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    药物研究
  • 药物研究
    DU Juan;WANG Qiongshu;JIA Ruhan
    2005, 24(4): 0-0.
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    ObjectiveTo study the effect of rhubarb extract on the expression of cycline kinase inhibitor p27 and glomerular cell proliferation in experimental murine glomerulosclerosis, so as to probe into the mechanism of rhubarb in retarding the progress of glomerulosclerosis.Methods24 adult male Wistar rats were randomly divided into 3 equal groups: the control group, the glomerulosclerosis group and test group. Rats of the glomerulosclerosis group were submitted to extirpation of the left kidney under aseptic condition. 7 days later these rats were given each an IV injection of 5 mg·kg-1 of doxorubicin. 28 days after the operation, each of these rats received another IV injection of 3 mg·kg-1 of doxorubicin. Rats of the test group were subjected to the same operation and the same IV injections as the animals of the glomerulosclerosis group. In addition, rats of the test group were given each by gastrogavage 0.5 mg·kg-1of rhubarb extract dissolved in 10% sodium cellulose, q.d., beginning from the day of operation .Rats of the control group were submitted to sham operation and received equivalent volumes of 0.9% sodium chloride solution by gastrogavage as well. 13 weeks after the operation or sham operation, 24 h urine specimen of each animal was collected and all rats of the 3 groups were then sacrificed. Blood urea nitrogen(BUN), serum creatinine(SCr) ,quantity of 24 h urine protein, profile of the average area(AG)and volume(VG)of the glomerulus were determined. Glomeruli were separated and the total RNAs extracted. Expression of PCNA(proliferation cell nuclear antigen) mRNA on the glomeruli was assayed with RTPCR while the expression of PCNA and cycline kinase inhibitor p27 in the glomeruli was detected with immunohistochemical methods. ResultsLevels of BUN and SCr were much lower and amounts of 24 h urinary protein much smaller in rats of the test group than those of the glomerulosclerosis group(P<0.05 or P<0.01). Histopathological examination revealed that the pathological lesions in the kidneys of the rats of the test group were distinctly milder and AG and VG remarkably smaller than those in rats of the glomerulosclerosis group. A significant attenuation of the expression of glomerular PCNA mRNA accompanied by a decrease in the proliferation index and an upregulation of p27 protein expression(P<0.01) was demonstrated in rats of the test group, as compared with those indices of the glomerulosclerosis group . ConclusionRhubarb extract was shown to retard the progress of glomerulosclerosis possibly by upregulating the glomerular expression of p27 and alleviating the glomerular cell proliferation .
  • 药物研究
    CHEN Siyan;ZHOU Yiping;HE Lihua;CHEN Qiyou;YANG Jinghua
    2005, 24(4): 0-0.
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    ObjectiveTo probe into the longterm toxicity of aceclofenac in rats. Methods112 Wistar rats were randomly divided into 4 groups. Both the low and medium dose groups consisted of 24 rats .Animals of these 2 groups were given each by gastrogavage 3 and 6 mg·kg-1·d-1 of aceclofenac ,respectively. 32 rats of the high dose group were given each in the same way 12 mg·kg-1·d-1 of aceclofenac, and 32 rats of the control group were given each equivalent volume of 0.5% CMC-Na(sodium carboxymethyl cellulose). The term of treatment in all 4 groups lasted 3 months .Indexes of hematology and blood biochemistry, weight coefficients of organs, histopathology of various organs etc., were subjected to systematic examinations.Results Accidental degeneration and necrosis of the gastrointestinal tract , increased content of serum total cholesterol and increased weight coefficient of the liver were demonstrated in rats treated with aceclofenac in a daily dose of 12 mg·kg-1 . These changes,however, disappeared after the drug administration had been discontinued. Rats treated with the drug in daily doses of 3 and 6 mg·kg-1 showed no significant changes as mentioned above. ConclusionA daily dose of 6 mg·kg-1of aceclofenac was safe in the rats and the pathological changes resulted from administration of 12 mg·kg-1·d-1of the drug were shown to be resversible.
