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    药物研究
  • 药物研究
    RAO Zichao;SI Luqin;GUAN Yanbin;XU Jiaqiang;LI Gao
    2010, 29(12): 1535-1539. https://doi.org/10.3870/yydb.2010.12.001
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    ABSTRACTObjectiveTo evaluate the effect of Cremophor RH40based selfmicroemulsiflying drug delivery system (SMEDDS) on the activity of CYP3A in rats. MethodsThe pharmacokinetics parameters for midazolam (MDZ),as a probe, and its metabolite 1’hydroxymidazolam were estimated from the plasma concentrations determined by HPLC.Effects of the SMEDDS on the intestinal CYP3A enzymes activity was detected by western blot analysis. ResultsThe pharmacokinetics parameters showed that oral bioavailability of MDZ in microemulsion was 3.14fold higher than that of Dormicum, and which inhibited the activity of CYP 3A by decreasing the ratio of AUC0∞ (1′OHMDZ)/ AUC0∞ (MDZ) in comparison to Dormicum (0.11 vs. 0.25, P<0.05). MRT and t1/2 of MDZ were obviously prolonged in MDZ microemulsiontreated group compared with Dormicum group [MRT:(1.23±0.38) vs.(0.63±0.13) h; t1/2:(0.65±0.25) vs.(0.33±0.11) h, P<0.05]. A significant decrease in CYP3A protein expression was observed in rat intestine mucosa treated with microemulsion. Conclusion It was found that the Cremophor RH40based SMEDDS inhibited the activity of CYP3A and significantly improved the oral bioavailability of MDZ in rats.
  • 药物研究
    WANG Xi;WANG Xin;TANG Yanhong;WANG Teng;XU Chao;HUANG Congxin
    2010, 29(12): 1539-1542. https://doi.org/10.3870/yydb.2010.12.002
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    ABSTRACTObjectiveTo study the effects of wenxin granule on the activation kinetics of transient outward potassium current(Ito) in single ventricular myocytes. MethodsThe wholecell patchclamp technique was used to investigate the effcts of wenxin granule(1, 5, 10, 20 g•L1)on Ito in acute isolated ventricular myocytes of adult rats. ResultsWenxin granule inhibited the current density of Ito and the decreased rates of peak Ito were (15.31±7.21)%, (32.86±5.08)%, (53.25±4.74)%, (73.23%±4.11)% at 1, 5, 10, 20 g•L1, respectively. The currentvoltage curve was shifted downward, and steadystate inactivation curve shifted rightward by wenxin granule. ConclusionWenxin granule has antiarrhythmic effects by blocking ventricular myocytes Ito of rats.
  • 药物研究
    HUANG Yanjing;GUI Ling;YU Shiying
    2010, 29(12): 1542-1545. https://doi.org/10.3870/yydb.2010.12.003
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    ABSTRACTObjectiveTo study the effects of aspirin on cell cycle of human glioma H4 cells, and explore its anticancer mechanisms. MethodsProliferation inhibition was detected by MTT assay. The cell cycle distribution of H4 cells induced by aspirin was analyzed by flow cytometry. The apoptosis of H4 cells induced by aspirin was determined by Annexin VFITC/PI double staining. The expression variation of p21 and p27 in H4 cells(treated with aspirin or not) were analyzed by Western blotting. ResultsAspirin inhibited proliferation of H4 cells in a dose and timedependent manner. In aspirin 8 mmol•L-1 group, the proportion of G0/G1 phase significantly increased compared with that of control group. Aspirin treatment could induce apoptosis of H4 cells, and also upregulate the expression of p21 and p27 proteins. ConclusionAspirin treatment could induce cell cycle arrest and apotosis, which might be associated with upregulation the p21 and p27 proteins expression.
