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    药物研究
  • 药物研究
    SHI Suying;JIN Ketao;WANG Yuguang;GAO Yue
    2007, 26(9): 975-979.
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    ABSTRACTObjectiveTo study the effect of Aconitum coadministration with ampelopsis on the enzyme activity, protein expression and mRNA level of cytochrome P450 isoenzymes in rat liver. MethodsCYP1A2 and CYP2E1 activities were quantitated by high performance liquid chromatographic(HPLC) assay; CYP3A1/2 activity was quantitated by UV chromatography. The protein expressions of CYP1A2, CYP2E1, CYP3A1, and CYP3A2 were detected by Western blot. The mRNA levels of CYP1A2, CYP2E1, CYP3A1, and CYP3A2 were detected by semiquantitative reverse transcriptasepolymerase chain reaction(RTPCR). ResultsAconitum coadministration with ampelopsis obviously inhibited the activities of CYP1A2,CYP2E1 and CYP3A1/2; Western Blot showed a decreased protein expression of CYP2E1, and CYP3A2 , and an increased protein expression of CYP1A2 and CYP3A1. RTPCR showed an increased mRNA level of CYP1A2, CYP2E1, CYP3A1, and CYP3A2 as compared with the control group. Conclusion Aconitum coadministration with ampelopsis has an inhibitory effect on the enzymes activity of CYP1A2, CYP2E1, and CYP3A1/2. The enzymes activity inhibitory effect of CYP2E1 may be related to the decrease of its protein expression, but not CYP1A2, CYP3A1, and CYP3A2.
  • 药物研究
    LIU Lu;WANG Hong;ZENG Fanbo
    2007, 26(9): 980-982.
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    ABSTRACTObjectiveTo observe the effect of PVA eyedrop on xerophthalmia and its reserving time in eye. MethodsRose bengal solution ,0.1 mL of 1%,was instilled into the conjunctiva for cornea staining , 5 minutes later, it was washed by 0.9% sodium chloride, then slit lamp examination was done and the areas of staining were graded with grade index(M) evaluated. Schirmer’s test 2% lidocaine ,0.1 mL ,was instilled into the conjunctiva and 5 minutes later ,the excess fluid was dried with sucker, 4 minutes later , filter paper was placed into lower palpebra, and the lenth of paper wetting measured after 5 minutes. Light microscope, transmission and scanning electron microscope were used to study the changes in dry eye models. Results The result of Rose bengal stain showed that the grade indexes of all treatment and prophylaxis groups were positive with significant difference as compared with the control group(P<0.05).By schirmer’s test ,all treatment and prophylaxis groups showed very significant difference as compared with the control dry eye (P<0.01). As compared with the control group, PVA eyedrop could significantly increase the reserve time of drug in rabbit eye (P<0.01). It was showen by pathologic sections examination that after treatment with PVA eyedrop ,the basement cells in cornea grew actively ,showing high columnar type,and the defective area formed by desguamation of epithelial cells was coverd by new epithelial cells with regular cellular arrangement,i.e.,there was recovery of the damage from dry eye. ConclusionPVA eyedrop can be used as a substitute of tears for treating and preventing xerophthalmia.
  • 药物研究
    TANG Yinghong;WU Canrong;WEI Yun;JI Lan
    2007, 26(9): 983-986.
    ABSTRACTObjectiveTo evaluate in vitro and in vivo antibacterial activities of levofloxacin hydrochloride against clinical isolates and compare with levofloxacin and ofloxacin . MethodsMinimal inhibitory concentration (MIC) tests were carried out using the brothdilutions methods . The affecting factors were also determined. Drugs were administered intravenously 1 h after mice were infected intraperitoneally with 1 mL of bacterial suspension . The median effective dose (ED50) was calculated by the probit method.ResultsLevofloxacin hydrochloride had strong activity against grampositive bacteria , such as staphylococcus aureus , staphylococcus epidermidis and streptococcus pneumoniae with MIC50s 0.160.62 μg·mL1 . It was also active against gramnegative bacteria , such as escherichia coli , proteus and klebsiella pneumoniae with MIC50s 0.311.25 μg· mL 1. The antibacterial activity of levofloxacin hydrochloride decreased under acidic condition , increase of serum concentration and bacteria inoculum size . The protective effects of levofloxacin hydrochloride against experimental systemic infections were observed. ED50s of levofloxacin hydrochloride against staphylococcus aureus and escherichia coli were 4.54 and 1.21 mg·kg1, respectively .Levofloxacin hydrochloride was as active as levofloxacin and was more active than ofloxacin . ConclusionLevofloxacin hydrochloride shows a good activity against clinical isolates , its in vitro antibacterial activities can be changed by pH , serum concentration in culture media and inoculum size .
