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    药物研究
  • 药物研究
    ZHANG Han;HUANG Yifei;WANG Liqiang;LIU Li
    2006, 0723(8): 723-0724.
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    To study the effect of a small-molecule compound J2 in the inhibition of skin allograft rejection in mice.MethodsC57BL/6 and Balb/c mice were used as donors and recipients respectively for the establishment of a skin allograft model. 45 mice with the model were then randomly divided into 3 equal groups. Mice of group A, B and C were given each placebo,10 mg·kg1 of cyclosporin A and 30 mg·kg1 of J2 administered by gastrogavage q.d., respectively. The course of treatment in the 3 groups lasted 12 days beginning at the day of transplantation. The graft survival time in mice of the different groups was assessed with the KaplanMeier analysis. 14 days after the transplantation, histological examination of the skin graft was carried out.ResultsThe average graft survival time in mice of allograft control (group A) was (13.7±1.4) d. The average graft survival tomes in mice of group B treated with cyclosporin A and mice of group C treated with J2 were (18.2±2.1) d and (17.7±2.4) d, respectively, both of which being significantly longer than that of group A (P<0.01). The difference between the average graft survival times in mice of group B and C, however, was insignificant(P>0.05). Histological examination demonstrated that no apparent lymphocyte infiltration could be found in the skin graft of mice treated with J2 (group C).ConclusionThese results show that J2 can inhibit allograft rejection dramatically.

  • 药物研究
    ZENG Ning;TANG Li;YUAN Jing;WU Ke;ZHOU Jie;HU Tao;CHEN Zhonghua
    2006, 0723(8): 725-0728.
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    To survey the effect of thalidomide on the survival of allograft skin in mice so as to probe into the role of the drug in resisting allograft rejection. MethodsThe skin transplantation model was set up by grafting skin flaps from Balb/c to C57BL/6 mice. 36 mice with the skin allograft model were randomly divided into 3 equal groups:① the control group,② cyclosporin(Cy A) group and ③ thalidomide (Tdm) group. Mice of group ① were given each an IP injection of 200 mL·kg1·d1 of 0.9% sodium chloride solution plus Tween 80(1∶999). Mice of group ② were given each an IP injection of 10 mg·kg1·d1 of CyA while those of group ③ were given each an IP injection of 200 mg·kg1·d1 of Tdm. A part of mice of the 3 groups was sacrificed on day 7,9 and 11 of the experiment separately and their skin grafts were taken for pathological examination. The average survival times of the allograft in the remaining mice of the different groups were noted down. ResultsThe average survival times of the allografts in mice of the control group, Cy A group and Tdm group were 8.2 days, 13.5 days and 13.2 days, respectively. Both of the average survival times of the allografts in mice of the Cy A group and Tdm group were significantly longer than that in mice of the control group(P<0.05, P<0.05). The difference between the average graft survival times in mice of the Cy A group and Tdm group, however, was insignificant(P>0.05). Pathologic examination of the skin grafts taken from mice sacrificed on day 7,9, and 11 of the experiment revealed a gradual aggravation of subcutaneous lmphocytic infiltration and destruction of glands and capillaries in animals of all 3 groups along with the prolongation of time. However, the destructive changes in the subcutaneous tissue was most serious in grafts from mice of the control group. The destructive changes were far less severe in skin grafts from mice of the Tdm group while those in skin grafts from mice of the Cy A group were the most trifling. Conclusion Thalidomide was shown to prolong the survival of skin allograft form Balb/c mice to C57BL/6 mice,denoting a fair prospect of its clinical application.
  • 药物研究
    FANG Shiping;WANG Zhiyong;SUN Manchun;LUO Guoqing
    2006, 0723(8): 729-0731.