  • 药物研究
    RABIGUL &#;Islam;YULTUZ &#;Mamat;MAHSUT&#;Kadir;YAN Ming;SIRAPIL &#;Abay
    2010, 29(12): 1546-1548. https://doi.org/10.3870/yydb.2010.12.004
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    ABSTRACTObjectiveTo investigate the toxicity of Datura stramonium L. seeds of Xinjiang. MethodsThe acute and subacute toxicity were tested on Datura stramonium L. seeds of Xinjiang in mice. Results①Acute toxicity: the maximum tolerance dose of Datura stramonium L. seeds is 40 g•kg-1; ②Subacute toxicity: the serum AST,ALT,BUN,Cr parameters were studied: compared with model group, serum AST in Datura stramonium L. seeds of Xinjiang group were increased(P<0.05)on the second day; and serum AST,ALT,BUN were raised(P<0.05 or P<0.01)on the seventh and fourteenth day; and serum Cr were also increased on the fourteenth day. Serum MAO,TCHE parameters were studied: compared with model group, serum TCHE in Datura stramonium L. seeds of Xinjiang group were increased(P<0.05)on the second day(female) and seventh day(female);and serum MAO were raised(P<0.01).ConclusionDatura stramonium L. seeds of Xinjiang possesses chronic toxicity; It could damage liver and kidney in mice and also inhibite acetylamine enzyme in female mice.
  • 药物研究
    SHEN Yanchun;ZHOU Dan;TUO Xinlan;CHEN Qiongxia
    2010, 29(12): 1549-1551. https://doi.org/10.3870/yydb.2010.12.005
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    ABSTRACTObjectiveTo study the effects of longterm administration of melatonin(MEL)on inflammation in subtotally nephrectomized rats and to explore the mechanism. MethodsEstablished a model of subtotal (5/6) nephrectomy(STN)and took melatonin (5 mg•kg1•d1) for 40 weeks. The changes of inflammatory cells infiltration(ED1) at the 1st, 2nd, 4th, 8th, 12th, 16th, 26th and 40th week after operation were detected. ResultsThe indexs of infiltration of inflammatory cells increased on the remnant kidney in STN group, which were lessened in renal interstitiun remarkably(P<0.05, P<0.01) in MEL group. ConclusionMelatonin has therapeutic effects on inhibiting inflammtion in interstitium by reducing urinary protein excretion.
  • 药物研究
    LI Li;WANG Jin;LU Furong;PING Yehong;WANG Wangdong;HAN Xiao;LIU Jianshe;LIU Jianguo
    2010, 29(12): 1552-1555. https://doi.org/10.3870/yydb.2010.12.006
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    ABSTRACTObjectiveTo investigate the protective effect of peroxisome proliferatorsactivated receptor gamma (PPARγ) agonist rosiglitazone(RSG) against doxorubicininduced nephropathy in rats by regulating transforming growth factor beta1 (TGFβ1) expression. MethodsThirty rats were randomly divided into the normal group, model group and RSGtreated group, ten in each. Total serum protein, serum albumin, serum creatinine, urea nitrogen, blood glucose, cholesterol, triglyceride and urine protein within 24hour were detected. ResultsBy the end of the experiment, hyperlipemia, hypoproteinemia and hyperproteinuria were observed in the model group. There were significant differences in TP,ALB,TC,TG and 24 hour urine protein between the model group and RSGtreated group,and nephrotic pathological lesion was ameliorated in RSGtreated group with increased expression of PPARγ and decreased expression of TGFβ1. ConclusionRSG has antifibrosis and protective effect on kidney by upregulating the expression of PPARγ and downgrading that of TGFβ1.
  • 药物研究
    LIU Shuang;WANG Bo
    2010, 29(12): 1556-1559. https://doi.org/10.3870/yydb.2010.12.007
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    ABSTRACTObjectiveTo investigate effects of ursolic acid(UA) on Ang Ⅱinduced proliferation and collagen syntheses of cardiac fibroblasts(CFb). MethodsThe proliferation of CFb in the primary cell culture of neonatal rats was detected by MTT assay; the level of collagen protein was determined by measuring hydroxyproline, collagen synthesis rate was measured by [3H]proline incorporation; and cell proliferation was assessed by texas redX phalloidin immunocytochemistry. The expression of p47 phox of NADPH was assessed by using Western blot. ResultsAng Ⅱ significantly increased the level of CFb proliferation, collagen synthesis rate, p47 phox expression. After treatment of UA, these indexes were obviously downregulated. ConclusionUA can decrease Ang Ⅱinduced the cell proliferation and synthesis of collagen protein in cardiac fibroblasts, through inhibiting p47 phox signaling pathway.