  • 药物研究
    HE Xuebin;JIANG Peng;XUE Cunkuan
    2007, 26(9): 987-988.
    ABSTRACTObjectiveTo observe the inhibitory effects of xiexiong tongmai diwan on experimental thrombosis. MethodsSilk suture was put into the common carotid arteryjugular vein to induce experimental thrombosis in the bypass vessel. The rats were fed with drugs(150,90,30 mg·kg-1·d1). The dry weight and inhibition rate were tested. ResultsThe inhibition rate of xiexiong tongmai diwan on experimental thrombosis were 30.0%40.0% with the wet weight of thrombus significantly decreased(P<0.05 or <0.01) .ConclusionXiexiong tongmai diwan has significantly inhibitory effect on experimental thrombosis.
  • 麻醉科用药专栏
  • 麻醉科用药专栏
    TONG Jiancheng;YAO Shanglong;ZHANG Guangxiong
    2007, 26(9): 996-998.
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    (2. ABSTRACTObjective To explore the effect of propofol preconditioning on lethal heatinduced rat pheochromocytoma(PC12) cells injury and the possible mechanism. MethodsPC12 cells were divided into 4 groups: control group, cells were untreated; lethal heat (H) group, cells were exposed to lethal heat (46℃ for 2 h); (P1+H) group and (P2+H) group in which propofol was added to the culture medium(the final concentrations of propofol were 25 μmol·L-1 and 50 μmol·L-1 respectively )1 h before exposed to lethal heat. MTT assay and LDH leakage were performed to study the cytotoxicity, superoxide dimutase (SOD) activity and malondialdehyde(MDA) formation were measured to reflect the activity of antioxidase. Results Compared with H group, elevation of MTT cell activity (P<0.01), and reduction of LDH leakage (P<0.01) in (P1+H) group and (P2+H) group were displayed, the activity of SOD was markedly decreased(P<0.01), and the content of cellular MDA was significantly increased(P<0.01). But there were no significant difference between (P1+H) group and (P2+H) group(P>0.05). ConclusionPropofol preconditioning produces protective effect against lethal heatinduced PC12 cells injury. The mechanism may be related to the ability of propofol against the oxidant injury.KEY WORDSPropofol; Preconditioning; Hyperthermia; PC12 cell
  • 麻醉科用药专栏
    YU Honghui;LUO Ailin;ZHOU Biyun;CHEN Yinghong;TIAN Yuke
    2007, 26(9): 999-1001.
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    ABSTRACTObjectiveTo compare the analgesic effects of varying regimens of butorphanol on patientcontrolled intravenous analgesia. MethodsOne hundred ASAⅠⅡ patients(3267 years) scheduled for elective orthopedic surgery under general anesthesia were divided randomly into four groups, 25 patients in each group. Group A received fentanyl 20 μg·mL-1, group B1 , butorphanol 0.1 mg·mL-1, group B2 ,butorphanol 0.2 mg·mL-1 and group B3 , butorphanol 0.4 mg·mL-1. The patients received PCIA when they were sent to postoperative recovery room with loading dose 2 mL, bolus 2 mL, and lockout time 10 minutes. Pain scores, drug consumption, sedative scores, blood pressure, respiratoy rate, SpO2 and HR were assessed at 0, 1, 4, 8, 12 and 24 hours after analgesia. The patients were considered having analgesia as uncomfortable when their VAS>3. Respiratory depression, nausea and vomiting, and pruritus were recorded . ResultsVAS in group B1 was significantly higher than that in groups B2 and B3 at 1 h and 4 h(P<0.05=;moreover, the number of VAS>3 was significantly higher in group B1 as compared with that in other groups(P<0.05=. In addition, we found that the sedative score in group B3 after the beginning of analgesia was higher than that in other groups, and the difference was significant at 1 h after analgesia(P<0.05=; furthermore, 21% patients (5/24) in group B3 had an incidence of over sedation with sedation scores≥3 ,which was higher than other groups but not significant. The patients in three butorphanol groups had higher sedative score with less respiratory depression, nausea , vomiting, and pruritus as compared with those in fentanyl group. ConclusionButorphanol 0.2 mg·mL-1 provides the optimum balance between pain relief and side effects following orthopedic surgery.