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    To survey the effects of the 4 separate components (AngiSY1, AngiSY2 , AngiYS1 and AngiYS1)of the Chinese Angelica root intravenous injection on the rat with a model of cerebral ischemia. Methods56 SD rats were randomly divided into 7 equal groups: ① the model group, ②sham operation group,③ red sage root injection group, ④ AngiSY1 group, ⑤ AngiSY2 group, ⑥AngiYS1 group and ⑦ AngiYS2 group. The model of cerebral ischemia was set up in the rats by ligating bilateral common carotid arteries under urethan anesthesia except for the animals of the sham operation group that were subjected to the same operation but without ligation of the carotid arteries. after the operation, rats of groups④⑤⑥ and ⑦ were given each a daily intraperitoned injection of 12.48 mL·kg1 of AngiSY1 ,AngiSY2, AngiYS1 and AngiYS2, respectively. Rats of group ③ were given each a daily intraperitoneal injection of 12.48 mL·kg1 of red sage root glucose solution while animals of the model group (①) and sham operation group (②) received injections of equivalent amounts of 0.9% sodium chloride by the same route. 2 weeks later, the contents of nitric oxide in the brain and serum, the activity of superoxide dismutase(SOD) in the brain tissue and levels of serum melonyldialdehyde(MDA) were determined. ResultsIn comparison with animals of the model group, rats of the groups AngiSY2, AngiYS1 and AngiYS2 had a much lower content of NO in the brain (P<0.01). Rats of AngiSY1 group had also a lower NO content in the brain (P<0.05). Rats of groups AngiSY1, AngiSY2, AngiYs1 and AngiYS2 had a significantly higher SOD activity in the brain tissue (P<0.01), and among these, rats of the AngiYS2 showed the highest SOD activity. Animals of the groups AngiSY2, AngiYS2 showed a striking decrease in the serum MDA content (P<0.01) while rats of the AngiSY1 had a prominent increase in the content of serum MDA (P<0.01). ConclusionThe 3 components of the Chinese Angelica root intravenous injection AngiSY2、AngiYS1 and AngiYS2 were shown to exert protective effective effects on the rat with a model of cerebral ischemia.
  • 药物研究
    ZHANG Hong;LI Guigang;XIE Erjuan;HU Weikun;ZHANG Jinling;CHENG Zheng
    2006, 0723(8): 732-0733.
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    To study the effects of water soluble azone on the viability and ultrastructure of corneal endothelial cells of the rabbit cultured in vitro in order to determine the safe concentration of the drug in its clinical application to ophthalmologic patients. MethodsCorneal endothelial cells of the rabbit were cultured in vitro with the digestion method. Cells of the 3rd or 4th generation were inoculated to 96well plates with a concentration of 1×104 cells·L1. The cells were then divided into 8 groups one of which serving as control with no addition of water soluble azone. To the remaining 7 groups of cells water soluble azone was added to bring about the drug concentrations of 0.001,0.005,0.010,0.050,0.100,0.500 and 1.000 g·L1,respectively. Viability of the cells were determined with the MTT method 24 h later. Cells of the 3rd or the 4th generation in a concentration of 1×104 cells·L1described above were pipetted onto sterile slides. Water soluble azone in concentration of 0.010,0.100 and 0.500 g·L1 was added to these cells, acting for 10 min. The ultrastructure of the cells was then examined under the scanning electron microscope. Besides, rabbit corneal endothelial cells in primary culture were subjected to the action of water soluble azone in the same concentrations described above for 10 min followed by electron microscopic examination as well. ResultsThe viability of cultured rabbit corneal endothelial cells in their 3rd or 4th generation was not significantly affected by water soluble azone in concentrations≤0.100 g·L1 acting for 24 h. The drug in concentrations≥0.500 g·L1, however, was shown to cause a reduction of the cell viability after acting for 24 h(P<0.01). The 10 min action of water soluble azone in concentration≤0.100 g·L1 was shown to result in slit formations on the memborane of the rabbit corneal endothelial cells but no significant changes in the organelles as shown by electron microscopy. Water soluble azone in concentrations≥0.500 g·L1, however, led to apoptosis of most of the cultured rabbit corneal endothelial cells. ConclusionWater soluable azone at concentrations no higher than 0.100 g·L1 was shown to have no harmful effects on the viability and ultrastructure of cultured rabbit corneal endothelial cells and may increase the permeability of the cell membrane to the drug. Water soluble azone may also be used in the research work of gene transfection of corneal endothelial cells.
  • 药物研究
    WANG Yan;LIU Min;ZHANG Yuanzhen
    2006, 0723(8): 734-0736.
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    To survey the preventive and therapeutic effects of tetramethylpyrazine(TMP) on rat embryos with fetal growth restriction(FGR) as well as its protective effects on the fetal brain. Methods80 pregnant SD rats were randomly divided into 4 equal groups: the control group, the model group, high and low dose TMP groups. The FGR model was set up with the passive smoking method in each animal of the model, high and low dose TMP groups. From the 7th to the 20th gestation days, rats of the high and low dose TMP groups were given each 0.4 g and 0.2 g of TMP administered by gastrogavage q.d., respectively. Animals of the control group and model group were given each equivalent amounts of 0.9% sodium chloride solution administered by gastrogavage q.d . as well. On day 21 of gestation, 10 rats from each of the 4 groups were sacrificed and the fetuses were taken for the measuring of body weight and body length as well as preparation of stereotaxic atlas of the brain and ultrathin brain sections for electron microscopic examination. The neonates given birth by the 10 remaining rats of each of the 4 groups were subjected to the same measurement and preparation as described above 1 day after the natural delivery. ResultsThe fetuses of the rats of high and low dose TMP groups had significantly greater body weight and body length as compared with those of rats of the model group (P<0.01). Disruption and even disappearance of mitochondrial cristae, chromatin aggregation and attachment around the nuclear membrane in neurous of the hippocampal CA1 region in neonates of the model group were demonstrated by electron microscopy. In contrast, only mitochondrial swelling was shown in a portion of the neurons of neonates of the high dose and low dose TMP groups, a condition similar to that in neonates of the control group. ConclusionTetramethylpyrazine was shown to promote the growth and development of the rat fetus, effectively preventing and treating FGR as well as protecting the brain development of rat neonates.
