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    药物研究
  • 药物研究
    LI Chuan;YANG Xi;HU Jun-bo;LIAO Jia-zhi
    Objective To investigate the role of isorhamnetin on the growth of PC9-IR cells.Methods The gefitinibresistant PC9(PC9-IR) cells were generated by consistently culturing the PC9 cells with 10%FBS/DMEM contained 0.5 μmol.L-1 gefitinib.Then, the PC9-IR cells were treated with isorhamnetin at different concentrations.The proliferation was detected by MTT assay after 24,48 and 72 h, respectively, with PBMNCs as control.Western blot assay was used to detect the change of growth signal pathway.Additionally, clonal assay was performed to analyze the clone formation ability of PC9-IR with or without isorhamnetin.Results Isorhamnetin inhibitted the growth of PC9-IR.The IC50 at the three time points were 212 μmol.L-1 (24 h),98 μmol.L-1 (48 h),64 μmol.L-1 (72 h),and PBMNCs was 204 μmol.L-1 (72 h).It was showed that the phosphAkt was suppressed and the clonal formation ability of PC9-IR was lowered by isorhamnetin. Conclusion Isorhmantin could inhibit the growth of PC9-IR cells through suppressing the phosphorylation of Akt.

  • 药物研究
    YU Pan-pan;HANG Peng-zhou;ZHANG Bo;LI Xiang-hui;AN Ran;ZHAO Wen-ting;DU Zhi-min;
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    Objective To investigate the effect of wenxin granule(WXG) on the activity of CYP1A2,2C9,2C19,2D6,2E1 and CYP3A4 by cocktail probe drugs in rats.Methods The male Wistar rats were divided randomly into the highdose group, lowdose group, which were treated by intragastric injection with WXG, and blank control group which was administrated by intragastric injection with 0.9% sodium chloride solution, for seven days.Cocktail probe drugs as caffeine,tolbutamide,omeprazole,metoprolol,chlorzoxazone and dapsone were administrated by intraperitoneal injection on the eighth day.Then,plasma was obtained from the caudal vein,and the blood samples were analyzed by HPLC.The pharmacokinetic parameters of both highdose and lowdose groups were compared with the control group.Results  The AUC(0-∞) of caffeine was increased 1.635fold and 1.435fold by the highdose and lowdose of WXG,respectively while that of dapsone was raised 1.816fold and 1.324fold, respectively.Furthermore,the AUC(0-∞) of omeprazole and chlorzoxazone were increased 2.748fold and 1.696fold by the high dose of WXG,respectively. Conclusion Our study suggests that the highdose of WXG has the potential to inhibit the activity of CYP2C19, CYP2E1, CYP1A2 and CYP 3A4.
  • 药物研究
    YING Jing-yan;XU Ai-ren;XU Jin-long;MA Wei-cheng
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    Objective To investigate the inhibition effect of paclitaxel polylactide glycolide nanoparticles (PTX-NPs) injection on mouse lung metastatic melanoma model and its mechanism.Methods The PTX-NPs were prepared by an improved emulsifieationdiffusion method and the murine lung metastatic melanoma model were established.A total of 60 tumorbearing mice then were divided into four groups (n=15), PTX-NPs, commercially available paclitaxel (PTX) group, control (saline) group and vehicle (Blank-NPs) group.The antitumor effect of paclitaxel nanoparticles in vivo has been evaluated by observing lung condition, and assessing tumor tissue proliferation and invasion with immunohistochemistry 30 d after tumor inoculation.The mice were i.v.injected every 3 d, for total 5 times.Drug concentrations in mouse plasma, heart, liver, spleen, lung and kidney were determined by highperformance liquid chromatography (HPLC).Results The entrapment efficiency of PTX-NPs was 65%, and the particle size distribution was 80100 nm.PTX-NPs showed good suppression against lung metastatic melanoma model.The number of PCNApositive cells(125±16) and HIFpositive cells(27±10) detected by immunohistochemistry in the PTX-NPs group exhibited significant difference compared with those in the PTX group [(217±19)and (94±15)](P<0.01).The HPLC results showed that the drug content in the lung of PTX-NPs group was (5.73±0.25) μg.g-1 24 h after the last administration,which was significantly higher than that of the PTX group (0.66±0.02) μg.g-1 (P<0.01). Conclusion PTX-NPs injection significantly inhibits the growth and metastasis of B16 carcinoma and exerts lung targeted effects.