  • 麻醉科用药专栏
    ZHOU Hongmei;ZHOU Qinghe;XIAO Wangpin
    2007, 26(9): 1002-1003.
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    ABSTRACTObjectiveTo investigate the effect on hemodynamics during general anesthesia induction by remifentanil in gerontal patients.MethodsSixty ASA classⅠ~Ⅱ gerontal patients were randomly divided into three groups: group F、group R1 and group R2,20 cases in each group. In group F , anesthesia was induced by midazolam 0.05 mg·kg-1,fentanyl 3 μg·kg-1,propofol 1 mg·kg-1 and norcuron 0.1 mg·kg-1. In group R1,fentanyl was replaced by remifentanil 1 μg·kg-1.In group R2, fentanyl was replaced by remifentanil 1.5 μg·kg-1. The change in blood pressure and heart rate was observed with simultaneous recording of the dosage of atropine and ephedrine during induction.ResultsMAP1 and MAP2 in group R2 were significantly lower than other two groups(P<0.05=.HR1 and HR2 in group R2 were significantly slower than group F(P<0.05=.Conclusion Remifntanil can be used in gerontal patients during anesthesia induction,but the change in hemodynamics should be watched carefully.
  • 麻醉科用药专栏
    YU Li;LIU Liang;LI Kun
    2007, 26(9): 1004-1006.
    ABSTRACTObjectiveTo study the influence of propoful under the two different general anesthetics (isoflurane inhalation and isofluranepropofol intravenousinhalation combined anesthesia) on the gastric mucosa pH in laparoscopic cholecystectomy(LC) during CO2 aeroperitoneum . MethodsFortytwo patients with LC surgery were randomly divided into two groups. The patients were anesthetized with isoflurane inhalation (A group) or isoflurane propofol intravenousinhalation (B group). There were 21 patients in each group. The values of CO2 partial pressure difference between gastric mucosa and arterial blood , P(ia)CO2 ,and pH of gastric mucosa,pHi, were recorded at T1 ( before aeroperitoneum ),T2 (40 minutes after the beginning of aeroperitoneum ) and T3(40 minutes after the end of aeroperitoneum). ResultsP(ia) CO2 at T2 was significantly higher than that at T1 and P(ia)CO2 at T3 dropped significantly in both A group and B group(P<0.05= . P(ia)CO2 at T2 in group B was significantly lower than that in group A. Phi at T2 was significantly higher ,and P(ia)CO2 significantly lower in group B than those in group A (P<0.05=. The values of P(ia)CO2 and pH at T3 almost returned to the level at T1. Conclusion Isofluranepropofol intravenousinhalation combined anesthesia is in favor of stabling the PH value of gastric mucosa during CO2 aeroperitoneum . It improves the blood perfusion of gastric mucosa and reduces the complications after the operations.
  • 麻醉科用药专栏
    YAN Meijuan;ZHU Shengmei;LI Yuhong
    2007, 26(9): 1006-1010.