  • 药物研究
    HU Qiaohong;JIANG Hongyan;XU Donghang;YANG Huizhen
    2006, 0723(8): 737-0739.
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    To study the effect of electric field direction on the percutaneous penetration of the nonionic drug caffeine mediated by skin electroporation and iontophoresis. MethodsThe percutaneous penetration of a saturated water solution of caffeine through the human cadaver skin by passive diffusion, electroporation (exponentially decaying pulse, voltage=350 V, pulse frequency=4 pulses·min1, pulse number=25, capacity =22 μF ) and iontophoresis [0.25 mA·(cm2)1, 4 h] was studied with the twochamber diffusion cell method in order to inspect the influences of electroporation and iontophoresis on the speed and cumulated amount of the drug through the skin. The effect of electric field direction on the enhanced percutaneous penetration of caffeine mediated by iontophoresis and electroporation was compared. ResultsThe speed and cumulated amounts of caffeine through the skin mediated by electroporation and iontophoresis were both significantly greater than those by passive diffusion. The speed and cumulated amount of caffeine across the skin mediated by positive electroporation were similar to those by negative electroporation, while the speed and cumulated amount of the drug across the skin mediated by positive iontophoresis were significantly greater than those by negative iontophoresis. The enhancing effect of iontophoresis was greater than that of electroporation on the percutaneous penetration of caffeine in the present experiment. ConclusionIn comparison with passive diffusion, electroporation and iontophoresis were shown to significantly increase the speed and cumulated amount of the nonionic drug caffeine passing through the skin. The direction of electric field had no obvious influence on the enhancing effect of electroporation but had significant influence on the enhancing effect of iontophoresis.
  • 药物研究
    JIA Mengliang;XIE Shouxia;ZHANG Wanfan;PANG Chunping;YANG Hongying;YANG Jixiang;LI Jianglin
    2006, 0723(8): 737-0739.
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    To study the protective effects of Ginkgo bilobae extract(EGb) on the mouse with a model of acute ischemiareperfusion injury of the kidney. Methods30 mice of the Kunning strair were randomly divided into 3 equal groups: the sham operation group, ischemiareperfusion model group, and trial group. Mice of the trial group were given each an intraperitoneal injection of 0.1 mg·g1 of EGb, while those of the model group and sham operation group were given each an intraperitoneal injection of equivalent amount of 0.9% sodium chloride solution. 30 min later, mice of the 3 groups were subjected to chloral hydrate anesthesia. The right kidney of each of the mice of the trial group and model group was removed. The left kidney was then exposed and the renal pedicle was clamped for 45 min followed by declamping and reperfusion for 24 h. Mice of the sham operation group were submitted only to right side nephrectomy followed by suturing of the surgical incision. 24 h after the operation, mice of all 3 groups were sacrificed. Serum creatinine(Cr) and blood urea nitrogen(BUN) were determined and the left kidney was subjected to histopathological examination. ResultsThe serum Cr[(49.90±12.02) μmol·L1] and BUN[(26.36±7.41) mmol·L1] in mice of the model group were significantly higher than those [(21.40±2.67) μmol·L1] and [(7.20±0.84) mmol·L1] in mice of the sham operation group, respectively(P<0.01, P<0.01). In contrast, the serum Cr[(30.20±6.30) μmol·L1] and BUN[(15.37±3.77) mmol·L1 ] in mice of the trial group were significantly lower than those in mice of the model group, respectively(P<0.01, P<0.01). Although these values were higher in mice of the trial group than those in mice of the sham operation group, the differences, however, were statistically insignificant. Striking ischemic changes in the renal tuberlar epithelial cells in mice of the model group were demonstrated while these changes were trivial in the renal tubular epithelial cells in mice of the trial group. ConclusionEGl was shown to exert dramatic protective effects on the mouse with a model of acute ischemiareperfusion injury of the kidney.
