma dodecandrum Lour.on blood glucose, blood lipid and antioxidant levels in diabetic mellitus (DM) mice induced by streptozotocin (STZ). Methods DM model was established by intraperitoneal administration of STZ at 150 mg.kg-1 in mice.Mice in the treatment groups were administrated with butyl alcohol extract of Melastoma dodecandrum Lour.at 60, 40 and 20 g.kg-1 respectively via gastric irrigation, while the DM and normal control groups were administrated with the same amount of distilled water via gastric irrigation daily.Fasting blood glucose (FBG), total cholesterol (TC), triglycerides (TG), superoxide dismutase (SOD) and malondialdehyde (MDA) were analysed.The organ indexs of liver and kidney were calculated. Results Compared with the DM group, FBG, TC and TG were reduced significantly (P<0.01 or P<0.05), serum SOD was increased (P<0.01 or P<0.05), and MDA was decreased (P<0.01) in the treatment groups.The organ index of kidney was significantly decreased (P<0.01). Conclusion Butyl alcohol extract of Melastoma dodecandrum Lour.can reduce blood glucose, improve lipid disorders and antioxidation fuction in DM mice.
  • 药物研究
    TIAN Yuan-chun;ZHANG Quan;LEI Chong-zhong;LU Gui-li
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    Objective To observe the immunoregulatory effect of shenqi qiangjing capsule (SQQJC) on mice treated with cyclophosphamide. Methods Sixty mice were randomly divided into the control group, model group, positive group, SQQJChigh, medium and low dose groups.Except in the control group, all mice were injected with cyclophosophamide (50 mg.kg-1).Mice in the SQQJChigh, medium and low dose groups were administered with 1.0, 0.5, and 0.25 mg.kg-1 SQQJC, respectively.Mice in the control group were administered with solvent.Mice in the positive group were administered with levamisole for 10 days.The mice were examined for the total peripheral white blood cells, immune organ weight index, carbon particle clearance capability of macrophage, the lymphocyte transformation rate and the serum hemolysin content. Results Compared with the model group, the peripheral white blood cells, carbon particle clearance capability of macrophage, the lymphocyte transformation rate and the serum hemolysin content were significantly increased in mice treated with SQQJC at low, medium and high doses (P<0.05 or P<0.01); the immune organ weight indexes were significantly increased in mice treated with SQQJC at high dose (P<0.05). Conclusion SQQJC can improve the immune function of the immunosuppressed mice.
  • 药物研究
    WU Yan-xia;LI Xiu-juan;MA Wei
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    Objective To study the neuroprotective effect of zhengan xifeng decoction (ZGXFD), a tranditional Chinese herbal compound, on conscious rats with middle cerebral artery occlusion (MCAO). Methods The rat model of focal cerebral ischemia was established with the sutureocculuded method and was treated with different doses of ZGXFD (1.5 and 3 g.mL-1, respectively) before MCAO.The effect of ZGXFD on the behavior disorder and extent of cerebral edema of the MCAO rats were detected.ET-1 expression in the rat brain tissues was examined by immunohistochemistry method.The AQP 4 and AQP 9 expression were determined by Western blotting. Results After MCAO, different degrees of behavior disorder appeared in all rats.Pretreatment with ZGXFD improved the grade of behavior disorder of the rats, reduced the extent of cerebral edema, and increased AQP4 and AQP9 obviously.After MCAO, the tissue ET-1 expression was increased obviously but the ZGXFD could reverse it.Compared with the MCAO group, the AQP9 protein expression significantly increased after 6 h of hypoxia while the AQP4 did not change. Conclusion These findings suggest that ZGXFD can directly modulate ET-1, AQP4 and AQP9 expression and reduce cerebral edema.
  • 药物研究
    LI Jian-xu;ZHENG Ya-mei;HU Xiao-yan;TENG Kai;CAO Ru-bo;LIU Li
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    Objective To study the effect of aidi injection on radiationinduced lung injury and the probable Mechanism. Methods One hundred and twenty C57BL/6 mice were exposed to either sham radiation or single fraction of 12 Gy delivered to the thorax.Four groups were defined as follows:in normal control group,the mice received neither radiation nor drug;in aidi injection+radiation group,the mice received radiation and aidi injection;in Solu Medrol+radiation group,the mice received Solu Medrol;in radiation group,the mice were exposed to radiation.Aidi or Solu Medrol were injected intraperitoneally 2 h before the radiation and daily after the radiation.Mice were sacrificed 1,24,72 hours,1 ,2 ,4,8,16 and 24 weeks after radiation.The left lungs were fixed and sectioned.The sections were stained by haematoxylin and eosin,masson stain and immunohistochemical stain for transforming growth factor β1 (TGF-β1).The right lungs were collected to detect TGF-β1 mRNA expression by realtime quantitative reverse transcipiase polymerase chain reaction (RTPCR) and TGF-β1 protein expression by Western blotting. Results Pneumonitis developed 1 to 2 weeks after radiation.Their TGF-β1 mRNA and protein expression levels in radiationtreated mice were significantly higher than those in normal control group (both P<0.05).But the effects were reversed by aidi and Solu Medrol treatment (P<0.05).The TGF-β1 mRNA and protein expression levels were not significantly different between aidi and Solu Medrol treatment. Conclusion Both aidi injection and Solu Medrol can significantly downregulate TGF-β1 mRNA and protein expression levels in the lungs of mice with radiationinduced lung injury.There is no significant difference in the effect between aidi injection and Solu Medrol.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    LI Lei-lei;LING Ping;WANG Hai-xia;JI Sheng-guo
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    Objective To develop a method for the determination of ethanol extracts content in Eriobotrya japonica by nearinfrared (NIR) spectroscopy. Methods The ethanol extract contents of 146 samples were determined by hot water extraction and ethanol precipitation method.NIR spectrums were measured.The multivariate calibration method and Second derivative test were used for spectral preprocessing.Calibration model of the ethanol extract content was established by the partial least squares regression analysis.Twentyeight batches of samples were tested to validate the model. Results The correlation coefficients, the Rootmeansquare error of calibration, the Rootmeansquare error of prediction and the Rootmeansquare error of crossvalidation of the calibration model for ethanol extract content were 0.984 80, 0.387, 0.659 and 1.836 52, respectively. Conclusion The method is steady, accurate, and can be used to predict ethanol extract contents of Eriobotrya japonica rapidly.
