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    药物研究
  • 药物研究
    DING Yuanyuan;QIU Lin;WANG Siwang;ZHAO Gangtao;YANG Fan;XU Jingfeng
    2009, 28(8): 970-974.
    TObjective To investigate the therapeutic effect of cinnamaldehyde(CA)on mice viral myocarditis caused by coxsackievirus B3(CVB3).MethodsOne hundred and seventy male Balb/c mice were randomly divided into 6 groups.The mice in the control group(n=20)was i.p injected with normal saline,those in other five groups(n=30 in each)were inoculated with Coxsackievirus B3m virus and bred in insulation lab.After viral inoculated for 72 h,Groups CA were i.g injected with CA at dose of 22.5,28.1,37.5 mg•kg1 ,respectively.Model group was treated with normal saline; Group RA was i.p.treated with 50 mg•kg-1 Radix astragali injective solution(RA) as a positive control.All groups were treated for 10 d.The heart histopathologic changes,content of CK,CKMB,LDH and NO in serum,and iNOS,NFκB in myocardium were detected.ResultsThe histopathologic score, death rate, median survival time,and the content of CK,CKMB,LDH in serum were lower in 22.5,28.1,37.5 mg•kg1 CA groups than those in the model group at 7 d after viral inoculation(P<0.05).The content of NO in serum,expression of NFκB and iNOS in myocardium were lower in 22.5,28.1,37.5 mg•kg1 CA groups than those in model group at 14 d after viral inoculation(P<0.05).The histopathologic changes (necrosis, degeneration and cellular infiltration) were lighter in CA groups than those in model group at 21 d after viral inoculation.ConclusionCA has a significant therapeutic effect on experimental VMC, the mechanism of which may be associated with inhibition of NFκB and iNOS expressions.
  • 药物研究
    YAN Shihai;WANG Xibiao;HUANG Chenghui
    2009, 28(8): 974-977.
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    ObjectiveTo observe the effects of buqilishihuoxue fomula (the formula has the effects of invigorating vital energy ,eliminating clamp and promoting blood flow )on the rats with chronic renal failure (CRF).MethodsCRF models were established by cutting 5/6 kidney of rats.Two weeks later, CRF rats were randomly divided into 3 groups: the model group, high dose and low dose of buqilishihuoxue fomula groups, and the sham operated group was operated .Rats were all treated orally with 10 mL•kg1•d-1 of solution, pure water in sham and model groups. 15,30 g•kg-1 herbs in low dose and high dose groups .Levels of urine protein, serum creatinine (Cr), blood urea nitrogen (BUN) were determined and the renal pathology were analyzed.Results It was shown that all the biochemistry markers in the model rats were significantly increased, but decreased in high dose of buqilishihuoxue fomula group.Compared with the model group, levels of SCr and BUN in the low dose of buqilishihuoxue fomula group were decreased obviously.The renal damages were attenuated in both buqilishihuoxue fomula groups.ConclusionBuqilishihuoxue fomula could step down the pathological proceeding of chronic renal failure.
  • 药物研究
    YIN Tao;WANG Weixing;CHEN Chen;ZHANG Changwei;YU Jia
    2009, 28(8): 977-980.
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    ObjectiveTo study effects of rosiglitazone on the expression of NF-κB and TNF-α in rats with acute pancreatitis.MethodsAcute pancreatitis model was induced by retrograde infusion of 5% sodium taurocholate into the biliopancreatic duct.Rosiglitazone (6 mg•kg1) was injected by femoral vein 30 minutes prior to the operation.Serum amylase (AMY), tissue myeloperoxidase (MPO) level and pancreatic pathologic score were detected.The expression of nuclear fator-kappa B (NF-κB) in pancreatic tissue was assayed by immunohistochemistry and TNFα mRNA was analyzed by reverse transcription polymerase chain reaction (PCR).ResultsCompared with the model group, the levels of amylase, MPO, and pathologic score in the rosiglitazone treated group were reduced (P<0.01), both the expression of NFκB and TNFα were decreased (P<0.01).ConclusionRosiglitazone exerts protective effects on acute pancreatitis, which could be associated with downregulation of NF-κB and TNF-α expression.
  • 药物研究
    WANG Jianzhi;ZHOU Fubo;YANG Jing;MI Yanjun
    2009, 28(8): 980-982.