    ABSTRACTObjective To observe the effects of 0.375% ropivacaine epidural anesthesia on the dosage of intravenous anesthetics induction , recovery time ,and stress response. Methods Thirtytwo patients undergoing selected major abdominal surgery were randomly doubleblind allocated into one of two groups: Group TIVA received only intravenous anesthesia with propofol , sufentynl and vecuronium by plasma concentration controlled infusion. Group EIVA,on the basis of group TIVA , 0.375% ropivacaine epidural anesthesia was added as a combination. The intravenous anesthetics were delivered according to electroencephalographic bispectyal index (BIS ) value , TOF value of muscle paralysis monitor and hemodynamic changes. The dosages of intravenous anesthetics for anesthesia induction and maintenance were recorded. The time interval from the beginning of anesthesia induction to unconsciousness ,the time of intubation ,the time from stopping propofol to eyes opening ,and the time of extubation after operation were observed. Arterial blood sample was collected for determination of plasma glucose, adrenaline, and cortisol.Hemodynamic changes were observed. ResultsThere was no signficant difference in the dosage of propofol and sufentynl for anesthesia induction and maintenance between the two groups. There was no signficant difference between the two groups in time interval from beginning of induction to unconsciousness and intubation , and that from stopping of propofol to eyes opening and extubation. Patients in the two groups had higher plasma glucose during operation and after extubation than the baseline values(P<0.05=. During operation and after extubation , patients in group TIVA had higher plasma glucose,adrenaline and cortisol than those in group EIVA(P<0.05=.The patients in group TIVA had higher MAP during operation than that in group EIVA(P<0.05=,and were given more uradilminto to lower blood pressure(P<0.05=.Conclusion When combined with intravenous anesthesia in upper abdominal surgery ,0.375% ropivacaine epidural anesthesia can restrain the stress response in perioperative period ,but cann’t decrease the requirement of intravenous anesthetics for anesthesia induction and maintenance,and cann’t shorten the time interval of unconsciousness during induction and that for recovery after operation .
  • 药物与临床
  • 药物与临床
    TIAN Liqun;LEI Jian;ZHENG Qiongli;LI Zuomin;KE Yuhe
    2007, 26(9): 1021-1023.
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    ABSTRACTObjectiveTo observe the influence of tirofiban on vascular endothelialial function in percutaneous coronary intervention of patients with acute coronary syndrome.Methods Fifitysix patients with acute coronary syndrome underwent PCI and CAG from July 2004 to July 2005. These patients were divided into three groups: PCI group (n=20), PCI+tirofiban group (n=18) and CAG group(n=18).The blood samples were obtained before and immediately after PCI/or CAG respectively. The serum level of NO and von willebrand factor (vWF) were measured. ResultsThe serum level of NO and vWF in CAG group did not change. The level of NO decreased, but one of vWF increased significantly after PCI in PCI group (P<0.05=. The serum level of NO and vWF show a significant difference in PCI group and PCI+tirofiban group. The level of NO increased and one of vWF decreased after using tirofiban. Conclusion Tirofiban can protect the vascular endothelial cell and improve the endothelial function during PCI.
  • 药物与临床
    WANG Ling;LIU Huiguo;YANG Rongshi;ZENG Yulan
    2007, 26(9): 1023-1025.
    ABSTRACTObjectiveTo study the curative effect of moxifloxacin in the treament of early hospital acquired pneumonia. MethodsSixty seven cases of early hospital acquired pneumonia were randomly divided into moxifloxacin (400 mg i.v. drip qd for 7 d) treament group (34 cases) and ceftrlaxone( ampule 2.0 g , i.v. drip qd for 7 d) treament group (33 cases). The therapeutic effect and safty were compared between the two groups. ResultsThe effective rate in moxifloxacin treament group was 91.2% and 63.6% in ceftrlaxone treament group. The effective rate in moxifloxacin treament group was significantly higher than that in ceftrlaxone treament group(P<0.05=. ConclusionMoxifloxacin is a safe and effective antibiotic for the treament of early hospital acquired pneumonia.
  • 药物与临床
    YE Linfeng;WU Shuhui;ZHOU Xuhong;JIANG Xiaoqing
    2007, 26(9): 1026-1027.
