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    药物研究
  • 药物研究
    Extraction of Gallotannins from Galla Turcica and Their Immune Effects
    FAN Xiaohong;LI Zhijian;Silafu&#;AIBAI;LIU Fa;ZHOU Lu;MENG Fanlong
    2011, 30(6): 695-698. https://doi.org/10.3870/yydb.2011.06.001
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    ABSTRACTObjectiveTo optimize the extraction process of gallotannins from Galla Turcica and study their immunological function in vitro.MethodsTannins were extracted from the crude extracts of Galla Turcica with different solvents. Gallic acids were determined by high performance liquid chromatography with hydrolysates of tannins as an indicator. The effects of the gallotannins from Galla Turcica produced by different extraction technology on lymphocyte proliferation were investigated in vitro with MTT method，which on macrophage cells activity were determined by using neutral red assay.ResultsThe content of gallic acid obtained by methyl alcohol supersonic way reached the highest level （77.01±2.97）% comparing with other extracting solvents.Gallotannins from Galla Turcica significantly accelerated lymphocytes proliferation and enhanced macrophages phagocytosis of neutral red. Conclusion70% methyl alcohol supersonic method is the best extraction method for total tannins isolation from Galla Turcica. It demonstrates that gallotannins from Galla Turcica potentiates immune function.
  • 药物研究
    Effects of Berberine Hydrochloride and 8hydroxy Dihydroberberine on the Activity of Acetylcholinesterase （AChE） in the Cerebral Tissue and Serum of Rats
    WANG Kaifu;XU Lijun;ZOU Xin;LU FuerWANG Kaifu;XU Lijun;ZOU Xin;LU Fuer
    2011, 30(6): 699-701. https://doi.org/10.3870/yydb.2011.06.002
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    ABSTRACTObjectiveTo investigate the inhibitory effects of monomer berberine hydrochloride and its structuremodified compound 8hydroxy dihydroberberine on the activity of acetylcholinesterase （AChE） in the cerebral tissue and serum of rats. MethodsThe rats were sacrificed by cervical dislocation after the blood was collected from abdominal aorta. The cerebral tissue was homogenized and the total protein level in it was measured using biuret. The AChE activity in cerebral tissue and serum was detected by enzymatic method. ResultsThe inhibitory rate of AChE activity in cerebral tissue by berberine hydrochloride was 52.57%－82.22% whereas 32.78%－96.14% by 8hydroxy dihydroberberine. The inhibitory rate of serum AChE activity by berberine hydrochloride was 8.44%－99.59% and 11.72%－99.59% by 8hydroxy dihydroberberine. The inhibitory extent was in a doseeffect relationship with berberine .ConclusionBoth berberine hydrochloride and 8hydroxy dihydroberberine could inhibit AChE activity in cerebral tissue and serum obviously，which may be a new target for the treatment of diabetes.
  • 药物研究
    Study on the Bioequivalence of Two Different Dose of Lansoprazole
    ZHANG Yue;ZHANG Aili;LI Muqiong;WANG Baolong;QIN Xiangyang;LI Xiaoye;SUN Xiaoli;WEN Aidong
    2011, 30(6): 702-705. https://doi.org/10.3870/yydb.2011.06.003
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    ABSTRACTObjectiveTo establish a simple and fast method for determing concentration of lansoprazole in human blood，and to estimate bioequivalence of two lansoprazole. MethodsChromatography was carried out on an Agilent C18 （250 mm×5 mm，5 μm）,with acetonitrilewater （contained 1‰ triethylamine） （pH=7.0） （30：70） as mobile phase，at a flow rate of 1.0 mL• min1，at 285 nm of wavelength with the sample loaded at 20 μL.ResultsTwenty volunteers were randomly divided into 2 groups. A single oral dose of 10 mg of test or reference tablets was delivered to each volunteer in an open crossover test. The plasma concentration of bisoprolol hemifumarate was determined by HPLCUV detection. Based on the parameters of pharmacokintic and relative bioavailability，the bioequivalance of bisoprolol hemifumarate was evaluated. The main pharmacokinetic parameters of the test prepartion were as follows: t1/2 were （2.19±0.49） and （2.38±0.48） h，tmax were （2.52±0.80） and （2.82±0.69） h，Cmax were （854.82±249.70） and （813.22±289.59） ng•mL1，AUC（012 h）were （3 513.00±742.25） and （3 779.90±1 191.52） μg•h•mL1，AUC（0∞） were （3 742.64±749.85） and （4 078.54±1 171.17） μg•h•mL1, respectively. ConclusionThe preparations of test and reference are bioequivalent.