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    ObjectiveTo investigate the antisportsfatigue effect of Chinese medicine curcuma longa and its mechanism.MethodsContinuously pole climbing and antianoxia experiments were carried out on mice which were given with curcuma longa intragastrically at different doses for 30 days.The skeletal muscle contraction of rats and content of superoxide dismutase(SOD), malonaldehyde(MDA) and Ca2+Mg2+ATPase activity were detected.ResultsIt was showed that curcuma longa obviously prolonged the time of climbing, raised antianoxia capability of mice, enforced the contraction of skeletal muscle and increased activities of Ca2+Mg2+ATPase and SOD, lowered the content of MDA.ConclusionCurcuma longa may have significant effect on the capability of adaptation to heavy exercise and prevention or elimination fatigue after exercise.
  • 药物研究
    YAO Jun;QIAN Cuijuan
    2009, 28(8): 983-986.
    ObjectiveTo investigate the effect of paeonol on NFκB signaling pathway and its molecular mechanism of inducing tumor cell apoptosis.MethodsAfter incubated with Tca8113 cells at different concentrations and different time, the inhibitory effect of paeonol on cell proliferation was detected by MTT assay, apoptosis of Tca8113 cells were tested by using Hoechst 33342 staining and flow cytometry, and expressions of apoptosisrelated proteins(Bax, Bcl2) and components of NFκB pathway(IκBα, pIκBα) were examined by Western blot, and activation of nuclear factor kappa B (NFκB) was determined by electrophoretic mobility shift assay.Results It was showed that paeonol inhibited the growth of Tca8113 cells in a time and concentration dependent manner.Morever, paeonol induced apoptosis of Tca8113 cells, upregulated Bax and IκBα, downregulated Bcl2, and decreased IκBα phosphorylation and NFκB activation by Western Blot and EMSA.ConclusionPaeonol inhibits NFκB signal pathway, and thus suppressing cell proliferation and inducing apoptosis of Tca8113 cell line.
  • 药物研究
    JIANG Guohui;LI Guangqin;LI Yu
    2009, 28(8): 986-990.
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    ObjectiveTo study the influence of doxycycline on urokinase thrombolysis therapy at different time(6,9,12 h)of cerebral arterial thrombosis,and evaluate its neuroprotective effects and intervention of thrombolysis time window.Methods168 healthy male SD rats were randomly divided into 7 groups: cerebral ischemia rats as model, urokinase thrombolysis at different time (6 hUK,9 hUK,and 12 hUK groups), and doxycycline on urokinase thrombolysis (6 hUK+Doxy,9 hUK+Doxy,and 12 hUK+Doxy groups).Rats were all sacrified after 24 h.The expression of MMP9 was detected with immunohistochemical staining.TTC staining were applied to detect the infarction volume.The permeability of the observed brainblood barrier was detected with Evan’ s blue and cerebral hemorrhage was quantified with spectrophotometer assay.Doxycycline was injected through tail vein 2 h postischemia at 30 mg•kg1.ResultsThe infarction volumes were decreased with urokinase treatment at the 6th hour.The expression of MMP9, permeability of the brainblood barrier and cerebral hemorrhage content were further raised with urokinase thrombolysis at more than 6 hours after ischemic stroke, however, those were decreased and improved by doxycycline.ConclusionDoxycycline could increase the effect of urokinase and decrease its complications in rats at different time.It has neuroprotective effects and may extend urokinase thrombolysis therapy time window.
  • 药物研究
    CHEN Fangfang;SHEN Nan;LEI Juntao;DING Xiaoliang;LI Yongliang;LIU Bin;HAO Chengjie;WANG Yuan;ZHANG Xiurong
    2009, 28(8): 990-993.