  • 药物研究
    YAN Ming;LI Hong-zhi;LIU Jie-ting;ZHAO Bing-hai;YUAN Xiao-huan;GUO Yan-qin;WU Yi-yan;CHU Yan-hui
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    Objective To study the effects of baicalin on H2O2-induced SH-SY5Y cell injury and Bcl-2 and Bcl-xL mRNA expression.Methods The H2O2-induced SH-SY5Y cell injury was established on SH-SY5Y neuroblastoma cell line in vitro.MTT assay was used to detect the proliferation of SH-SY5Y cells under different concentrations of baicalin, and Bcl-2 and Bcl-xL mRNA expression were measured by Realtime quantitative PCR.Results The survival rates of cells were 130.4%,89.9% and 60.9% by baicalin at 50,100,200 μmol.L-1 , respectively, the two low dose of which showed significantly difference compared with the H2O2 injury model group which was 33.9%(P<0.01).Bcl-2 mRNA expression levels were (11.48±0.48),(7.37±1.57),(7.39±2.01), and(5.84±0.58); Bcl-xL mRNA expressions were(19.96±2.22),(11.36±3.94),(13.07±2.37), and(7.95±0.58)in the group of 50,100,200 μmol.L-1 of baicalin and H2O2 injury control one, respectively.The conspicuous difference was found on Bcl-2 and Bcl-xL mRNA expression between the H2O2 injury group and baicalin at 50 μmol.L-1(P<0.01). Conclusion Baicalin can protect SH-SY5Y cell from H2O2 injury, the mechanism of which may be associated with Bcl-2 and Bcl-xL up-regulation resulting in anti-apoptosis effects.

  • 药物研究
    LIANG Li;LI Xi;WANG Qing-wei;LIU Xue-ying;ZHANG Sheng-yong
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    Objective To develop a HPLC-UV method for quantitative determination of resveratrol in mice plasma and to study the pharmacokinetics of resvetrol in mice after oral administration.Methods Chromatographic separation was achieved on an Ultimate AQ-C18 column (150 mm × 4.6 mm, 5 μm) using acetonitrilewater (32:68, V:V) as mobile phase at a flow rate of 1.0 mL.min-1.The UV detection wavelength was set at 306 nm, and the assay was executed at 30 ℃.Results The method was validated and found to be linear in the range of 0.10-10.00 μg.mL-1.The assay accuracy and precision were within the range of 98.0%-102.0%. The main pharmacokinetic parameters of resveratrol ,Cmax was 3.589 μg.mL-1,tmax was 30 min, t1/2α was 10.5 min, t1/2β was 172.7 min. Conclusion The method was sensitive, simple and successfully applied in the study of pharmacokinetics of resveratrol in mice.