  • 药物研究
    WANG Xu;LI Shangying;SUN Baodan;JIANG Chunmei;GUO Xingjie
    2010, 29(12): 1560-1562.
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    ABSTRACTObjectiveTo study the bioequivalence of levofloxacin hydrochloride capsules in healthy volunteers. Methods20 healthy male volunteers were administered orally with single dose of either the tested or referenced formulations by a randomized crossover way. The blood concentrations of levofloxacin hydrochloride were determined by RPHPLC, and the pharmacokinetics parameters and relative bioavailability were calculated. ResultsThe Cmax were(3.05±0.64) and(3.25±0.82) μg•mL1, tmax of the tested and referenced formulations were(1.00±0.30)and(1.10±0.50) h, t1/2 were(7.51±1.26) and (7.45±1.30) h, AUC0~t were(17.58±3.25) and (18.21±2.96) μg•h•mL1, AUC0∞ were(19.04±3.35)and(18.96±3.12) μg•h•mL1. AUC0~t at 90% degree of confidence of the tested were 90.9%~102.5% of the referenced; while, Cmax were 84.7%~105.4%. ConclusionThe relative bioavailability of the tested to referenced capsules is(98.5±16.3)%, which shows that the two levofloxacin hydrochloride capsules are bioequivalent.
  • 药物研究
    LIU Yu;REN Xiuhua
    2010, 29(12): 1563-1565. https://doi.org/10.3870/yydb.2010.12.009
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    ABSTRACTObjectiveTo establish a LC/MS/MS method for determination of pseudoephedrine hydrochloride in human plasma. MethodsThe analysis was carried out by using Thermo Hypurity C18 column(150 mm× 2.1 mm,5 μm).The mobile phase consisted of 5 mmol•L1 ammonium acetatemethanol (70:30) with a flow rate at 0.3 mL•min1.The column temperature was set at 40 ℃ and concentrations in plasma were determined at ion pairs(166.2/148.2 ) by MRM of LC/MS/MS. ResultsThe linear range of pseudoephedrine hydrochloride was 17.67~565.3 ng•mL1 (r=0.999 5), the recoveries were 101.96%,102.08%,98.85%,at low, middle and high concentrations, respectively, and RSD were below 10%. ConclusionThe method is simple and precise, which can be used for determination of pseudoephedrine hydrochloride in human plasma and its pharmacokinetics study.
  • 皮肤病性病用药专栏
  • 皮肤病性病用药专栏
    WANG Qiang;LANG Yiyong;ZHANG Xiaoli;DAI Hua;LIU Landi
    2010, 29(12): 1566-1568. https://doi.org/10.3870/yydb.2010.12.011
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    ABSTRACTObjectiveTo stuty on the antiinflammatory, antibacterial and annlgesic effect of shuanghuang burn ointment. MethodsThe acute antiinflammation of shuanghuang burn ointment was tested by xyleneinduced mouse ear swelling; the in vitro antimicrobial effect was studied by agar diffusion method through paper; the analgesic action was detected through the hotplate regarding to pain threshold. ResultsThe significant difference was showed between all doses of shuanghuang burn ointment and control for xyleneinduced ear swelling (P<0.05, P<0.01). The shuanghuang burn ointment had no significant difference compared with jingwanhong. Shuanghuang burn ointment showed obvious antimicrobial effect on staphylococcus aureus and escherichia coli.The diameter of inhibited halo for staphylococcus aureus, escherichia coli were more than 10 mm.shuanghuang burn ointment significantly increased the pain threshold of mice and prolonged their pain latency(P<0.01). ConclusionShuanghuang burn ointment has a good antiinflammatory, antibacterial and analgesic effect.