  • 药物研究
    CHEN Hao
    2006, 0723(8): 743-0745.
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    To probe into the protective effects of minocycline on the rat brain with a model of ischemiareperfusion injury and their underlying mechanisms. Methods40 adult male SD rats in good health were randomly divided into 4 equal groups:① the sham operation group, ② ischemiareperfusion model group, ③ minocycline group and ④ 0.9% sodium chloride solution group. A model of ischemia reperfusion injury of the brain in each of the rats in group ②③ and ④ was set up by creating a transient occlusion of the middle cerebral artery according to the method deseribed by Kuizami et al.. Rats of the group ① (sham operation were subjected to the same operation except for that the cerebral artery was not occluded. Rats of group ③ and ④ were given each an intraperitoneal injection of 450 mg·kg1 of minocycline injection and an equivalent amount of 0.9%sodium chloride solution, respectively, after the beginning of the ischemiareperfusion injury. The cerebral functions of the animals were assessed with the five grade scoring method after the 90 min ischemia and 24 h reperfusion. The rats were then sacrificed by decapitation and the activity of lactic dehydrogenase(LDH) of the ischemic cerebral cortex was determined, and RTPCR method was used to assay the expression of the nerve growth factor receptor TrkAmRNA in the cerebral cortex of rats in all 4 groups. ResultsA striking improvement in the impaired cerebral function in rats of the minocycline group was demonstrated by a much lower scoring[(0.95±0.46) in average] as compared with that of the ischemiareperfusion model group[(2.28±0.73) in average](P<0.05). The cerebral cortex LDH activity and expression of TrkA mRNA in rats of the minocycline group were [(7.91±0.32)×103 U·g1 in average]and [(1.28±0.04) in average],respectively, which were significantly higher than those in rats of the model group[(5.12±0.36)×103 U·g1 in average ] and [(0.71±0.06) in average],respectively(P<0.01,P<0.01). Conclusion Minocycline was shown to exert protective effects on the rat brain subjected to an ischemiarepersion injury possibly by regulation of the expression of the nerve growth factor TrkA.
  • 药物研究
    YE Wu;MAO Wei;HUA Junyi;LIU Yan
    2006, 0723(8): 746-0747.
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    To probe into the effects of atorvastatin on the proliferation and cell cycle of cultured human umbilical vein endothelial cells (HUVECs) in a hypoxic environment. MethodsHUVECs were cultured in a DMEM medium with 10% fetal calf serum in 24 well plates with a concentration of 1×105 cells per well. The cells were then randomly divided into 5 groups, with 8 wells of cells per group. Cells of the normal control group were further incubated in a serumfree DMEM medium for 12 h under normoxic condition. Cells of the hypoxia model group were further incubated in a serumfree DMEM medium for 12 h in a hypoxia device(PO2<1.0 kPa).Cells of the low, medium and high dose trial groups were further incubated in a serumfree DMEM mediumn containing 0.05,0.10 and 0.20 mmol·L1 of atorvastatin, respectively, for 12 h in the hypoxia device. The proliferation of the cells was assayed with the MTT method while the preparations of cells in their different cycles were analyzed with flow cytomelry.ResultsProliferation of the cells was strikingly depressed in the hypoxic environment. Atorvastatin in different concentrations was shown to significantly promote the proliferation of the endothelial cells subjected to hypoxia (P<0.05 or P<0.01 as compared with cells of the hypoxia model group). The doseeffect relationship, however, was not linear. Atorvastatin at the medium dose was shown to have the strongest effect in promoting the cell proliferationa. The drug at the high dose had a much weaker effects on the promotion of cell proliferation. Atorvastatin in different doses was also shown to result in significant increase in the proportion of the cells in S phase and reduce that of the cells in G0/G1 phase. ConclusionAtorvastatin in appropriate concentrations was shown to promote the proliferation and DNA synthesis of HUVECs in a hypoxic environment. It seems possible that atorvastatin may play a certain role in the neogenesis of blood vessels in the ischemic myocardium.
  • 药物研究
    ZHAO Yongjiu;CHEN Zhaodian;SHEN Liming;HE Chaoqi;ZHAN Zhaohui;Ren Fujin;YAO Ji;TANG Zhongmu
    2006, 0723(8): 748-0750.