  • 药物研究
    Effect of Probucol on TNFα and Atherosclerosis Induced by Hyperhomocysteinemia in Rabbits
    WU Le;LI Honghua;WU Qiang;WANG Xiaokun
    2011, 30(6): 705-708. https://doi.org/10.3870/yydb.2011.06.004
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    ABSTRACTObjectiveTo study the effects of probucol on tumor necrosis factoralpha （TNFα） and atherosclerosis induced by hyperhomocysteinemia in rabbits. MethodsTwentyfour male rabbits were randomly divided into three groups. The control group was fed with common food；the homocysterinemia （Hcy） model group was fed with highmethionine food which composed of 1% methionine；the treatment group was given with highmethionine food and i.g. treated with probucol 1 g•d1. Blood samples were collected from the ear vein by the end of 20 weeks and we measured the levels of TNFα and total Hcy （tHcy）. The mRNA expression in abdominal aorta was measured by RTPCR. The sections were made for light microscopy to observe the vascular pathomorphological changes. ResultsThe serum levels of TNFα were （4.01±1.13） and （7.65±1.73） pg•mL1 in the treatment group and the model group respectively（P＜0.05）. The mRNA expression of TNFα in the treatment group was lower than that in the model group（P＜0.05）,but the plasma levels of Hcy in two groups were not different. Aortic lesion in the treatment group was attenuated compared with that in the model control. ConclusionProbucol could decrease serum TNFα level but not plasma Hcy. Probucol has an antiatherosclerosis effect，which is associated with suppressing TNFα mRNA expression and mitigating endometrial hyperplasia.
  • 药物研究
    Preparation of Monoclonal Antibody Against Neisseria Meningococcal Serogroup A Polysaccharide （GAMP） by Using the Conjugate Vaccine of both GAMP and Tetanus Toxoid
    LI Peishan;ZHANG Chunyan;LI Shijun;CHEN yan;XIANG Meijuan;LI Fanghe;ZHANG Hong
    2011, 30(6): 709-712. https://doi.org/10.3870/yydb.2011.06.005
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    ABSTRACTObjectiveTo prepare monoclonal antibodies against Neisseria meningococcal serogroup A polysaccharide （GAMP）. MethodsBALB/c mouse was immunized by GAMPTetanus Toxoid（TT）. Hybridoma cell lines secreting monoclonal antibodies against GAMP were screened after the fusion of mouse splenic cells with SP2/0 cells.The number of chromosome in hybridoma cell was tested by colchicinesinterception，and the ascite of mice was prepared by pristaneinducing method. The mAb was purified by octansic acidammonium sulfate precipitation，and purity of the extracted protein was measured by gray scalescanning assay of SDSPAGE. The specificity of antiGAMP mAb was identified by neutration of antigen and antigensubstitute method. ResultsThe hybridoma （2E7） had a healthy growth state，and the chromosome of which was 139.73. It produced proper amount of mAb，which was identified to be IgG1. The concentration of extracts was 1.76－2.32 mg•mL1,and the purity was 97.2%. The potency of HRPmarked antiGAMP mAb was 1：25 600，and the antiGAMP E7 mAb showed a specificity for GAMP by antigen substitution and neutralization assay. ConclusionThe antiGAMP E7 mAb has been successfully obtained，and it makes a necessary foundation for the quality control and manufacture monitoring during preparation of the GAMPTT vaccine.