  • 感染科用药专栏
  • 感染科用药专栏
    DAI Yongan;NING Yiyun;WU Hui;GAO Shicheng;LUO Mingqi
    2005, 24(4): 0-0.
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    ObjectiveTo probe into the shortterm effect of lamivudine in the treatment of chronic hepatitis B(CHB) patients with lowlevel replication of HBV. Methods119 patients with CHB served as the subject of the study. Prior to the study,the liver function of these patients had repeatedly been shown to be abnormal. HbeAg, as well as HBV DNA assayed with dot hybridization ,was negative. HBV DNA, however, was shown to be postive when tested with PCR. These patients were randomly divided into 2 groups.59 patients of the test group were given each 100 mg of lamivudine, PO, q.d..60 patients of the control group were submitted only to conventional liver protective and general supportive therapy. The course of treatment in both groups lasted one year. Liver function was checked monthly while HBV DNA was assayed with PCR every three months in patients of both groups during the course of treatment. ResultsAt the termination of the treatment,the serum HBV DNA in 56 patients of the test group turned to be negative in the PCR and the liver function of 52 patients of the same group was completely restored to normal. The corresponding numbers of patients in the control group were 6 and 31, respectively. ConclusionLamivudine was shown to be effective in the treatment of CHB patients with serum HBV DNA detected by PCR but not by dot hybridization.
  • 药物与临床
  • 药物与临床
    XIONG Jing;LIU Jianshe;ZHU Zhonghua;WANG Yang;ZENG Ji;HU Haiyan
    2005, 24(4): 0-0.
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    ObjectiveTo probe into the clinical effectiveness and safety rate of gatifloxacin in combination with vancomycin in the treatment of enterococal infection of the urinary tract.Methods48 inpatients with enterococal infection of the urinary tract were randomly divided into 2 equal groups with the matchedpair method. 24 patients of the control group were given each 2.0 g of vancomycin administered by IV instillation q.d.. 24 patients of the treatment group were given each 400 mg of gatifloxacin and 1.0 g of vancomycin administered by IV instillation q.d.. The course of treatment in both groups lasted 14 d. The clinical effectiveness and incidence of adverse reactions in patients of the 2 groups were compared. ResultsThe clinical effective rates in patients of the control group and the treatment group were 91.7% and 87.5%, respectively (P>0.05).24 of the 33 strains(72.7%) of Enterococcus faecalis were sensitive to gatifloxacin. The elimination rates of enterococcus in patients of the control group and the treatment group were 83.3% and 75.0% ,respectively (P>0.05). Abnormalities of renal function were shown in 3 patients of the control group. No major adverse reactions were encountered in patients of the treatment group. ConclusionThe majority of enterococci, in particular E. faecalis were sensitive to gatifloxacin. The effect of gatifloxacin combined with vancomycin in the treatment of enterococcal infection of the urinary tract was reliable. The dose of vancomycin in the combined therapy could be reduced by 50%, so that adverse reactions could be decreased and tolerance of the enterococcus to vancomycin could be prevented.
  • 药物制剂
  • 药物制剂
    WU Wei;YANG Zheng;CHEN Ya;SHU Lingling;ZHANG Xigang
    2005, 24(4): 0-0.
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    ObjectiveTo develop a method for the preparation and quality control of compound ornidazole emulsion. MethodsTo sodium carboxymethyl cellulose (CMCNa) was added water for injection quantum satis. Sodium bisulfite was added after complete swelling of the CMC-Na, followed by trituration for thorough mixing. Cod liver oil,Tween-80,ornidazole and ketoconazole were then successively added, followed by trituration for thorough mixing.By adding water and further trituration finally, the preparation of compound ornidazole emulsion was finished. The content of ornidazole in the suspension was determined with dual wavelength κratio spectrophotometry. ResultsThe calibration curves were linear when the concentrations of ornidazole and ketoconazole were within the ranges of 7.04-14.08 μg·mL-1 , r=0.999 5 and 9.984-19.968 μg·mL-1 ,r=0.999 9 (n=7), respectively. The average rates of recovery of ornidazole and ketoconazole were 100.10%(RSD=0.58%, n=4) and 100.10%(RSD=0.90%, n=4), respectively.ConclusionCompound ornidazole emulsion was shown to be stable, handy in preparation and the method of its quality control was accurate.