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    To study the effect of alcohol on the testicular cell apoptosis in the rat. Methods72 adult male Wistar rats were randomly divided into 3 equal groups. Rats of the control group were given each 6 mL·kg1 of 0.9% sodium chloride solution administered by gastrogavage q.d.. Rats of the trial group A and trial group B were given each 6 mL·kg1 and 12 mL·kg1 of alcohol(50% alcohol, containing 0.378 g of ethanol per mL),respectively, administered by gastrogavage q.d.. The course of treatment in all 3 groups lasted 39 days. On each of the 14th ,27th and 40th day of the experiment, 8 rats from each of the 3 groups were sacrificed by cervical dislocation and the testes were removed for the assay of testicular cell apoptosis with flow cytometry(FCM) and fluorescent staining (FITCArnexin V/PI). ResultsTesticular cell apoptosis indexes (AI) in rats of the control group on the days 14,27and 40 were (7.41±1.97)%,(9.06±2.36)% and (8.58±1.64)% respectively, differences between these values being insignificant(P>0.05). The AIs in rats of the trial group A on the days 27 and 40 were (48.26±6.27)% and (53.18±6.56)% ,respectively,the difference being insignificant as well(P>0.05). However, they were significantly higher than the AI on the day14 (13.07±2.05)%(P<0.01). The AIs in rats of the trial group B on the days 27 and 40 were (53.41±6.93)% and (59.89±7.05)%, respectively,the difference being insignificant(P>0.05). They were, however, significantly higher than the AI on the day 14 (19.68±3.84)%(P<0.01). AI in rats of both the trial groups A and B on the days 14,27 and 40 were significantly higher than those in rats of the control group on the corresponding days, respectively (P<0.01). The AI in rats of the trial group B was significantly higher than that in rats of the trial group A on the day 14(P<0.01). ConclusionAlcohol administered by gastrogavage was shown to increase the apoptosis of testicular cells in the rat in a dosage and timedependant manner in the first 27 days, and the extent of the apoptosis then became stable within 40 days.
  • 药物研究
    LEI Xiaoguang;HUANG Jiangeng;GONG Wenhui;SI Luqin;LI Gao
    2006, 0723(8): 751-0752.
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    To study the bioequivalence of the 2 preparations of benzoyl metronidazole in the human body. Methods18 healthy male subjects were divided into 2 equal groups with a randomized, open and doubleblind crossover experimental design. Subjects of the 2 groups were given each a single oral dose of 1 280 mg of the test preparation benzoyl metronidazole suspension and reference preparation benzoyl metronidazole capsules, respectively. The serum concentrations of the drug were then determined with HPLC at different time points after the medication and the bioequivalence of the 2 preparations was compared. ResultsThe main pharmacokinetic parameters of the test preparation benzoyl metronidazole suspension and reference preparation benzoyl metronidazole capsule were as follows: Cmax were (10.79±0.96)μg·mL1 and (10.12±2.12)μg·mL1,tmax , (4.00±0.84)h and(4.67±1.14)h,t1/2 , (10.69±2.46)h and(10.80±2.00)h; AUC0→t, (196.25±30.67)μg·h1·mL1 and(191.95±30.13)μg·h1·mL1,AUC0→∞, (207.26±37.46)μg·h1·mL1 and(202.64±34.49)μg·h1·mL1, respectively. The relative bioavailability of the test preparation benzoyl metronidazole suspension was (103.60±17.50)%. ConclusionThe method used in the study was shown to be sensitive, accurate and handy and the Results showed that the two preparations of benzoyl metronidazole were bioequivalent.
  • 药物研究
    XIA Chunhua;MIN Shengyun;DAI Qun;ZHANG Xinjing;XIONG Yuqing
    2006, 0723(8): 753-0755.
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    To develop a microbiological method for the determination of the blood concentration of azithromycin so as to assess the bioequivalence of the entericcoated azithromycin tablets and reference azithromycin tablets in healthy volunteers. MethodsThe azithromycin concentrations in the blood plasma were determined with by a microbiological method at different time points after a single oral dose of 500 mg of tested azithromycin entericcoated tablets and ordinary azithromycin tablets given respectively to each of the 24 healthy male volunteers in an open randomized crossover design。 The pharmacokinetic parameters and relative bioavailability were calculated for the assessment of the bioequivalence of the 2 dosage forms. ResultsThe AUC0→144 h of the tested azithromycin entericcoated tablets and ordinary azithromycin tablets were (21.021±4.053) and (20.597±3.850) mg·h1·L1, Cmax were(0.583±0.073)and(0.603±0.061) mg·L1,tmax were(3.900±0.800)and(3.000±0.700)h,t1/2 were(29.799±1.935)and(28.850±1.598)h,respectively. These main pharmacokinetic parameters showed that the differences between the 2 dosage forms of the drug were not statistically significant. ConclusionThe method was simple, convenient and rapid. The 2 dosage forms of azithromycin were bioequivalent. The absorption of the tested azithromycin entericcoated tablets in the human body, however, was slower than that of the reference tablets.