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    ObjectiveTo explore effects of different solvent extractions of yikouzhong(fruit of eycalptus globlus) on rat adjuvant arthritis.Methods Different extracts were obtained from yikouzhong with different organic solvents.70 Female Wistar rats were randomly divided into normal group (saline), model group, petroleum ether group, chloroform group, acetoacetate group, 95% ethanol group and 50% ehanol .Adjuvant arthritis (AA) in rats was established by intradermal injection with Freund’s complete adjuvant (0.1 mL / one) in Wistar rats, while 0.9% sodium chloride as normal control.The rats in normal and model controls were treated with normal saline, others with different extracts, all at 0.5 mL•(200 g)1,for consecutive 16 d.Swelling in foot pads, spleen index, thymus index as well as levels of nitric oxide (NO) in sera were determined.ResultsCompared with model group, all extracts significantly inhibited foot pad swelling, but petroleum group.Meanwhile, the thymus index, spleen index and serum concentrations of NO were markedly reduced by different solvent extracts.ConclusionExtracts from yikouzhong has obvious therapeutic effect on rat adjuvant arthritis, the active components of which is supposed to be liposoluble.
  • 药物研究
    MA Xiaoya;WANG Meina;WANG Yuhu;LIANG Weiwei
    2009, 28(8): 993-995.
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    ObjectiveTo study the effects of shuluo on focal cerebral ischemia in rats and blood pressure in spontaneously hypertensive rats (SHR). MethodsThe focal cerebral ischemia model was produced by permanent occluding the right middle cerebral artery (MCAO).The infarct area, contents of malondihyde (MDA) in cerebrum and brain histopathology were examined.Systolic blood pressure (SBP) was measured in conscious SHR by tailcuff method. ResultsShuluo (1.00 and 0.50 g•kg1 , ig) significantly decreased the infarct area and contents of MDA after MCAO for 24 h in rats. Shuluo markedly ameliorated the ischemia injury of brain tissue and decreased SBP in SHR.ConclusionShuluo not only has protective effects on focal cerebral ischemia in rats , but also decreases the blood pressure in SHR.
  • 药物研究
    GONG Weimin;ZH0U Zewei;SHEN Xiu;SHEN Hongsheng;WANG Jie
    2009, 28(8): 996-999.
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    ObjectiveTo study the antitumor effect of TH in vitro and in vivo and identify a new highefficient and lowtoxic compound recipe.MethodsInhibition rate of growth and halfinhibitory concentrations (IC50) were assessed in human lung cancer cell A549, human esophageal carcinoma cell EC9706,human colon cancer cell LoVo, human hepatocellular carcinoma cell HepG2 and human breast cancer cells MCF7 by MTT method.The mice transplanted with hepatoma H22 were randomly divided into 5 groups: negative control, positive control (CDDP0.005 g•kg1), three doses of TH(0.030,0.060,0.090 g•kg1), which were treated intragavagely with 0.3 mL of solution since the next day, for consecutive 8 d.Other groups were treated with 0.2 mL every other day for total three times.Mice were sacrificed 24 h after the last drug administration the indexes of thymus, spleen and inhibitory rates were measured.ResultsIC50 of TH in A549,EC9706,LoVo,HepG2 and MCF7 were 7.15,5.41,2.49,2.18 and 1.37 μg•mL1,respectively.Tumor inhibitory rates of low, middle and high dose group of TH in mice with H22 were 52.8%,44.9% and 47.9%,which were significantly higher than those of the control group (P<0.01).The indexes of spleen,thymus and liver in TH groups showed no remarkable changes compared with those in the control group, but were significantly different from those in the positive control(P<0.01).ConclusionTH has strong antitumor activities by markedly inhibiting cell growth in vitro and suppressing tumorigenesis in vivo.
  • 药物研究
    WANG Yan
    2009, 28(8): 999-1002.
    ObjectiveTo study effects of quercetin on osteoprotegerin(OPG) and receptor activator of NFκB ligand( RANKL) in femurs of ovariectomized rats.Methods48 female SD rats were randomly assigned into 6 groups: shamoperated group(SHAM), ovariectomized group(OVX), 17βestradiol replacement therapy group(ERT,0.1 mg• kg-1• d-1,sc), highdose quercetin treated group (QH,300 mg• kg-1• d-1,ig), middledose quercetin treated group (QM, 150 mg• kg-1• d-1, ig), lowdose quercetin treated group (QL, 75 mg• kg-1• d-1,ig).Except for SHAM group, rats in other groups were bilaterally ovariectomized.Administration started on the 8th day after operation and lasted 16 weeks.At the end of the 17th week,all rats were sacrificed.The bone vitodynamics properties (including ELASTIC, MSTRESS, MLORD and STIFFNESS) of femurs and lumbar vertebrae were measured.The expressions of OPG and RANKL in femurs were detected by immunohistochemical method.ResultsCompared with OVX group, quercetin (300 and 150 mg• kg-1• d-1) increased expression of OPG in femurs while decreased that of RANKL in ovariectmized rats, and partly improved the bone vitodynamics properties.ConclusionQuercetin increases expression of OPG in femur while decreases that of RANKL, therefore inhibiting bone absorption and preventing osteoporosis.