  • 皮肤病性病用药专栏
    LIAN Xin;QIAN Yue;WU Yan;CHEN Shanjuan;LIN Nengxing
    2010, 29(12): 1569-1571. https://doi.org/10.3870/yydb.2010.12.012
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    ABSTRACTObjectiveTo investigate the clinical efficacy and safety of acitretin in treatment of psoriasis vulgaris and its effect of plasma endothelin (ET). MethodsForty eight patients with psoriasis vulgaris were treated with 2030 mg acitretin per day with meal. Dosage decreased to 1020 mg when no more lesions appeared and old lesions almost disappeared. Patients were totally treated for 12 weeks. Efficacy was evaluated by the change of psoriasis area and severity index (PASI).Radioimmunoassay was used to determine the plasma levels of ET. ResultsTotal effective rates after eight weeks and twelve weeks’ treatment were 91.7% and 95.8%, respectively, and no severe side effect was found. Plasma endothelin level was(62.91±16.32) pg•mL1 before the treatment and decreased to(56.94±17.62) pg•mL1 after treatment (P<0.05), the difference was significant. ConclusionAcitretin is effective and safe for treatment of psoriasis vulgaris, and plasma ET decreases significantly after treatment, which may contribute to the therapeutic mechanism of acitretin.
  • 药物与临床
  • 药物与临床
    WU Kun;CHEN Shanshan;WEN Mingling;XIE Shouzhen
    2010, 29(12): 1577-1579. https://doi.org/10.3870/yydb.2010.12.016
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    ABSTRACTObjectiveTo compare the efficacy and safety of paclitaxel liposome and paclitaxel in neoadjunvant chemotherapy for locally advanced cervical cancer. Methods55 comparability patients with locally advanced cervical were divided into treatment group (n=35)and control group(n=20).The patients in the treatment group were treated with paclitaxel liposome combined with carboplatin 135 mg•(m2)1 of paclitaxel liposome at the first day given intravenously lasting for at least 3 hours,300 mg•(m2)1 of carboplatin at the second day given intravenously 3 weeks as a cycle.Those patients in the control were treated with paclitaxel combined with carboplatin (same usage as in the tested group). At the end of the treatment cycle, the therapeutic effects and toxicity in both group were evaluated. ResultsThe total effective rate in the treated and control groups were 85.7% and 55.0%, respectively. The difference was statistically significant (P<0.05). Pathologic examination showed that one case and five cases of lymph node metastasis in the treated and control group, respectively, with remarkablely significance (P<0.05). Referring to hematologic toxicity, no significant difference between the two groups was found. While the incidence of nonhematologic toxicity like skin rash and peripheral neuritis was higher in the control group than that in the treatment group, the difference was statistically significant (P<0.01 or P<0.05). Conclusion It is concluded that paclitaxel liposome is more effective and has less adverse reactions such as rash and peripheral nerve toxicity than paclitaxel. The paclitaxel liposome is a new adjunvant chemotherapy for locally advanced cervical cancer, providing patients more chance of surgical opation and improve prognosis.
  • 药物与临床
    WU Yuan;DENG Qian;ZHANG Yi;ZHANG Xianwei
    2010, 29(12): 1580-1584. https://doi.org/10.3870/yydb.2010.12.017
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    ABSTRACTObjectiveTo observe whether combination of parecoxib sodium with tramadol improves the effect of patientcontrolled intravenous analgesia with sufentanil after thoracotomy. MethodsSixty patients(ASAⅠⅡ) were randomly divided into there groups: control group(group S, n=20); parecoxib sodium group(group P, n=20), in which parecoxib sodium 40 mg was intravenously administered 0.5 h before operation; combination of parecoxib sodium and tramadol group (group C, n=20), in which parecoxib sodium was intravenously injected 0.5 h before operation and tramadol 2 mg•kg1 was administrated 0.5 h before the end of operation. The visual analogue scale (VAS) for asssessing resting and motion pain, the actual/effective number of PCA, the level of restlessness and residence time in PACU at 0.5,8,12,24,48 h postoperatively were evaluated and recorded, the side effects and overall satisfaction to analgesic therapy were questioned at 48 h. ResultsThe resting and motion VAS of pain were significantly lower in group C and group P compared to those in group S at each time points postoperatively(P<0.05), the resting VAS of pain in group C and group P were separately recorded as 1.80±0.52 and 2.50±0.95 (P<0.05), and the motion VAS of pain were 2.85±0.76 and 3.30±1.38 (P<0.05); The effective number of PCA was significantly fewer in group C and group P than that in group S; The rates of restlessness were 10.0%, 50.0% and 90.0% in group C, group P and group S(P<0.05). No significant differences among three groups of the residence time at PACU and side effects were found(P>0.05). The overall satisfaction to analgesic therapy of group C and group P were similar(P>0.05), and better than group S(P<0.05). ConclusionIntravenous parecoxib sodium combining with tramadol can improve the effect of patientcontrolled intravenous analgesia with sufentanil after thoracotomy.