  • 药物研究
    LIU Yu;LIU Dong;LIU Zhelong;ZHU Shuihong;ZHANG Donglin;QIU Lin;LIU Yi;WANG Zhen
    2006, 0723(8): 756-0757.
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    To study the pharmacokinetics of mosapride citrate tablets in healthy humans. Methods12 healthy male volunteers were given each a single oral dose of 10 mg of mosapride citrate tablets. The concentrations of mosapride in the blood plasma before the administration and at different time points within 10 hours after the medication were determined with HPLC [Stationary phase: a Hypersil C18 chromatographic column(5 μm, 4.6 mm×200 mm) ; flow rate: 1.0 mL·min1;mobile phase: 0.02 mol·L1 potassium dihydrogen phosphate solution(pH adjusted to 5.0 with 1 mol·L1 phosphoric acid solution)∶acetonitrile=75∶25; column temperature:40 ℃; excitation wavelength:314 nm; emission wavelength:352 nm]. The DAS 1.0 program was used to calculate the pharmacokinetic parameters. ResultsThe management process of mosapride citrate in the human body after the administration accorded with the onecompartment model. The main pharmacokinetic parameters of the drug were as follows: Ka was(1.45±0.93) h1;tmax (determined value) was (1.15±0.57) h;Cmax, (58.57±22.01) μg·L1;AUC0→10 ( 176.60±69.40) μg·h1·L1;t1/2, (1.41±0.38) h.ConclusionThe pharmacokinetic process of mosapride citrate in the human body was shown to be in accordance with the onecompartment model.
  • 抗微生物药物专栏
  • 抗微生物药物专栏
    CHEN Zhilan;XIE Shouzhen
    2006, 0723(8): 765-0766.
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    To study the in vitro antimicrobial effects of 14 Chinese herbal medicines (CHMs) on Candida albicans. MethodsAlcoholic extracts of the following 14 CHMs were prepared: coptis root, Phellodendron bark, giant knotweed rhizome, clove, pomegranate rind, Chinensis Franch,Chinese gall, pulsatilla root, hairy vein agrimony, forsythia root, honey suckle flower, flavescent sophora root, cnidium fruit and chebula fruit. The extracts were then diluted into solutions containing 1 000.00, 500.00, 250.00, 125.00, 62.50, 31.25 mg·mL1 of the cuude drug, respectively. The in vitro antimicrobial effects of the 14 CHMs on Candida allicans were determined with the disk diffusion method and disk dilution method. ResultsThe minimal inhibitory concentration (MIC) of coptis root was 6.25 mg·mL1. The MIC of Phellodendron bark and giant knotweed rhizome was 25.00 mg·mL1.The MIC of clove, pomegranate rind, Chinensis Franch and Chinese gall was 50.00 mg·mL1. The remaining CHMs were shown to have no apparent inhibitory effect on Candida albicans in vitro. ConclusionAmong the 14 CHMs, coptis roots was shown to have the strongest in vitro inhibitory effect on Candida albicans. Giant knotweed rhizome, Phellondendron bark, clove, pomegranate rind, Chinensis Franch and Chinese gall had also in vitro inhibitory effects on the microbe to a certain degree.
  • 抗微生物药物专栏
    PENG Li;LUO Yongai;CHEN Baowen;LI Youlun;SHEN Xiaobing;WANG Guozhi
    2006, 0723(8): 767-0770.