  • 药物研究
    Effect of Ginger（Zingiber officinale Rosc.） Oleoresin on Experimental Gastric Ulcer in Rats
    JIANG Suzhen;XIE Fangfei
    2011, 30(6): 713-715. https://doi.org/10.3870/yydb.2011.06.006
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    ABSTRACTObjectiveTo study the effect of ginger（Zingiber officinale Rosc.） oleoresin on experimental gastric ulcer in rats. MethodsThe water immersion restraintstressed ulcer，ethanolinduced ulcer and pylorusligated rat gastric ulcer models were established，and the antigastric ulcer activity of ginger oleoresin，indicated as gastric juice and acid secretion and peptic activity was evaluated at dose of 50，100，200 mg•kg1. ResultsGinger oleoresin at 50，100，200 mg•kg1 significantly inhibited gastric ulcer formation induced by ethanol and water immersion restraintstress in rats. In pylorusligated rats，pretreatment with ginger oleoresin had no effect on ulcer index（UI） of gastric mucosa，gastric juice volume，acidity and peptic activity.ConclusionThe findings indicate that ginger oleoresin possesses gastroprotective potential which is unrelated to inhibition of gastric acid secretion and activity of pepsin.
  • 药物研究
    Effect of Pirfenidone on Tubulointerstitial Fibrosis in Rats with Unilateral Ureteral Obstruction
    LI Dixin;ZENG Hongbing;JI Chunyang;LIANG Pingping;WEI Honglan
    2011, 30(6): 716-720. https://doi.org/10.3870/yydb.2011.03.007
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    ABSTRACTObjectiveTo explore the effect of pirfenidone（PFD） on tubulointerstitial fibrosis（TIF） in rats with unilateral ureteral obstruction（UUO）and its possible mechanism. MethodsThirtyfive female SD rats were randomly divided into three groups:（Ⅰ）shamoperated group (n=7),（Ⅱ）UUO model group (n=14),（Ⅲ） PFD group (n=14)：rats underwent UUO and were treated with PFD 250 mg•kg1•d1for 14 days. Rats in group I were all sacrificed at day 14 after operation，those in group Ⅱ and Ⅲ were sacrificed at day 7 and 14,respectively. Renal tissues were examined by PAS and MASSON stain；TUNEL and immunohistochemistry were applied to determine the apoptosis and caspase3 protein expression of renal tubular epithelial cells（RTC）；the content of MDA and activity of SOD in renal cortex were assessed by chemical colorimetry. ResultsNo pathology changes were found in group I;while compared with group I，the TIF,TUNELpositive and caspase3positive cells all remarkably increased in group Ⅱ，especially at day 14，all of which were ameliorated in group Ⅲ（P＜0.05）. Compared with group I，the content of MDA was raised in group Ⅱ，especially at day 7，whereas activity of SOD declined，especiall at day 14；compared with group Ⅱ，MDA in group Ⅲ was decreased obviously at day 7，activity of SOD increased significantly，especiall at day 14. ConclusionPFD remarkably ameliorates tubulointerstitial fibrosis in UUO rats and improve TIF，which may be associated with reduction of oxidative stress and caspase3 related apoptosis.
    • 消化内科药物专栏
  • 消化内科药物专栏
    DFT Studies on the Matrine Type Alkaloids and Their AntiHBV Activity
    WANG Chunlu;LONG Wei;LIU Peixun
    2011, 30(6): 724-728.
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    ABSTRACTObjectiveTo make a theoretical calculation on the structure of 10 kinds of matrine type alkaloid compounds by using the quantum chemistry density functional methods （DFT），and to analyze their antiHBV activity. MethodsThe geometric and electronic structures of matrine typed alkaloids were optimized by DFT （B3LYP） method first，then the relationship of the matrines’ molecular structures and their antiHBV activity was analyzed based on the theoretical calculation，and the structureactivity relationship model was established by heuristic method（HM）. ResultsA preferable QSAR equation was obtained: IR=－0.155－0.023 MSA+0.078 Sxy （R=0.82，q=0.72）.ConclusionDipole，molecular surface area，stability of acid amide bond and Q C13 are important factors affecting the antiHBV activity of matrine type alkaloid compounds.