  • 药物研究
    CHEN Wu;XU Jin-long;CHEN Yuan-na
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    Objective To investigate the protective effect of tea polyphenols on liver of rats exposed to lead.Methods Forty SD rats were randomly divided into the normal control (NG), model control (CG), highdose (HG), middledose (MG) and lowdose of tea polyphenols groups (LN), 8 rats in each group.The rats in the NG were given with intraperitoneal injection of 1.0 mL deionized water, those in the others were intraperitoneally injected with lead acetate 15 mg.kg-1, once a day for consecutively 10 days; meanwhile, rats in the NG and CG were treated with 0.9% NaCl, and those in the HG, MG, LG were orally administered with 2.0, 1.0, 0.5 g.kg-1 tea polyphenols for 30 consecutive days, respectively.The serum ALT, AST and liver SOD, MDA were determined to assess the liver protection of tea polyphenols for rats exposed to lead.Results ALT of NG, CG, HG, MG, LG were (52±7) ,(245±32), (139±47), (158±67), (240±28) U.L-1, respectively; AST were (45±8), (256±35), (147±53),(174±23), (236±32) U.L-1,respectively; SOD were (120±13), (33±9), (89±28), (79±24), (67±15) U.mg-1 ,respectively; MDA were (2.6±0.7), (10.5±1.6), (3.6±1.2), (5.3±1.5) ,(9.5±1.2) nmol.mg-1, respectively. Compared with those in NG, ALT, AST and liver MDA of CG were significantly increased, while liver SOD significantly reduced (P<0.01); the ALT, AST and liver MDA in HG and MG were significantly lower (P<0.01), but the liver SOD was significantly higher than those in CG (P<0.01).While the LG significantly increased SOD activity (P<0.01), but didn’t obviously clear liver MDA. Conclusion Tea polyphenols showed liver protective effect, the mechanism of which might be related to enhancing peroxidase activity and scavenging free radicals.
  • 药物研究
    JING Yun-jie;ZHANG Wen-pin;ZHANG Hai-ning
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    Objective To investigate the immunomodulatory effect of fuzheng powder on immunodepressive mice induced by cyclophosphamide.Methods The immunosuppressive murine model was induced by intraperitoneally injecting cyclophosphamide at the dose of 80 mg&#8226;kg-1, then they were treated with different doses of fuzheng powder(2.5, 5.0,10.0 g.kg-1)by intragastric administration, and the mass of immune organs, carbon clearance index, serum hemolysin, the total WBC in peripheral blood and NK cell activity were measured.Results Thymus index(P<0.05) was remarkably increased in the fuzheng powder at middle- and low-dose groups of immunosuppressive mice, while the spleen index (P<0.01), the entire number of WBC in peripheral blood(P<0.01)and NK cell activity(P<0.01)in the middle- and high-dose groups, and each dose of fuzheng powder raised the levels of serum hemolysin(P<0.01).In addition, Fuzheng powder at highdose played an important role in raising the carbon clearance index K and phagocytic index α of the immunodeppressive mice(P<0.05). Conclusion Fuzheng powder could enhance the nonspecific and specific immunity of immunosuppressive mice induced by cyclophosphamide and also protect immune system imbalance.
  • 药物研究
    YUAN Chun-ping;LU Qi-chun;YOU Wei-liang;REN Xiu-hua;DU Guang
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    Objective To develop and evaluate the in vitro-in vivo correlation model(IVIVC) of nifedipine extended-release tablets.Methods A release condition that distinguished different formulations was screened and the accumulated release rate (Fd) of nifedipine extendedrelease tablets was determined by HPLC.The plasma drug level of healthy volunteers after single oral dose of nifedipine extendedrelease tablets with different release rates were determined by LC-MS/MS.The accumulated absorption percentage (Fa) was calculated by the equation of Wagner-Nelson.Results Our study showed that good correlation appeared between in vitro release and in vivo absorption of the two formulations.The formulation which was bioequivalent to Adalat GITS was used to create a IVIVC model: Fa = 0.831 4 Fd+0.005 2, r=0.980 8, P=0.0006 (P<0.01).Another formulation was used to estimate the prediction error externally of the model, and the prediction error was: PE% (AUC0~24)=3.2%, PE%(Cmax)=3.5%. Conclusion The IVIVC model can well forecast the characteristics of the in vivo absorption of nifedipine extended-release tablets effectively, which provides the basis for making product quality standards.