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    To observe the effect of bacteriophage D29 on the humoral as well as cellular immune function of guinea pigs with a model of tuberculosis. MethodsGuinea pig models of drugsensitive and drugresistant tuberculosis were set up by using the method of subcutaneous challenge with the corresponding bacteria. The animals infected with drugsensitive or drugresistant bacteria were then randomly divided into the following groups respectively: the control group, bacterophage group, rifampin(RFP) group and combined chemotherapy group. Guinea pigs of the control group were given each 0.9% sodium chloride solution administered by gastrogavage q.o.d.. Those of the RFP group were given each RFP solution containing 15 mg·kg1 of the drug administered by gastrogavage 3 times a week. Animals of the combined chemotherapy group were given each RFP+ethambutol+pyrazinamide+levofloxacin administered by gastrogavage q.o.d., the doses of the 4 drugs being 15,25,25 and 6 mg·kg1, respectively. Guinea pigs of the bacteriophage group were given each 1×108 PFU(0.5 mL) of bacteriophage D29 administered by nasal dripping 3 times a week. The course of treatment in all 4 groups lasted 4-7 weeks. The dynamic changes in the serum titer of neutralizing antibodies against the bacteriophage in animals of the bacteriophage group, the changes in serum levels of IL1, IL4, IFNγ in animals of all 4 groups 4 weeks after the beginning of the experiment were kept under observation. Phagocytosis of the bacteriophage by the macrophage was examined with electron microscopy. ResultsNeutralizing antibodies against the bacteriophage began to appear in the sera of the guinea pigs after they had been treated with the bacteriophage for 18 days and the titers of the antibodies were positively correlated with the time. Macrophages were shown to phagocytize and digest a portion of the bacteriophages as revealed by electron microscopy. The serum IL2 contents in guinea pigs with the model of drugsensitive tubercle bacilli infection were greater than those of the control animals after the former had been treated with RFP or the bacteriophage for 4 weeks. The serum IL2 contents in guinea pigs with the drugresistant tubercle bacilli infection were greater in those animals treated with RFP, bacteriophage and combined chemotherapy as compared with those in control animals. Among these, animals treated with the bacteriophage had the highest serum IL2 content as compared with that of the controls (P<0.05). Differences between the different groups of animals with respect to serum IL4 and IFNγ levels were insignificant. ConclusionThe bacteriophage was shown to be provided with antigenic characteristics. It could stimulate the organism to produce neutralizing antibodies and promote the cellular immune function of the body so that the latter could act synergetically with the bacteriophage in the elimination of tubercle bacilli in the organism.
  • 抗微生物药物专栏
    XU Chengrong;LI Wengang;LI Yan
    2006, 0723(8): 771-0772.
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    To assess the therapeutic effectiveness of ganciclovir in the treatment of condyloma accuminatum(CA). MethodsSixtyone patients with CA were randomly divided into 2 groups: the trial group and the control group. Patients of the trial group (n=31, 1 case excluded from the group later during the treatment course) and control group (n=30) were given each 0.25 g of ganciclovir and 0.25 g of aciclovir administered by intravenous instillation q.d. for 5 consecutive days, respectively, after the bodies of the warts in all of the patients had been extirpated with laser. The clinical recurrence rates and adverse reactions of the drugs in patients of the 2 groups were compared. ResultsThe recurrence rate of CA within 3 months in patients of the trial group(25.81%) was significantly lower than that in patients of the control group(53.33%)(P<0.05). The incidences of adverse reactions of the drugs in patients of both groups were low. ConclusionGanciclovir was shown to be safe and effective in the treatment of CA.
  • 抗微生物药物专栏
    ZHANG Jianchu;XIN Jianbao;YANG Weibing;XIONG Xianzhi;LI Hong;JIN Yang;ZHANG Xiaoju;GUO Yi
    2006, 0723(8): 773-0774.
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    To assess the therapeutic effectiveness and safety rate of gatifloxacin hydrochloride in the treatment of infections of the respiratory or urinary system. Methods225 patients with infections of the respiratory or urinary system were randomly divided into 2 groups: the trial group (n=114) and control group (n=111). Patients of the trial group were given each 0.4 g of gatifloxacin hydrochloride tablets PO,q.d. while those of the control group were given each 0.2 g of levofloxacin, PO, b.i.d.. The course of treatment in both groups lasted 7-14 days. The therapeutic effectiveness and adverse reactions of the drugs were kept under observation. ResultsIn patients of the trial group and control group, the clinical effective rates were 88.60% and 92.79%, the bacteria elimination rates were 94.32% and 96.63% and the incidences of adverse reactions were 9.32% and 11.97%, respectively. Differences between the 2 groups with respect to the above mentioned data were insignificant (P>0.05). ConclusionGatifloxcin hydrochloride was shown to be effective and safe in the treatment of infections of the respiratory or urinary system.
  • 药物与临床
  • 药物与临床
    WEN Xiuying;XIONG Liang;LIU Hao;WANG Qinghua
    2006, 0723(8): 782-0784.