  • 药物研究
    MA Guoping;YANG Jingli;TIAN Yuke;LIU Juying
    2009, 28(8): 1003-1006.
    ObjectiveTo investigate the effect of fentanyl on the expression of TNFα in spinal cord and its protective effect on diabetic rats with peripheral neuropathy.MethodsNormal rats injected intrathecally with 0.9% sodium chloride 10 μL was as a normal control ( group A).STZinduced diabetic rats with an intrathecal catheter were allocated to two groups randomly: 16 diabetic rats received 10 μL 0.9% normal saline as group B, another 16 received fentanyl at 0.5 μg•(10 μL)-1 injected intrathecally via an intrathecal catheter once a day as group C.The treatment lasted for 4 weeks.Paw withdrawal mechanical threshold was measured by using the up/down method with von Frey monofilaments at 1th, 2th, 3th, 4th week since the treatment started.TNFα expression on cornu dorsale medullae spinalis was detected by immunohistochemistry and image analysis, and spinal pathomorphism was measured by Nissl’s staining.ResultsCompared with group A, the paw withdrawal mechanical thresholds in group B and C were markedly lowered (P<0.05), while expressions of TNFα in spinal cord were significantly increased (P<0.01).The paw withdrawal mechanical threshold in group C was raised (P<0.05) and expression of TNFα was significantly lower in comparison to group B (P<0.01).Nissl’s granules appeared to be broken and thawed in diabetic rats, however, which were improved by intrathecal injection of fentanyl.ConclusionThe cause of neuropathic pain by diabetes with peripheral neuropathy is associated with overexpression of TNFα in spinal cord.Intrathecal injection of fentanyl reduces the expression of TNFα, protects the spinal cord and relieves peripheral neuropathic pain in diabetic rats.
  • 药物研究
    ZHAO Weijuan;HUANG Tongrui;ZHANG Mei
    2009, 28(8): 1006-1008.
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    ObjectiveTo study the percutaneous permeability of two kinds of nanoargentum hydrogels with different content of cellulose and phosphate as filling stuff in vitro.MethodsIsolated rat skin was taken as permeable barrier, the skin permeability of nanoargentum in each hydrogels were observed by HSvitro apparatus.ResultsPermeability accelerant increased the argentum content in skin effectively and cellulose lasted the action of nanoargentum.Conclusion0.1% cellulose nanoargentum hydrogels have a good permeability and stable release property, which is benefit for local therapeutic application.
  • 药物研究
    WAN Yan;WU Li;LOU Huan;SU Ping
    2009, 28(8): 1008-1012.
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    ObjectiveTo study the effects of Ouabain and it’s receptors: Na+/K+ATPase α1 polyclonal antibody and α4 polyclonal antibody on human sperm movement.Methods60 normal semen samples were optimized by swimup technique.30 samples were coincubated with highdose(1×102~1×105 mol•L-1)and lowdose(1×106~1×107 mol•L-1) of Ouabain, respectively.The sperm movement was detected by CASA system at 1 h,2 h,3 h and 4 h.The other 30 samples were coincubated with Na+/K+ATPase α1 antibody and α4 antibody, respectively, the same parameters were detected in the same way 1 h later.Results①Compared with the control group, both the ratio of sperm activity and sperm motility were decreased significantly after coincubated with highdose(1×102~1×105 mol•L-1)of Ouabain for 4 hour(P<0.05); ②Compared with the control group, both the sperm motility and sperm activity ratio were decreased slightly after coincubated with lowdose(1×106~1×107 mol•L-1)of Ouabain for 4 h; And the changes among the two groups had no statistical significance yet; ③No statistical significance was found for the rest of movement parameters as linear velocity, whiplash frequency, rectilinearity, prorsad and wobble motility.④Compared with the control group, the sperm activity ratio decreased significantly after coincubated with antiα1 and antiα4(P<0.01);But the changes between the two groups have no statistical significance; ⑤Compared with the control group, the sperm motility decreased significantly after coincubated with antiα1 and antiα4(P<0.01);And the effect of antiα4 on sperm motility was dramatically obvious compared with antiα1(P<0.01); ⑥The rest of movement parameters had no statistical significance.ConclusionOuabain can degrade the motor function of human sperm in vitro; Both antiNa+/K+ATPase α1 polyclonal antibody and α4 polyclonal antibody can degrade the motor function of human sperm as well, antiα4 being better.