  • 药物研究
    ZHU Qing;YU Xiao-mei;WANG Sheng-li
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    Objective To investigate the change of left ventricular myocardium radial strain and circumferential strain in spontaneously hypertensive rats SHR) with drug intervention for three months by speckle tracking imaging(STI) and determine a way capable of evaluating the effect of drug intervention on left ventricular function of SHR earlier than conventional echocardiography.Methods Echocardiographic examinations were performed in ten Wistar rats and thirty SHR.The latter were made into normotensive group, nifedipine group and sanziyangying decoction group.Left ventricular fractional shortening(FS) and ejection fraction (EF) were measured by trasthoracic echocardiography.Radial strain and circumferential strain were measured in the left ventricular shotaxis views with 2D strain software.Results No significant difference in EF and FS were found between the four groups.However, the peak systolic radial strain(PRS)and circumferential strain (PCS) of SHR were significantly decreased(P<0.05).Compared with the SHR model control, the PRS of all segments were increased in the nifedipine group except for the inferial and septal segments P<0.05).Circumferential peak systolic strain of 6 segments in the sanziyangying decoction group was significantly lower than that of the SHR model control, especially for that of the septal, antetheca, side wall and back wall (P<0.05). Conclusion STI is superior to the conventional echocardiography on evaluating the myocardial radial strain and circumferential strain in left ventricle.

  • 药物研究
    FU Lian-qun;LI Xiu-ying;YANG Cheng-xiong
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    Objective To investigate the effect of galangin (GL) on cognitive impairment in the senescent mice induced by D-galactose (D-gal).Methods D-gal was subcutaneously injected to establish a senescent mice model.The Morris water maze test and step-down avoidance one were performed to study the learning and memory abilities of mice.The activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT) and content of malondialdehyde (MDA) in mice hippocampus were detected by biochemical examination.Results The mice treated with D-gal generated significant cognitive deficiency.Administration of GL to D-gal treated mice ameliorated cognitive impairment in the hippocampus.Biochemical examination revealed that GL attenuated the decreased activities of SOD, GPx, CAT and reduced MDA levels in the hippocampus of D-galtreated mice. Conclusion Galangin possesses anti-oxidative effect by improving the cognitive function, and increasing activities of SOD, GPx, CAT and lowering MDA of the senescent mice induced by D-gal.
  • 中药及天然药物专栏
  • 中药及天然药物专栏
    ZHOU Xiao-wei;JIANG Ru;WANG Qing-wei;LI Xi;XU Yuan;LI Xiao-ye
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    Objective To study the effects of the essential oil from Cyperus rotundus L.on percutaneous permeability of nitrazepam through rat skin in vitro, and provide the basis for screening penetration enhancers from traditional Chinese medicine and developing the transdermal formulation of nitrazepam.Methods Transdermal test was performed by the modified Franz diffusion cell in vitro and the cumulative permeation content of nitrazepam was determined by HPLC.Results A good percutaneous permeability was obtained when the essential oil from Cyperus rotundus L.was more than 1%, and the effect of which was in a dosedependent manner.The 24hour average cumulative permeation amounts of 0.5 mg.mL-1 nitrazepam with 3% Azone, and 3%, 5% Cyperus rotundus volatile oil were 143.7,172.6 and 229.3 μg.(cm2)-1, respectively; the average penetration constants were 6.381, 7.511, and 10.32 μg.(cm2).h-1, respectively; the enhanced permeability factors were 1.970, 2.319, 3.186, respectively. Conclusion The essential oil from Cyperus rotundus L.shows strong penetration enhancing effect for nitrazepam.

  • 中药及天然药物专栏
    DING Yuan-yuan;QIU Lin;ZENG Ming;XU Qian;XU Jing-feng
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    Objective To investigate the effects and mechanism of oleum cinnamomi (OC) on primary rat myocardial cells infected with Coxsackie virus B3(CVB3) by the serum pharmacological method.Methods The primary rat myocardial cells from the ventricle muscle of new born SpragueDawley rats were prepared.After 72 hours, different doses of OC contained sera obtained via i.v.injection with OC in rats were added in myocardial cells infected with CVB3, to establish the model and control groups at the same time.The cinnamaldehyde and cinnamic acid in sera were detected at different time points.And the relative content of CVB3mRNA was assayed by Realtime PCR.The survival rate of myocardial cells was determined through a metabolic 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.A simple correlation test was implemented to analyze the relationship by using the SPSS software.Results The results showed that the effect of OC contained serum on the myocardial cell survival rate and relative amount of CVB3 mRNA was contributed to cinnamic acid P<0.05 or P<0.01) rather than cinnamaldehyde. Conclusion Oleum cinnamon is an effective antiviral agent against viral myocarditis, the cinnamic acid is the main effective component for which.