    • 药物与临床
  • 药物与临床
    Comparative Study of Rosuvastatin in Single Use and in Combination with Aspirin for the Treatment of Carotid Atherosclerosis
    HUA Xianping;YANG Yong;CHEN Pingying
    2011, 30(6): 743-746. https://doi.org/10.3870/yydb.2011.06.016
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    ABSTRACTObjectiveTo investigate the effects of single use of rosuvastatin （RS） or plus with aspirin （ASA） on serum inflammatory factors and carotid intimamedia thickness （IMT） in patients with carotid atherosclerosis （CAS）. MethodsSixty healthy people with the normal carotid artery were randomly selected as a control group，while 214 CAS patients were randomly divided into ASA group （n=72，po. aspirin entericcoated tablets 100 mg•d1），RS group （n=71,oral RS 10 mg•d1） and RA group （n=71，oral RS10 mg•d1 plus aspirin 100 mg•d1） for 6 months. All people must take low fat food during observation period. Carotid IMT，plaque number，serum lipids，highsensitivity Cresponsive protein（hsCRP） and matrix metalloproteinase9（MMP9） were detected before treatment and after 6 months. Results①Compared with those before treatment，hsCRP and MMP9 were lower （P＜0.05） ；HDLC was obviously increased （P＜0.05） and TC，TG，LDLC，hsCRP，MMP9，carotid IMT and plaque number were significantly decreased（P＜0.05 or P＜0.01） in RS and RA group. ②After treatment，HDLC was higher（P＜0.05 ） and TC,TG,LDLC,hsCRP,MMP9,carotid IMT and plaque number were lower（P＜0.05 or P＜0.01） in RS and RA group than those in ASA group；HsCRP,MMP9 and carotid IMT were lower in RA group than those in RS group （P＜0.05）. ConclusionRS and ASA have an antiatherosclerosis effect，and RS is superior to ASA；Combination therapy of RS plus ASA could exert significantly synergistic effect，and the mechanisms of which may be associated with lipidlowering，plateletblocking，and inflammatory inhibition.
  • 药物与临床
    Thirtythree Cases of Acute Cerebral Infarction Treated with Sodium Ozagrel in Combination with Aspirin
    GAO Chuansheng;CHEN Weiyan;TANG Qi
    2011, 30(6): 747-749. https://doi.org/10.3870/yydb.2011.06.017
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    ABSTRACTObjectiveTo explore the therapeutic effect on acute cerebral infarction by sodium ozagrel and kudiezi injection combined with aspirin. MethodsSixtysix eligible patients with acute cerebral infarction were enrolled in our study and randomly divided into 2 groups: thirtythree patients were treated with sodium ozagrel 80 mg ivgtt qd×14 d，NS 250 mL plus kudiezi injection 40 mL ivgtt qd×14 d as tested group; and 33 in the control group who were treated with dextran 40（Rhentran） 500 mL ivgtt qd×14 d，0.9% NS 250 mL plus kudiezi injection 40 mL ivgtt qd×14 d，ASA 0.1 g po qd×14 d；The effectiveness was evaluated according to the nervous defect standard （NDS） after 14 d’s treatmeant. ResultsThe genereal effective rate of the therapeutic group and the control one was 81.82%，63.64%（P＜0.05）,respectively.ConclusionThe curative effect of sodium ozagrel combined with kudiezi injection and aspirin is satisfied and without any toxic side effect.
  • 药物与临床
    132 Cases Oral Local Anesthesia Treated by Compound Articaine
    GUO Yuanlong;LV Yi
    2011, 30(6): 749-750. https://doi.org/10.3870/yydb.2011.06.018
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    ABSTRACTObjectiveTo observe clinical effects of compound articaine for oral local anesthesia. Methods220 patients in department of mouth rehabilitation were randomly divided into two groups: 132 patients were anesthetized by compound articaine group with a dose less than 1.7 mL, and 88 patients were anesthetized by 2% lidocaine hydrochloride with a dose less than 5 mL. Pains occurred during surgery，anesthetic effects and complications developed during anesthetization were analyzed. ResultsThe effective rate of compound articaine group and lidocaine hydrochoride group were 100.0% and 89.8%（P＜0.01）,respectively. The rate of side effects in the compound articaine group and lidocaine hydrochloride group were 1.5% and 12.5%（P＜0.01）,respectively.ConclusionCompound articaine is safe and effective for oral repairing anesthesia, which deserves wide clinical use.