  • 用药指南
  • 用药指南
    FANG Qingxia;HOU Sien
    2005, 24(4): 0-0.
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    ObjectiveTo analyze the treatment and pharmacoeconomics in patients with chronic bronchitis complicated by deep mycotic infection in the hospital. MethodsCase histories 126 patients with chronic bronchitis admitted to our hospitals from September 2003 to April 2004 were reviewed and an analysis of the kinds and duration of the application of antibiotics, the use of glucocorticoids, site of mycotic infection, kinds of fungi, the use of antimycotics , as well as expenses and average duration of hospitaligation was carried out.ResultsProlonged use of large amount of broadspectrum antibiotics was the major factor leading to mycotic infection. In addition, application of glucocorticoids was another pathogenic factor inducing mycotic infection in the hospital. Chronic bronchitis complicated by mycotic infection resulted in an striking increase in the duration and expenses of hospitaligation.ConclusionRational use of broadspectrum antibiotics and glucocorticoids, cutting down the incidence of mycotic infections in the hospital are of great significance for controlling the increase in medical expenses and saving health expenditures of our country.
  • 用药指南
    LIN Nengming;FANG Luo;WU Yefang
    2005, 24(4): 0-0.
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    ObjectiveTo study the stability of fluorouracil injection in 8 different conventional infusion fluids.MethodsA clinical routine dose of fluorouracil injection was added to each of the 8 conventional infusion fluids and the mixtures were kept at 25 ℃ and 35 ℃ for 240 h. RPHPLC was used to determine the contents of fluorouracil in the fluids at different time points. Besides, the outward appearance, pH value, changes in the ultraviolet absorption spectrum and chromatogram were kept under observation. ResultsWithin the 10 days. the outward appearance, pH value(RSD<2%), fluorouracil content(RSD<2%), ultraviolet absorption spectrum and chromatogram of each of the 8 different fluids were shown to have undergone no apparent changes at different temperatures.ConclusionFluorouracil injection was shown to be stable in 8 conventional infusion fluids within 10 days.
  • 药物研究
  • 药物研究
    CHEN Menglan;RUAN Jinlan
    2005, 24(4): 0-0.
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    Objective To extract and identify the active chemical constituents of Wujincao.MethodsSilica gel column chromatography and Sephadex LH-20 gel column chromatography were used to separate the active chemical constituents from Wujincao. The structures of the monomers thus obtained were identified with physicochemical and spectrum analyses.Results 4 active chemical constituents were separated from Wujincao and their structures identified named AristololactamⅠ, 9-methoxyaristololactamⅣ, β-sitosterol and 1-octacosanol.Conclusion 4 active chemical compounds were isolated from this genus for the first time.
  • 药物研究
    LI Lin;ZHANG Zhihua;WU Jianliang;JIN Zheng
    2005, 24(4): 0-0.
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    ObjectiveTo study the behavioral and pathological changes characteristic of Alzhemier’s disease (AD) induced by high iron concentration in the cerebrospinal fluid in rats.Methods16 adult Wistar rats were randomly divided into the test group (n=10) and the control group(n=6). Rats of both groups were anesthetized by giving an intraperitoneal injection of 40 mg·kg-1 of pentobarbital to each animal. 10 rats of the test group were then given each an injection of 10 μL of artificial cerebrospinal fluid(CSF) containing 52 μg·μL-1of ferric chloride into the lateral ventricles of the brain. Rats of the control group were given each an injection of 10 μL of artificial CSF via the same route. These injections were repeated on the fifth and tenth days. Behavioral changes were assayed with the Morris water maze test. Apoptotic cells of the murine cerebral cortex were detected with flow cytometry, Aβ immune plaques stained with immunohistochemical methods and ultrastructural changes examined by transmission electron microscopy. ResultsThe average times for rats of the test group and control group to reach the platform were (34.67±2.82 ) s and (17.79±2.04)s, respectively (P<0.01). The average distances for rats of the test group and control group to reach the platform were (1 122.00±3.24) cm and (617.00±2.51) cm , respectively (P<0.01). The percentages of apoptotic cells from rats of the test group and control group were (14.27±0.40) % and (3.20±0.19) %, respectively(P<0.01). Light browncoloured Aβ immune plaques were seen widely interspersed in the cerebral cortex and hippocampus of rats of the test group. Vacuolar degeneration of neuronal processes accompanied by dense bodies formed as a result of mitochondria degeneration was shown in the brain of the rats of the test group. ConclusionBehavioral and pathological changes characteristic of AD were induced in rats by high iron concentration in the cerebrospinal fluid in rats
  • 药物研究
    HU Wenjun;WAN Xinxiang
    2005, 24(4): 0-0.