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    To probe into the therapeutic effectiveness of Zhenqing prescription (ZQP) in the treatment of senile patients with diabetic nephropathy(DN).Methods98 cases of type 2 diabetes mellitus with senile diabetic nephropathy were randomly divided into two groups: the trial group(n=50) and control group(n=48). Patients of both groups were subjected to the same basic treatment including restriction of sodium salt ingestion, intake of high-quality low-protein diet, oral administration of gliquidone or hypodermic injection of insulin, amlodipine PO if complicated by hypertension, isosorbide mononitrate PO if complicated by coronary heart disease. Patients of the trial group were given each additionally 50 mL of ZQP oral liquid t.i.d., while those of the control group were given each additionally 10 mg of benalapril q.d.. The course of treatment in both groups lasted 3 months. Blood glucose, blood lipids, serum tissueplasminogen activitator(tPA) and plasminogen activator inhibitor1(PAI1) activities, 24 hour urine microalbumin excretory rate(UAER) and urine protein quantity(24h UPQ), blood urea nitrogen(BUN) and serum creatinine(SCr) in patients of both groups before and after the treatment were determined. Results The overall effective rates in patients of the trial group(86.0%) was significantly higher than that in those of the control group(72.9%)(P<0.05). Levels of blood glucose, blood lipids, UAER, 24h UPQ, BUN and SCr were significantcantly lowered after the treatment in patients of the trial group(P<0.01 or P<0.05). Besides, these parameters in patients of the trial group were also lower than the corresponding ones in patients of the control group(P<0.05). ConclusionZQP was shown to be effective in the treatment of diabetic nephropathy in senile patients probably by improving blood glucose and lipid metabolism as well as regulating tPA/PA11 activities.
  • 药物与临床
    CHEN huaqian;LIU wei;HUANG yunfang;ZHAO li;YANG tao
    2006, 0723(8): 785-0786.
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    To study the safeness and tolerability of high-dose valsartan (higher than that currently approved by the Food and Drug Administration) in the treatment of chronic kidney disease(CKD). MethodsEighteen patients with a history of diabetic or nondiabetic CKD were enrolled in an 8week open-label trial. The patients received valsartan(an angiotensin-receptor blocker) treatment with an initial dose of 160 mg·d1 PO. 2 weeks and 4 weeks later,the daily dose of the drug was increased to 320 mg and 640 mg, respectively. Treatment with the daily dose of 640 mg of the drug, which was 4 times higher than the currently approved maximum dose, lasted the subsequent 4 weeks. The safeness and tolerability of the highdose drug was appraised by monitoring the blood pressure, serum creatinine and potassium levels of the patients. Results Highdose valsartan was well tolerated by the patients. No serious drugrelated adverse reactions were encountered. The average serum creatinine concentration throughout the study fluctuated near the baseline level[(2.1±0.3) mg·dL1]. The differences between the baseline level and the maximum as well as the minimum serum creatinine concentrations were not significant(P>0.05, P>0.05). The average serum potassium concentration[(5.0±0.6) mmol·L1] during the 640 mg daily dose period was similar to that of the baseline level[(4.9±0.5)mmol·L1] (P>0.05). ConclusionSupramaximal doses of valsartan was shown to be safe and well tolerated in the treatment of patients with CKD, resulting in lowering of blood pressure and reduction of proteinuria.
  • 药物制剂
  • 药物制剂
    SHI Hui;SHANGGUAN Yingying;Weng Lin
    2006, 0723(8): 810-0811.
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    To study the formula and preparation technology of aminobutyric acid for injection and to set up a method for its content determination. MethodsThe excipients of the sterilized powder of the aminobutyric acid for injection were screened and its preparation technology was studied. The content of aminobutyric acid was determined with the precolumn derivation HPLC by reacting with 6aminoquinolyNhydroxysuccinimdyl carbamate(AQC). The other amino acids were assayed with thin layer chromatography (TLC). The stability of the sterilized powder of the aminobutyric acid for injection was inspected. ResultsThe best excipient for the aminobutyric acid for injection as glycine. The RPHPLC method was sensitive and accurate in the content determination of aminobutyric acid and the TLC method was feasible in the assay of other amino acids. The preparation of aminobutyric acid also showed good stability. ConclusionThe preparation technology of the aminobutyric acid for injection was shown to be simple and convenient, and the preparation was also stable.
  • 药品质量控制
  • 药品质量控制
    LIU Xinyun;GAN Chunying;LI Zhirong;YAN Wenqiang
    2006, 0723(8): 821-0822.
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    To set up an HPLC method for the simultaneous determination of ephedrine hydrochloride and furacilin in compound furacilin nose drops. MethodsStationary phase: HypersilC18 stainless steel column(150 mm×4.5 mm,5 μm);mobile phase: methanol -0.02 mol·L1ammonium dihydrogen phosphate buffer solution [pH adjusted to (3.5±0.1) with H3PO4 and ammonia solution](45∶55) ; flow rate: 1 mL·min1 ;detection wavelength: 260 nm. ResultsGood linear relationships were shown when the concentrations of ephedrine hydrochloride and faracillin were within the range of 40-600 mg·L1 and 0.8-2.0 mg·L1, respectively. The average rates of recovery of ephedrine hydrochloride and furacilin were 99.98%, RSD=0.15% and 99.95%, RSD=0.14%, respectively. The replication of the method was good. ConclusionThe method was shown to be handy, accurate and may be used in the quality control of the preparation.