  • 药物与临床
    MA Weitao;YUWei
    2010, 29(12): 1585-1587. https://doi.org/10.3870/yydb.2010.12.018
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    ABSTRACTObjectiveTo study the efficiency and safety of parecoxib combined with patient controlled intravenous analgesia (PCA) for laparoscopic colorectomy. Methods90 patients under laparoscopic colorectomy were randomly divided into 3 groups,group A(i.v. 40 mg parecoxib 30 min before the end of operation and 10 mL N.S. instead 12 h and 24 h after operation), B(only with 40 mg parecoxib) andC (only with N.S.). All patients received 3 injections with different recipes, but PCA. The effective pump bolus times and total fentanil consumed dosage, VAS score(12,24,36,48 h postoperation), time of first flatus and first defecation, Ramsay score and PONV( at 0~12 h,~24 h,~48 h) were recorded. ResultsThere were no statistical difference in VAS score among three groups(P>0.05).Times of effective pump bolus and fentanil consumed dosage in group B were lower and time of first flatus and first defecation was earlier compared with those in group A and C(P<0.05). ConclusionMultiple injection of parecoxib has a good postoperative analgesic effect, reduces the fentanil consumption and accelerates the gastrointestinal recovery.
  • 药物制剂
  • 药物制剂
    ZHANG Geng;XIAO Weihong;CHENG Lu;ZHANG Changgong
    2010, 29(12): 1620-1621. https://doi.org/10.3870/yydb.2010.12.030
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    ABSTRACTObjectiveTo find out the optimum condition for mixing volatile oil from mint and honeysuckle flower with βcyclodextrin for yanshuyin effervescent tablets. MethodsThe inclusion was prepared by mixing saturated solution. The clathration procedure was optimized by L9(34)orthogonal test. The utilization rate of volatile oil and the bitumen content of inclusion were used as the assessment index. ResultsThe optimum process was applying the ratio of volatile oil and βCD as 1:6, carried out at 40 ℃ and lasted for 30 min. ConclusionThis method can be used for preparing the inclusion of volatile oil from mint and honeysuckle flower with βcyclodextrin for yanshuyin effervescent tablets.
  • 药物制剂
    ZHANG Changchun;CHEN Ping;QIN Weihui;ZOU Zexian;CHEN Xin
    2010, 29(12): 1622-1624. https://doi.org/10.3870/yydb.2010.12.031
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    ABSTRACTObjectiveTo optimize the extraction process for chikusetsusaponinⅠb in Panax japonicus. MethodsBased on the content of chikusetsusaponinⅠb, effects of alcohol concentration, solvent consumption, reflux time and refluxing frequency on the extraction of chikusetsusaponinⅠb was investigated by using orthogonal design. ResultsThe optimum conditions for the extraction of chikusetsusaponinⅠb was using 10 times amount of 75% ethanol, refluxing for 3 times, and 2 hours once. ConclusionThe optimized extraction process for chikusetsusaponinⅠb present the reference for new drug research and commercial process.