  • 心血管系统用药专栏
  • 心血管系统用药专栏
    XU Qiumei;CHENG Bei;LI Wei;GUAN Siming
    2009, 28(8): 1013-1016.
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    ObjectiveTo explore the characteristics and causes of using secondary prevention drugs for elderly patients with acute STelevation myocardial infarction (STEMI).Methods105 elderly patients (≥60 years) with STEMI in 2006 were retrospectively analyzed for using secondary prevention drugs by comparing with 77 nonelderly patients (<60 years) with STEMI.Results In elderly group the percentage of using βreceptor blocker (51.43%:72.73%) and aspirin (67.62%:89.61%)were both significantly lower and the incidence of poor heart function(≥ level 3, 34.29%:16.88%) and digestive system abnormalities (25.71%:12.99 %)were both significantly higher.Conclusionβreceptor blocker and aspirin are rarely used for the elderly STEMI patients, the reasons lie in the poor heart function and digestive system diseases which restrict the use of two drugs.
  • 心血管系统用药专栏
    LU Guangkui;YU Qijing;ZHOU Qingshan;CHEN Zhie;CAI Zhongxiang
    2009, 28(8): 1016-1020.
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    ObjectiveTo compare the cardioprotective effects of etominate and midazolam in children with cyanotic heart disease undergoing open heart surgery.MethodsThirtysix children with cyanotic heart disease in NYHA class III were randomly divided into two groups: etominate combined with low dose of fentanyl(Group EF, n=18) and midazolam combined with low dose of fentanyl(Group MF, n=18).The changes of heamodynamics,SpO2, nasopharyngeal and rectal temperature were continuously monitored; the time of tracheal extubation and staying in ICU were recorded.Blood samples were collected to detect the change of plasma angiotensin II(AngII) at the following time points: intravenous catheter (t0), 0 min after anesthesia induction (t2), 20 min after aorta crossclamp(t2), 20 min after releasing of aorta crossclamp(t3),2 hours after releasing of aorta crossclamp(t4) , and 24 hours after operation(t5).Myocardium samples were collected to measure the change of AngII and observe the expression of hemeoxygenase1(HO1) at t2 and t3 respectively.And the change of plasma cardiac troponin I(cTnI) was observed at the following time points:t0, t4, t5.ResultsThe time of tracheal extubation and staying in ICU in group EF were significantly shorter than those in group MF (P<0.05).The concentration of myocardium AngII at t3 was higher than that in both groups at t2,and which in group EF at t3 was higher than that in group MF at the same time point (P<0.05).In both groups, the level of plasma cTnI at t5 was significantly higher than that at t0 or t5 (P<0.01),and which at t5 was higher than that at t0(P<0.01).The expression of HO1 at t2 was significantly lower than that at t3 in both groups, respectively (P<0.01), and the expression of HO1 at t3 or t4 in group EF was significantly lower than that in group MF at the corresponding time point (P<0.05).ConclusionBoth etominate and midazolam have cardioprotective effects for children with cyanotic heart disease undergoing open heart surgery.Midazolam is superior to etominate in inhibiting the expression of AngII, while etominate is better than midazolam in stimulating the expression of HO1 and shortening postoperative recovery time.
  • 心血管系统用药专栏
    LU Yingjia;ZENG Qiutang
    2009, 28(8): 1021-1025.