  • 药物制剂与药品质量控制
    CHENG Lu;ZHANG Geng
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    Objective To study the optimum enzymesolvent extraction conditions of steroidal compounds from Fistular Onion Stalk. Methods The process was optimized by single factor experiments and orthogonal test according to the yield of steroidal compounds. Results The optimum extraction conditions were established as follows:pH was 5.0;the concentration of enzyme was 0.5 mg.mL-1;enzymatic hydrolysis temperature was 50 ℃;enzymatic hydrolysis time was 2 h.The factors which influenced the extraction of steroidal compounds from Fistular Onion Stalk were listed as follows:pH value>enzymatic hydrolysis time>enzyme concentration>enzymatic hydrolysis temperature. Conclusion Enzymesolvent extraction of steroidal compounds from Fistular Onion Stalk is a simple process.It can improve the extraction efficiency and reduce energy consumption.
  • 药物制剂与药品质量控制
    WANG Jie;LIU Wei;YE Yong;HE Cheng-zhang;LU Hua;CHENG Dao-hai;LI Yuan-hong
    Objective To study the quality control method for longzhi capsule. Methods Fibrin plate method was used to detect the drug fibrinolytic activity.Anticoagulantion effect of the drug in vitro was measured by using automatic coagulation analyzer.Ferulic acid and safflor yellow in the drug were identified by thinlayer chromatography (TLC).The contents of ferulic acid and hydroxysafflor yellow A in longzhi capsules were determined by high performance liquid chromatograghy (HPLC). Results Longzhi capsule had obvious fibrinolytic effect.It could obviously prolong activated partial thromboplastin time (APTT), prothrombin time (PT) and thrombin time (TT).The calibration curve of ferulic acid was linear in the range of 0.04-0.40 μg (r=0.999 9), the average recovery was 99.32%.The calibration curve of hydroxysafflor yellow A was linear in the range of 0.5-5.0 μg (r=0.999 8), the average recovery was 99.14%. Conclusion This method is simple, accurate and capable to effectively control the quality of longzhi capsules.
  • 药物制剂与药品质量控制
    SHENG Yan;CHEN Hao;ZHANG Wen-ting
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    Objective To study and revise the quality standard for baihe gujin tablets. Methods Angelicae sinensis radix, scrophulariae radix, paeoniae radix alba, and glycyrrhizae radix et rhizome were qualitatively identified by thinlayer chromatography (TLC).The content of paeoniflorin was analyzed by high performance liquid chromatography (HPLC).Chromatographic condition included a Agilent SB C18 column (250 mm×4.6 mm, 5 μm), acetonitrile0.05% triethylamine solution (pH adjusted to 2.5 with phosphoric acid) (14:86) as the mobile phase, and the detection wavelength at 230 nm. Results Angelicae sinensis radix, scrophulariae radix, paeoniae radix alba and glycyrrhizae radix et rhizoma could be detected by TLC.The concentration of paeoniflorin was linear in the range of 15.01-3 752.50 ng (r=0.999 9).The average recovery was 103.3%, and RSD was 0.93% (n=9). Conclusion The method was simple, sensitive, accurate, and reproducible.It can be used for the quality control of baihe gujin tablets.
  • 药物制剂与药品质量控制
    WANG Xiao-ming;QIN Ling-hao;ZHENG Li-xian;ZHENG Qing;TAN Zai-you
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    Objective To optimize synthesis process of diclofenac sodium-β-cyclodextrin polymer microspheres (DFS-β-CDP-MS), to characterize its structure and evaluate its characteristics of in vitro release. Methods The orthogonal test was employed. Drug loading ratio and encapsulation efficiency served as evaluating indexes.The effects of various factors, such as drug concentration, drug loading temperature, mass ratio of microsphere to drug, and drug loading time on the experiment results were investigated. In vitro analytical method was established to study the influence of each ingredient on the release of DFS. Results The best technological conditions were:DFS%=30%; temperature=45 ℃; m(β-CDP MS):m(DFS)=1:1; time=24 h.Drug release pattern in vitro was best described by firstorder kinetics; the 24 haccumulative release was 86.13%. Conclusion Synthetic process of DFS-β-CDP MS is optimized.The reproducibility of the technology is good.The DFS-β-CDP MS has sustained release characteristic.