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    ObjectiveTo study the antiHBV effect of the active principle of Styelec plicata in vitro. MethodsThe active principle of Styelec plicata was extracted and separated from the fresh organism. HBV transfected cells of the 2.2.15 cell line were coincubated with the active principle in different concentrations(64,32,16,8,4,2,1 mg·mL-1) in 96 well plates for 12 days. The titers of HBsAg and HBeAg in the supernatants of the culture medium were then determined and served as indices for assessing the antiHBV effect of the drug. The median toxic dose(TD50) of the active principle for the cells were assayed with the MTT test. The therapeutic indices of the drug were also determined. ResultsThe active principle of Styelec plicate was shown to have a relatively prominent inhibitory effect on the secretion of both HBsAg and HBeAg. The toxicity of the principle to the cells was low and its therapeutic indices were all greater than 10. ConclusionThe active principle of Styelec plicata was shown to have an evident anti- HBV effect in vitro.
  • 感染科用药专栏
  • 感染科用药专栏
    YANG Daofeng;WU Liang;ZHANG Bei;TIAN Deying
    2005, 24(4): 0-0.
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    ObjectiveTo assess the therapeutic efficiency and safety rate of rifaximin in the treatment of acute bacterial infection of the intestine. MethodsA multicentre, random, doubleblind and doubledummy parallel control protocol was employed in the trial. 211 patients with acute bacterial infection of the intestine were randomly divided into the treatment group and control group. 107 cases in the treatment group were given each 0.2 g of rifaximin, PO, q.6 h. and 1 ciprofloxacin dummy tablet, PO,b.i.d.. 104 cases in the control group were given each 0.25 g of ciprofloxacin, PO, b.i.d. and 2 rifaximin dummy tablets,q.6 h.. The course of treatment in both groups lasted 5 days.The therapeutic efficiency of the 2 drugs was appraised. ResultsThe overall effective rates in patients of the treatment group and control group were 94.4% and 96.1%,respectively, while the corresponding cure rates were 75.7% and 84.6%,respectively. The bacteria elimination rates were 96.2% and 96.3%,respectively, and the incidences of adverse reactions were 2.8% and 2.9%, respectively. Differences between the two groups were not statistically significant(P>0.05).ConclusionRifaximin was shown to be effective and safe in the treatment of acute bacterial infection of the intestine. Its adverse reactions were rare and mild. The therapeutic efficiency and safety rate of rifaximin were similar to those of ciprofloxacin.
  • 药品质量控制
  • 药品质量控制
    WANG Xiayan;MAO Wei
    2005, 24(4): 0-0.
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    ObjectiveTo set up an HPLC method for the determination of the content and homogeneity of chlorphenamine maleate in xiaoeranfenhuangnamin granules.MethodsIn the method, a C18 column(4.6 mm×250 mm,5 μm) was used,the mobile phase was methanol0.5 mol·L-1 sodium dihydrogen phosphatetriethylamine(150∶850∶0.25),its pH value being adjusted to 2.3 with phosphoric acid,the flow rate was 1 mL·min-1 and the detection wavelength , 215 nm.The external standard method was adopted for the assay. ResultsA good linear relationship was shown when the amount of chlorphenamine maleate applied was in the range of 0.05-0.50 μg(r=0.999 8).The average recovery rate of was 96.02%,RSD=0.9%(n=5).ConclusionThe method was shown to be simple, quick , precise and well reproducible.