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    ABSTRACTObjectiveTo investigate the therapeutic efficacy and safety of the combined use of nimesulide dispersible tablets with amoxicillin on the treatment of acute suppurative tonsillitis.MethodsOne hundred patients with acute suppurative tonsillitis were divided randomly into two groups: the combination treatment group was treated with nimesulide dispersible tablets 100 mg twice a day and amoxicillin sodium 500 mg three times a day for 7 d; the control group was treated with amoxicillin sodium 500 mg three times a day for 7 d. The beginning time of body temperature falling, the recovery time of body temperature, the disappearance time of tonsilar congestion, the disappearance time of tonsilar purulent secretion and the disappearance time of clinical symptoms were observed, with the efficacy of two groups evaluated by these indexes. ResultsThe results of the combination treatment group and the control group were as follows: the average beginning time of body temperature falling was 1.0 d and 1.5 d , respectively; the average recovery time of body temperature was 1.0 d and 2.5 d, respectively; the average disappearance time of tonsilar congestion was 1.5 d and 3.5 d ,respectively; the average disappearance time of tonsilar purulent secretion was 3.0 d and 5.0 d ,respectively; the average disappearance time of clinical symptoms was 3.5 d and 6.0 d ,respectively; the recovery rates were 78.8% and 62.5% ,respectively; the total response rates were 98.1% and 79.2%, respectively. ConclusionThe efficacy of the combined use of nimesulide dispersible tablets and amoxicillin sodium on the treatment of acute suppurative tonsillitis is better and faster than that of the use of amoxicillin sodium alone.
  • 药物制剂
  • 药物制剂
    CHEN Baolin;YANG Xin;ZHANG Changgong
    2007, 26(9): 1064-1067.
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    ABSTRACTObjectiveTo prepare betulinic acid sustainedrelease tablets and investigate their release characteristics. MethodsDifferent particle sizes of betunilic acid and HPMC,different viscosity grades and amount of HPMC and different pressures were used to prepare betulinic acid sustainedrelease tablets. The drug release was determined in 0.5%SDS solution medium. ResultsThe HPMC particle size, viscosity grade and the particle size of betulinic acid had greater influence on drug release. Accompanying the increasing amount of HPMC, the drug release rate slowed down. ConclusionThe releasing behavior of the betulinic acid sustainedrelease tablets in vitro through simulation of the Peppas equation, the n value of release index was found to be 0.75, indicating that the betulinic acid sustainedrelease tablets release by both diffusion and erosion (anomalous transport). The main factors affecting drug release are particle size of betulinic acid and HPMC, and the content of HPMC.
  • 药物制剂
    XU Xianwu;CHEN Keli
    2007, 26(9): 1067-1069.
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    ABSTRACTObjectiveTo study the methods and technological parameters of the purification process of total alkaloids from Leonurus Heterophyllus by means of cation exchange resin. MethodsThe purification process of total alkaloids from Leonurus Heterophyllus was performed by means of 732 Cation Exchange Resin , and the content of total alkaloids from Leonurus Heterophyllus was determined as an index by spectrophotometry to choose the optimal technological parameters. ResultsTen grams 732 cation exchange resin could absorb 100.79 mg of the total alkaloids,and 5% hydrochloric acid can wash off 83.1% of the total alkaloids. The content of total alkaloids in the purified extract of Leonurus Heterophyllu was above 50%.Conclusion732 cation exchange resin has the good ability of absorbing the total alkaloids from Leonurus Heterophyllus.It can be used for purificating total alkaloids from Leonurus Heterophyllus.
  • 药物制剂
    HUANG Lili;FEI Luhua;ZENG Fanbo;CHENG Bo;ZHANG Limin;LV Baihua
    2007, 26(9): 1070-1071.
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    ABSTRACTObjectiveTo investigate the preparation technology of compound lidocaine hydrochloride suppository. MethodsWith lidocaine hydrochloride and zinc oxide as the chief drug, semisynthetic glyceride as the matrix, surfactant Tween80s of different doses were employed to study the correlation between the drug release rates from suppositories and the concentrations of Tween80. ResultsDrug was released more rapidly from suppositories accompanying an increasing dose of Tween80. When the concentration of Tween80reached 1%, drug release could reach above 90% in 60 min. ConclusionTween80 can increase the release rate of drug from suppositories. The suppositories with 1% Tween80 can meet the design requirements.