  • 药物与临床
    Earlyphase of Clinical Phenomenon of Diabetes Caused by Clozapine in the Treatment of Schizophrenia
    YUE Weiqing;YAO Mingrong;CAO Ming;YUAN Tianyi;ZHA Xianyou;XIA Jiangming
    2011, 30(6): 751-753. https://doi.org/10.3870/yydb.2011.06.019
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    ABSTRACTObjectiveTo study the clinical features before development of diabetes caused by clozapine. MethodsThe clinical open surveys were used in 82 patients with schizophrenics who were given with clozapine only. The fasting plasma glucose，2 hours postprandial blood glucose，triglyceride（TG），blood cholesterol（TC），body weight，height，body mass index（BMI） were tested every month. The international physical activity questionnaire short form（IPAQSF） was used to assess these patients’ physical activity level. After one year followup，22 patients were diagnosed as diabetes. The diagnosed diabetes or the end of study was regarded as baseline. the investigated indicators were analyzed. ResultsTriglyceride and BMI in both diabetes groups were 2.95－3.94,1.93－2.31 mol•L-1 and 24.78－26.30,22.91－23.67,respectively（P＜0.01），physical activity of the diabetes group was lower than that of the nondiabetes group（P＜0.01）. ConclusionTriglyceride，BMI and physical activity level were abnormal 1 a before diabetes caused by clozapine.
  • 药物与临床
    Synergistic Effects by Small Dosage of Quetiapine in Treatment of Somatization Disorders
    WANG Jinlong;ZHAO Hedan
    2011, 30(6): 754-756. https://doi.org/10.3870/yydb.2011.06.020
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    ABSTRACTObjectiveTo explore the synergistic effects by small dosage of quetiapine in treatment of somatization disorders. MethodsA total of 84 patients with somatization disorder were randomly divided into the tested group（n=42） and control group（n=42）. Besides both groups were given with sertraline 100 mg•d1，the tested group was treated with small dosage of quetiapine gradually from 25 mg•d1 to 100 mg•d1 within a week for 8 weeks. The clinical efficacy was assessed by Hamilton Rating Scale of depression（HAMD） and Hamilton Rating Scale for Anxiety （HAMA），and adverse reactions were evaluated by Treatment Emergent Side Effect Scale（TESS） before and 1，2，4，8 week after treatment. ResultsThe effective rate of the tested group was 86.5% and the control was 77.1%（P＜0.05）. After one and two week’s treatment，the HAMD and HAMA scores in the tested group were significantly lower than those in the control group（P＜0.05 or P＜0.01），and adverse ractions in both groups were mild. ConclusionThe small dosage of quetiapine shows synergistic effects for the treatment of somatization disorders，which is safe and rapidaction and deserves to be widely used in clinical settings.
    • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    Quality Control of Yixinjiannao Soft Capsule
    ZHANG Shudan;JIANG Jianmin;YANG Minghua;NIE Lei
    2011, 30(6): 780-784. https://doi.org/10.3870/yydb.2011.06.031
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    ABSTRACTObjectiveTo establish a quality control method for yixinjiannao soft capsule. MethodsThe thin layer chromatography（TLC） for identification of Rhizoma chuanxiong，Rhizoma acori tatarinowii，Fructus schisandrae chinensis，Radix astragali and Radix dipsaci were established and the contents of schizandrin and asperosaponin Ⅵ were determined by HPLC. ResultsThe spots on TLC plates were clear and without interference in the blank reference. The calibration curves of Schizandrin and asperosaponin Ⅵ was linear between 0.08－1.60 μg （r= 0.999 96，n=7） and between 0.92－11.04 μg （r=0.999 99，n=7），respectively. The average recoveries of these two constituents were 99.56% with RSD=0.82% （n=6），and 99.49% with RSD=2.69%（n=6），respectively. ConclusionThe methods are reliable and reproducible，and which can be used for the quality control of this preparation.