  • 药物研究
  • 药物研究
    ZHU Xiaohua;SHI Youen
    2005, 24(4): 0-0.
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    ObjectiveTo probe into the adjuvant effect of interleukin 12(IL-12) in the immunization of mice with Schistosoma japonicum fatty acid binding protein (Sj14FABP)DNA vaccine. MethodspVIVO2,pVIVO2-IL-12,pVIVO2-Sj14FABP plasmid DNAs were prepared in large amounts. 48 male Balb/c mice were randomly divided into 4 equal groups : A,B,C and D. Mice of all the 4 groups were given each an I.M. injection of 30 μL of 0.75% bupivacaine hydrochloride into the quadriceps femoris . One day later, mice of group A ,B,C and D were given each an I.M. injection of 100 μL of 0.9% sodium chloride solution, 100 μg of pVIVO2 plasmid DNA, 100 μg of pVIVO2-Sj14FABP plasmid DNA and 50 μg of pVIVO2Sj14FABP plasmid DNA as well as 50μg of pVIVO2-IL-12 plasmid DNA ,respectively. 30 days thereafter, each mouse of all the 4 groups was challenged with (40±2 ) Schistosoma japonicum cercariae. 45 days after the challenge, all of the animals were sacrificed for counting the number of the recovered adult worms and the eggs of the parasites in the liver. The serum levels of IgG antibodies were assayed with ELISA. ResultsThe worm reduction rates of group C and D were 24.11% and 38.83% ,respectively, meanwhile, the egg reduction rates in the liver of group C and D were 27.20% and 40.27% , respectively. The difference between groups D and group C were significant(P<0.05). 30 days after the immunization, the titer of IgG in mice of all the 4 groups did not increase dramatically,and the differences of the IgG levels were not significant among the 4 groups (P>0.05).ConclusionSj14FABP DNA vaccine was shown to induce a partial protective immunity against Schistosoma japonicum infection in Balb/c mice, and IL-12 was found to be a good adjuvant of Schistosoma DNA vaccine.
  • 药物与临床
  • 药物与临床
    LIAO Zhipin;ZHANG Yi;TIAN Yuke
    2005, 24(4): 0-0.
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    ObjectiveTo study the timecourse of the cerebral uptake of propofol and ketamine during intravenous infusion of the drugs at a constant speed. Methods30 ASA I-Ⅱ grade adult patients scheduled for elective surgeries were randomly divided into 2 groups,the propofol group and ketamine group.Patients of the 2 groups were given each 6 mg·kg-1·h-1 of propofol and ketamine ,respectively, administered by intravenous instillation lasting 35 min at a constant speed. Blood samples were taken simultaneously at different time points from the radial artery and internal jugular venous bulb for the determination of the concentrations of propofol and ketamine. ResultsThe arterial blood concentrations (Ca)of both drug sincreased progressively along with the ongoing instillation,reaching a stable plateau 15 min later. The propopol concentrations in the venous blood from the internal jugular venous bulb(Cijbv) increased gradually from 0 to 30 min of the instillation. They were, however, lower than Ca at every corresponding time point(P<0.05).From the 30th to the 35th minute, the Cijbv of propopol came to a stable plateau, which was near to Ca of the drug. In patients of the ketamine group, Cijbv increased along with time from 0 to 20 minutes of instillation but were lower than Ca of the drug at corresponding time points(P<0.05). From the 20th to the 30th minute, Cijbv of ketamine was kept stable,nearing that of Ca of the drug. Before reaching stabilization of the cerebral drug uptake, the AUCa-v in patients of the ketamine group was greater than that of the propofol group(P<0.05). ConclusionCerebral uptake of propofol and ketamine had been shown to be timedependent before the uptake of the drugs by the brain reached its equilibrium. The dynamic equilibrium of the cerebral drug uptake lagged behind the equilibrium of arterial drug concentrations.Propofol and ketamine were shown not or hardly to be metabolized by the human brain.