  • 药物制剂
    LI Dongming;GE Baosheng;WANG Zhong
    2007, 26(9): 1072-1074.
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    ABSTRACTObjectiveTo improve the plastic packing (antiseptic) craft of shengmai oral liquid to make the production operation simply controllable. MethodsOrthogonal testing method was used to optimize the boiling antisepsis and the heat preservation packing craft .ResultsThe technological conditions were determined as follows :the preservation temperature was controled to 60 ℃, the solution pH to 4.0, the time limit of heat preservation to with in 8 hours,with detection result conforming internal control standard. ConclusionThe test results provide the experimental basis for determinaing the formal production craft.
  • 药品质量控制
  • 药品质量控制
    ZHAO Jiangqiong;YI Yimu;XU Yi
    2007, 26(9): 1075-1076.
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    ABSTRACTObjectiveTo establish a simple method of determination on total saponin in Fistular onion bulb by colorimetric method. MethodsUsing diosgenin as a standard substance , the reaction condition of vanillin colorimetric method was optimized through orthogonal experiment. The reaction condition was to heat samples heat for 30 min at water bath of 80 ℃ after adding 0.5% vanillin glacial acetic acid 0.2 mL and glacial acetic acid 1.0 mL. ResultsThe concentration of total saponin in fistular onion bulb extract was 11.50%,and the average recovery was 101.30% with relative standard deviation of 2.08%(n=6). ConclusionThis colorimetry method is simple and reliable to measure the concentration of total saponin in fistular onion bulb.
  • 药品质量控制
    HUANG Qiaoqiao;CHEN Xuefan;LI Huilin
    2007, 26(9): 1077-1078.
    ABSTRACTObjectiveTo establish HPLC method for the determination on the content of diacerein and its related substances. MethodsA C18 column was used , the mobile phase of acetonitrilewater (adjust pH to 2.7 with acetic acid) (47:53) and the detection wavelength was 254 nm. ResultsDiacerein and related substances could be well isolated. The calibration curve was linear in the range of 12~100 μg·min1 with r=1.000 0(n=7). The detection limit was 0.5 ng. ConclusionThis method is simple, rapid, accurate and suitable for the determination on the content of diacerein and its related substances.
  • 药品质量控制
    MEI Zhinan;SUN Xianming;LI Xiaokuan
    2007, 26(9): 1079-1080.
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    (1. ABSTRACTObjectiveTo establish an HPLC determination of andrographolide and dehydroandrographolide contents in xiaoyanzhike tablets. MethodsA ZORBAX XDBC18 Column (4.6 mm×150 mm, 5 μm) was used, methanol water (55:45) was used as mobile phase , the detection wavelength was 250 nm, flow rate 1.0 mL·min1 and column temperature at 25 ℃. Results Linear rang of andrographolide was 14.5~145.0 μg·mL1 (r=0.999 8), linear rang of dehydroandrographolide was 11.7~117.0 mg·mL1(r=0.999 9) , the average recovery of andrographolide was 98.8 % and the average recovery of dehydroandrographolide was 99.4 %.ConclusionThe method is simple, accurate ,reliable and can be used to control the quality of this preparation .
  • 药品质量控制
    LIU Jianhua;YIN Jiye;YANG Dezhu
    2007, 26(9): 1081-1083.
    (1. ABSTRACTObjectiveTo establish the related substsnce examination in miconazole nitrate ointment by HPLC. MethodsA C18 column was used with the mobile phase of 0.5%NH4ACCH3CN and CH3OH (1:1) mixture solution (200:900) . The detection wavelength was 230 nm .Results Linearity regression was A=0.439 0 C+0.411 9 , r = 0.999 9 . Repetitiveness RSD was 1.59% (n= 5) . Detectability was 0.33 ng . ConclusionThis method is single,rapid , and accurate ,suitable for examining the related substance examination in ointment preparation.