    ObjectiveTo study the effect of MMP8,TIMP2 on protein expression of Ⅰ、Ⅲcollagen after myocardial infarction in rats and the intervention effects of captopril.MethodsRats survived from AMI induced by left anterior descending branch ligation were randomized to AMI control group(12 cases) and captopril treatment group(10 cases,i.g.10 mg•kg-1•d-1 24 h after operation).At the end of the forth week,the ventricular remodeling index, expression of myocardium MMP8,TIMP2 protein in left ventricular noninfarcted myocardium were examined by immunohistochemical analysis; type I and type Ⅲ collagen volume fraction (CVF) were analyzed by using polarized light with picrosirius red satining.ResultsCompared with shamoperated rats, the protein expression of MMP8,TIMP2 and MMP8/TIMP2 ratio in AMI control group were significantly increased (P<0.01), but increasing extent of TIMP2 was less than that of MMP8.TypeⅠand Ⅲcollagen in the noninfarcted myocardium were increased subsequently (allP<0.01), while left ventricular(LV) end diastolicpressure(LVEDP), relative weight(LVRW), right ventricular relative weight (RVRW) were significantly increased(all P<0.01); whereas±dp/dt were significantly reduced(P<0.01)at 4 weeks after AMI.In comparison with the AMI control group, the protein expression of MMP8 ,the CVF of typeⅠ、Ⅲcollagen and MMP8/ TIMP2 ratio were in captopril treatment group were significantly reduced (all P<0.01),while there were no significantly changes in the expression of TIMP2.And LVEDP, LVRW, RVRW were lower as well (all P<0.01).Whereas ±dp/d was significantly increased (P<0.01) .ConclusionCaptopril could not only inhibit the growth of typeⅠ、Ⅲcollagen in AMI and NIZ, but also reduce the MMP8 expression and downregulate the ratio of MMP8/TIMP after AMI.
  • 药物与临床
  • 药物与临床
    BAI Shonjun;ZHANG Yong;ZHANG Yamin;XU Gang;LIU Xiaocheng
    2009, 28(8): 1030-1033.
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    ObjectiveTo investigate the effect and safety of tranilast in earlystage diabetic nephropathy.MethodsTwenty patients with earlystage diabetic nephropathy were divided into two groups at random.The tranlist treated group were administered with tranlist 100 mg,tid for 12 months, and the control group received no tranlist.If the blood pressure consistently increased, added no more ACEI and ARB, used calcium channel blocker, β receptor blocker and /or diuretics instead, to control blood pressure <140/90 mmHg.The clinical data were collected and evaluated before and 3, 6,9,12 months after treatment.ResultsBoth urinary type IV collagen excretion and albumin decreased significantly (P<0.05) after tranlist therapy.No significant changes was found for serum creatinine.The side effects were mild, and could be tolerated.ConclusionTranilast is safe and effect for treating earlystage diabetic nephropathy.
  • 药物与临床
    CHEN Li;ZHOU Qingshan;LUO Zhihong;CHEN Jinhui
    2009, 28(8): 1033-1035.
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    ObjectiveTo assess the effects of preemptive analgesia with flurbiprofen on the postoperative pain in patients undergone uvulopalatopharyngoplasty surgery.Methods40 cases of patients scheduled for selective uvulopalatopharyngoplasty surgery were randomly divided into two groups, and they were under general anesthesia by tracheal intubation.Patients in group A received flurbiprofen 1 mg•kg-1 intravenously thirty minutes before operation .those in group B received flurbiprofen 1 mg•kg-1 after operation.The analgesia effects after operation were assessed by visual analogue scale (VAS)at 1,3,6, 24 hours after operation, and side effects were assessed as well.ResultsThe VAS of group A was significant lower than that of group B at 1 hour after operation (P<0.01), at 3 and 6 hours after operation (P<0.05), but no obvious difference was found between two groups at 24 hour.ConclusionPreemptive analgesia with flurbiprofen 1 mg•kg1 could provide satisfactory pain relief without obvious side effects.
  • 药物制剂
  • 药物制剂
    SHI Daohua;LIAO Qin;GUO Lijiao;LIN Qiaoling
    2009, 28(8): 1068-1069.
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    ObjectiveTo investigate and improve the extraction process of cardamonin from alpinia katsumadai. MethodsThe seeds of alpinia katsumadai were extracted with 95% ethanol, isolated and purified by combining with abstraction and column chromatography.The identification and purity of cardamonin were determined by spectroscopic methods. ResultsAn orange crystal like compound was obtained and identified as cardamonin.The output ratio and purity of cardamonin were 0.084% and 99.67%, respectively. ConclusionThe modified extraction method is easy to manipulate and effective to produce a highoutput and highpurity of cardamonin.