  • 药物制剂与药品质量控制
    Content Determination of Osthole in Lifukang Lotion by HPLC
    LI Peng;CHEN Qinhua;ZHU Jun;PENG Lin
    2011, 30(6): 785-786. https://doi.org/10.3870/yydb.2011.06.032
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    ABSTRACTObjectiveTo establish a method for detecting osthole in lifukang lotion by RPHPLC. Methods RPHPLC was performed on DLC18 column （4.6 mm×150 mm，5 μm） with methanol：water （65：35） as mobile phase at flowing rate of 1.0 mL•min1. The detection wavelength was 322 nm. ResultsThe liner range of osthole was over 2100 μg•mL1，r=0.999 5. The precision expressed as the relative standard deviation （RSD） for the method was 1.52%. The mean extraction recovery was 99.7%，RSD was 1.12%. ConclusionThe method is proved to be accurate，sensitive and reliable，which is suitable for the determination of osthole in lifukang lotion.
  • 药物制剂与药品质量控制
    Content Determination of Dexamethasone in Dexamethasone Ointment by RPHPLC
    YANG Xijiang;HA Na;HA Li
    2011, 30(6): 787-788. https://doi.org/10.3870/yydb.2011.06.033
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    ABSTRACTObjectiveTo develop a method for content determination of dexamethasone in dexamethasone ointment by RPHPLC. MethodsThe separation was performed on Sinochrom ODSBP（4.6 mm×250 mm，5 μm）column with methanol：water（80：20） as a mobile phase，and with a wavelength of UV detector at 240 nm. The flowing rate was 1.0 mL•min1 and the loading volumn was 20 μL. ResultsThe linear range of dexamethasone was within 0.25－2.50 μg （r=0.999 9）.The average recovery of dexamethasone was 100.1% with RSD as 0.75%（n=9）. ConclusionThe method is simple，rapid，accurate and reliable，which can be applied to the quality control of dexamethasone ointment.
  • 药物制剂与药品质量控制
    Preparation and Quality Control of Ambroxol Hydrochloride Dispersible Tablets
    LIU Zuxiong;ZHANG Hong;YANG Xiaosong;FU Xudong;WANG Zhichao
    2011, 30(6): 789-791. https://doi.org/10.3870/yydb.2011.06.034
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    ABSTRACTObjectiveTo study the preparation and quality control of ambroxol hydrochloride dispersible tablets.MethodsUV spectrophotometry was used to detect dissolution of ambroxol hydroehloride dispersible tablets and HPLC was used to determine the content of ambroxol hydroehloride. ResultsThe linear range of ambroxol hydrochloride was over 15－45 μg•mL1. The average rate of recovery was 100.33% and RSD was 0.58%（n=9）. The dissolution of 3 batches of samples were all above 86.0%. ConclusionThe ambroxol hydrochloride dispersible tablets can disintegrate quickly in the water and disperse homogeneously. The preparation technology is reliable，simpl e and accurate，which can be used in producing and use of hospital preparations.
  • 药物制剂与药品质量控制
    In Vitro Dissolution Test of Propolis Soft Capsules
    WANG Lingbo;JIANG Xukai
    2011, 30(6): 792-794. https://doi.org/10.3870/yydb.2011.06.035
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    ABSTRACTObjectiveTo detect the dissolution of total flavonoids from propolis soft capsules. MethodsStirring basket method was used，and 1 000 mL 0.1 mol•L1 HCl was taken as dissolution medium. The rotation rate was 100 r•min1 and the test time was 45 min. The test solution was determined by UVVis at 265 nm. ResultsThe linearity regression equation was: Y=0.093 1X－0.058 8，and correlation coefficient was 0.999 5. The average recovery was 99.35%，RSD=1.51%. The same batch showed good uniformity. Dissolution parameters were as follows: T50=16.41，Td=22.98，T80=35.6，m=1.087 3. The dissolution of different batches were all above 80.0%. ConclusionThe established method is reliable，accurate，precise and rapid，which can be used to test the dissolution of propolis soft capsules.
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