  • 中药及天然药物专栏
    LI Yan-ju;DING Wen;LI Qin-shan;LIU Yang
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    Objective To detect the content of total saponin (ASP) in Asparagus racemosus from Guizhou and study its scavenging action on oxygen free radicals.Methods The total saponin was isolated from Cochinchinese Asparagus root from Guizhou.The content of which was calculated by determining absorbability with spectrophotometric method at 310 nm and coloring the perehloric acid by referring the bamboo brier sapogenin as control.The effect of ASP upon O2-and&#8226;OH was detected by the autooxidation in pyrogallol and phenathroline-Fe(Ⅱ)/H2O2 system.Results The content o ASP was 2.390%,RSD=1.19%.ASP cleared O2- in vitro (P<0.01) in a dosedependant manner. It inhibited the generation of &#8226;OH in vitro by (29.1±0.17)%(P<0.05). Conclusion ASP in Asparagus racemosus from Guizhou could scavenge O2- markedly and inhibit &#8226;OH as we11.
  • 中药及天然药物专栏
    LIN Mei-yu;ZHANG Qing-he;LIU Hai-yu;LIU Chuan-gui;LI Ping-ya
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    Objective To study the chemical constituents in volatile oil extracted from nuanwei shule tablets.Methods The volatile oil were extracted and isolated with steam distillation method according to the Chinese pharmacopeia (ChP,2010).The chemical composition was identified by GC-MS with capillary column chromatography, and the relative contents were analyzed via area normalization method.Results The total of 51 components were detected, 45 compounds of which were identified and accounting for 95.1% of total flow area.The compounds with the relative contents over 5% were hexadecanoic acid(55.80%) and hexadecanoic acid ethyl ester(11.81%). Conclusion The volatile oil of nuanwei shule tablet mainly contains acids and esters.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    AiKeBaiEr&#;AnZhaEr;XiaMuXiNuEr&#;XiaoGaiTi;SiLaFu&#;AiBai
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    Objective To optimize the extraction technology of anthraquinones from the root of Radix Rumicis Obtusifolii.Methods The extraction study was carried out through orthogonal experiment regarding content of anthraquinones as an index .Results The total anthraquinones were thoroughly obtained by 30 min of circumfluence reflux with 15 times volume of water for 3 cycles. Conclusion The method is easy, quick and can be used for extracting the total anthraquinones from the root of Radix Rumicis Obtusifolii.

  • 药物制剂与药品质量控制
    CAO Gao-zhong;WU Ji-yu;HUANG Ai-fang;WANG Zhi-qiang
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    Objective To prepare the linezolid gel and control its quality.Methods Carbomer940 and glycerol were used as the main ancillary materials for the gel production, triethanolamine was used to regulate pH, the content was determined by HPLC.And the gel was stored at 25 ℃ for the stability study.Results The quality of the gel was stable and the content was accurate.The average recovery was 100.91%, RSD= 1.93% (n=9). Conclusion The preparation is simple and quality is controllable, which is an ideal clinic preparation.
  • 药物制剂与药品质量控制
    LV ling;LIU Hong;YU Jin;LUO Yuan-ju;SHEN Yu-li;WANG Qi;CHEN Dan;LI Shan
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    Objective To study the formulation and preparation of hydrochloric acid 5-aminolevulinic acid(5-ALA) liposomes.Methods The 5-ALA lipsomes were produced by using filmpH gradient method evaluated by the encapsulation efficiency which was determined by HPLC.The prescription of 5-ALA was optimized by the orthogonal design.The physical and chemical properties as the particle size and electronic potential were studied.Results The optimum preparation technics were obtained as follows: the ratio of lecithin to cholesterol was 6:1, lecithin to 5-ALA was 6:1,which were incubated at 60 ℃.The liposomes produced was milk white,with an average particle size of 100 nm, Zeta potential as -40 mV,and the average encapsulation efficiency was 65.0%. Conclusion The formulation of 5-ALA liposomes is reasonable, the technology is practicable and efficient.