  • 药品质量控制
  • 药品质量控制
    GAO Xiaofei;WEN Xiaojing
    2010, 29(12): 1630-1633. https://doi.org/10.3870/yydb.2010.12.036
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    ABSTRACTObjectiveTo determine the concentration of protein in lipid samples by the ethanol precipitationBCA method. MethodsThreephase diagram for bovine serum albumin (BSA)waterethanol mixture and the effect of ethanol/lipid (V/V) on turbidity of lipid were investigated to determine the voluminal ratio of ethanol to sample, when ethanol was used to precipitate protein. Cold ethanol centrifugation was adoped to precipitate protein and the 2,2’biquinoline4,4dicarboxylic acid disodium salt (BCA) method was used to determine concentration of protein. ResultsUsing ethanol to precipitate protein before protein determination by BCA eliminated lipid effect. The good linear relation was showed as BSA being ranged within 1001 000 μg•mL1 (r=0.998 9), the relative standard deviation (RSD,%) and recoveries were all consistent with requirement of analysis. ConclusionThe protein concentration in lipid samples can be easily and accurately determined by ethanol precipitationBCA method, which avoiding interference of lipids.
  • 药品质量控制
    ZHAO Weijuan;WANG Zhanqing;XU Qian
    2010, 29(12): 1634-1636. https://doi.org/10.3870/yydb.2010.12.037
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    ABSTRACTObjectiveTo establish a HPLC method to determine dexamethasone acetonide in compound lianqiaopikang ointment. MethodsContents were determined by using a ZORBAX SBC18 column (4.6 mm×250 mm,5 μm) as the fixed phase, a mixture of acetonitrile and purified water (52:48) as a mobile phase, and detecting at 240 nm wavelength. ResultsThe linear range of dexamethasone acetonide was 50-800 ng. The average recovery was 101.32% and RSD was 2.01%. ConclusionThis method of determination of dexamethasone acetonide in compound lianqiaopikang ointment is rapid, simple and accurate, which fitting for quality control.
  • 药品质量控制
    LIU Minhua
    2010, 29(12): 1636-1638. https://doi.org/10.3870/yydb.2010.12.038
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    ABSTRACTObjectiveTo develop a HPLC method to determine the content of 2,3,5,4′tetrahydroxystilbene2OβDglucoside in shengxuetiaoyuan decoction by HPLC. MethodsThe HPLC method was carried out on an HypersilODS C18 (4.6 mm×250 mm,5 μm) column using a mobile phase of methanolwater (30:70) and detection wavelength as 320 nm. Flow rate was 1 mL•min1.Column temperature was set at 35 ℃.Sample size was 20 μL. ResultsWith a relation efficient of 1.000 0, a good linear relationship between area and amount was noted for 0.026~0.826 μg.The average recovery of 2,3,5,4′tetrahydroxystilbene2OβDglucoside and RSD were 99.91% and 0.96%, respectively. Conclusion It was proved that the method is available, simple and accurate, which is suitable for the quality control of shengxuetiaoyuan decoction.
  • 用药指南
  • 用药指南
    CHENG Ying;JIN Lu;WANG Xiaotong;KANG Hanlin;YUAN Hai;TAN Yanjuan
    2010, 29(12): 1648-1651. https://doi.org/10.3870/yydb.2010.12.044
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    ABSTRACTObjectiveTo evaluate the safety of memantine in treating patients with Alzheiemr’s disease. MethodsDatabases(Pubmed,Medline,Cochrane Library,CNNI,CBMdisc and Wanfang)were retrieved using keywords like Alzheimer,Meta analysis,clinical trials and so on. The 6 references consistent with inclusion criteria were analyzed by reviewing manager 4.2. The odds ratio and 95%confidence interval were calculated. ResultsConfusion,headache,dizziness,fall and agitation were the most common adverse reactions(ADRs). The Metaanalysis in RCTs showed that between t groups treated with memantine or placebo, no significant difference in the rate of ADRs(OR=0.94,9 5%CI 0.78-1.14,P=0.53),headache(OR=1.37,9 5%CI 0.51-3.67,P=0.54),dizziness(OR=1.04,9 5%CI 0.72-1.5,P=0.84),fall(OR=1.01,9 5%CI 0.7-1.46,P=0.97) occurred. There was significant difference in the occurrence rate of confusion(OR=1.70,9 5%CI 0.54-0.96,P=0.03),which implied the incidence of mementine was higher than that of placebo group.The agitation was significant lower in mementine (OR=0.70,9 5%CI 0.52-0.93,P=0.01),than that in placebo group. ConclusionMetaanalysis show that memantine is a safe agent for treating Alzheiemr’s disease.