  • 药物制剂与药品质量控制
    HUANG Ze-zhong;HE Li-hua;YIN Xiong-zhang
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    Objective To develop a method for determination of paeoniflorin in xiao’er huadu powder san by HPLC.Methods Chromatography was carried out on a column of HiQ sil C18 W(4.6 mm×250 mm,5 μm),at 30 ℃.The mobile phase was composed of acetonitrile0.1% phosphoric acid(83:17).The flow rate was 1.0 mL.min-1,and the detection wavelength was set at 230 nm.Results The content of paeoniflorin showed a good linearity in the range of 0.243-2.430 μg and the average recovery was 100.1%,with RSD as 1.61%(n=6). Conclusion The method is simple,rapid,accurate,reproducible and can be used for the quality control of the preparation.
  • 药物制剂与药品质量控制
    MA Hong-da;LI Yang;ZHAO Qing-chun;SHI Guo-bing
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    Objective To establish a HPLC method for determination of ferulic acid in tianning granules.Methods The RPHPLC method was used to determine the content of ferulic acid.The separation was achieved on Diamonsil ODS C18 column(200 mm×4.6 mm,5 μm)with a mobile phase of acetonitrile0.1% phosphoric acid (20:80) at a flow rate of 1 mL.min-1 by loading with 20 μL of samples, the wave length was set at 322 nm and the process was carried out at room temperature.Results The linearity range of ferulic acid was within 1.0-100.0 μg.mL-1,r=0.999 6.The average recovery was 99.78%,RSD=2.96%(n=9). Conclusion The HPLC method is simple, accurate, reproducible and highly selective, which can be used to determine the content of ferulic acid in tianning granules.
  • 药物制剂与药品质量控制
    CHEN Lin;HE Xiu-li;ZHU Hai-tao;FANG Nian-bo
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    Objective To optimize the technology of extraction for saponins in the roots of Momordica charantia.L.Methods The total saponins of Momordica charantia.L and Ginsenoside were taken as indexes,which were detected by spectrometric method.And optimum extraction technology for the total saponins was studied by the L9(34)orthogonal test. Results The optimum extraction technology was obtained as extracting twice, two hours for each, with 8 times 60% alcohol at 80 ℃. Conclusion The optimized technology is stable, feasible and reproducible,which provides evidence for total saponins extraction from the roots of Momordica charantia.L.
  • 用药指南
  • 用药指南
    ZHANG Dong-lin;LIU Dong;YAN Li
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    Objective To investigate the application of fluoroquinolone and provide the evidence for rational use of medicines.Methods The number and cost of fluoroquinolone consumed in 24 hospitals of Wuhan from 2008-2010, frequency of drug use (DDDs) and average daily costs (DDC) were analyzed statistically.Results During three years, the annual sales of fluoroquinolone were around 110-120 million, in which the injection occupied around 83%-84%.Levofloxacin, gatifloxacin, pazufloxacin, moxifloxacin, enoxacin had been ranked as the top five in sales, in which levofloxacin was the highest DDDs. Conclusion With the expanding use of fluoroquinolone, drug resistance becomes more seriously.The rational use and related index of drug economics of fluoroquinolone need further evaluating.

  • 用药指南
    ZHANG Hua-xiang;DENG Feng-xiang;XIAO Yong-xin;YANG Jie-jiao;XIANG Li
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    Objective To study the stability of the drugs in secondary packaging in Shenzhen area. Methods The drug contents at different observation time points were determined according to the methods from the Part Ⅱ of Pharmacopoeia of the People’s Republic of China (2010). Results The percentages of principal agents of the selected drugs were all above 90% in 12 months. Conclusion The expiry date of the drugs in secondary packaging in Shenzhen is at least 1 year.