Archive

• 01 March 2013 Volume 32 Issue 3

    

  ---

  药物研究
  论文
  药物研究
  呼吸系统疾病用药专栏
  药物与临床
  药物制剂与药品质量控制
  

• Select all
  |

药物研究
• Select
  药物研究

  Antioxidant Activity of Naringin on Myocardial Ischemia/Reperfusion Injury in Rats

  LIU Dan

  2013, 32(3): 275-277.

    Knowledge map   Save

  ABSTRACT ObjectiveTo investigate the protective effect of naringin on myocardial ischemia/reperfusion injury in rats and its possible mechanism. MethodsFifty male SD rats were randomly divided into five groups: sham operation group， ischemia reperfusion injury model group， and groups of naringin at low， middle and high doses, each containing 10 rats. Myocardial ischemia reperfusion injury was inflicted and the sham group was only threaded without ligation after completing all the operation. Three naringin groups were intragastrically administrated with corresponding doses of naringin once daily for 7 successive days. Sixty minutes after the last dose, animals were ligated for 30 minutes followed by 120 minutes of reperfusion. The model control was intragastrically administrated with the same volume of physiological saline and operated as other groups. The activities of glutathion peroxidase (GSHPx), superoxide dismutase （SOD）and the content of melondialdehyde (MDA) were detected in the myocardial tissue， and the activities of creatine kinase（CK）， lactate dehydrogenase (LDH)， catalase (CAT) in blood serum were also analyzed by the end of reperfusion.ResultsCompared with the model group， the activities of CK (3.44±0.06，2.71±0.08，and 2.21±0.08 U·mL－1) and LDH (3 780.88±248.44，3 339.58±234.28，and 2 693.57±130.59 U·mL－1) in blood serum and the content of MDA (4.46±0.27， 3.81±0.21，and 2.92±0.17 nmol·mg－1) in myocardial tissue were decreased in the low，middle and high dose groups of naringin (P＜0.05 and P＜0.01). On the contrary， the activities of the CAT (19.77±0.98，22.83±0.83，and 24.47±0.63 U·mL－1) in blood serum and GSHPx (25.36±0.84，31.40±1.10，and 39.08±1.16 U·mg－1) and SOD (92.05±3.08，112.59±4.83，and 129.88±5.82 U·mg－1) in myocardial tissue were increased in these groups (P＜0.01).ConclusionNaringin has protective effects on myocardial ischemia/reperfusion injury， the mechanism of which may be correlated with the antioxidant activity and reducing the lipid peroxidation.
• Select
  药物研究

  Effects of Shenqi Qiangjing Capsule on Sperm Quality, and Epididymic MDA and SOD Levels of the Rat Asthenospermia Model

  TIAN Yuanchun;ZHANG Quan;LU Haiwang;BIN Bin;LIANG Liying

  2013, 32(3): 278-281. https://doi.org/10.3870/yydb.2013.03.002

    Knowledge map   Save

  ABSTRACT ObjectiveTo investigate the effect of shenqi qiangjing capsule on the sperm quality in ornidazoleinduced asthenospermic rats.MethodsThe rat asthenospermia model was established by intragastric administration of ornidazole at the dose of 400 mg·kg－1·d－1. Animals were administrated with low， middle and high doses (400，800，1 600 mg·kg－1·d－1) of shenqi qiangjing capsules. The sperm motility， viability， and quantity as well as superoxide dismutase (SOD) and malondialdehyde (MDA) levels in epididymis were measured.ResultsCompared with the normal control，sperm motility was significantly decreased (P＜0.01)， MDA content in epididymis was significantly increased (P＜0.01), and the SOD activity was significantly reduced (P＜0.01) in the model control group. In the mid and high dose group, the sperm motility was increased significantly (P＜0.05 and P＜0.01, respectively), and the MDA level was decreased significantly (P＜0.01) in comparison with the model control. The SOD activity was enhanced in all three treatment groups (P＜0.05 or P＜0.01).Conclusion Shenqi qiangjing capsule can improve sperm motility of the male rats with ornidazoleinduced asthenospermia， which might be related to modulation of the oxidative stress injury.
• Select
  药物研究

  Effect of Aqueous Extracts from Shirako on Key Enzyme Activity in InsulinResistant HepG2 Cell Line

  WEI Nai-qiu;YANG Ke;XIAN Hanmei;HAO Yongjing;LIU Junhui;HUANG Xu

  2013, 32(3): 281-284.

    Knowledge map   Save

  ABSTRACT ObjectiveTo explore the effect of aqueous extracts from shirako on key enzyme activity in insulinresistant HepG2 cells. MethodsGlucose consumption and glycogen content of insulinresistant HepG2 were detected by glucose clinic test kit and hepatic glycogen test kit after treatment with water extracts of shirako. Activities of glucokinase (GK)， phosphoenolpyruvate carboxylase kinase (PEPCK)， and glucose6phosphatase (G6Pase) were assayed by the glucose 6phosphate dehydrogenase coupling colorimetric， lactate dehydrogenase coupling colorimetric and ammonium molybdate constant phosphorus methods.ResultsThe aqueous extracts of shirako enhanced glucose consumption， lowered the activity of G6Pase and PEPCK(71.41%,82.14%)， increased the activity of GK and glycogen content of insulinresistant HepG2(28.77%,96.73%).ConclusionAqueous extracts of shirako plays a role in lowering PEPCK and G6Pase activities and inhibiting glucogenesis， resulting in the reduction of endogenous glucose in the cell. In addition， it also can augment the activity of GK， accelerate the process of glucolysis， increase the glycogen content， and alleviate insulin resistance of HepG2.
• Select
  药物研究

  Screening of the Effective Fraction from Ganershu Compound on Liver Protection and Transaminase Reduction

  ZHANG Ting;YAN Guojun;MAO Minjue;JIANG Zhitao;PAN Jinhuo

  2013, 32(3): 285-288.

    Knowledge map   Save

  ABSTRACT ObjectiveTo evaluate the effects of four fractions isolated from ganershu compound on protecting liver and lowering transaminase. MethodsTotal flavonoids， saponins， alkaloids and organic acids were purified from water extracts of ganershu compound by macroporous resin， cationic resin， and anionic resin. Each of the four fractions and the mixture were given to mice with liver injury induced by 0.2% carbon tetrachloride (CCl4). The alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the mouse serum were detected， and both superoxide dismutase (SOD) and malondialdehyde (MDA) in the hepatic tissue were tested.ResultsThe fourfraction mixture， the total flavonoids and the saponins significantly inhibited the activity of serum ALT， AST in mice with acute liver injury (P＜0.01). The total alkaloids and total organic acids also decreased the activity of AST, ALT (P＜0.05) and SOD， and reduced the content of MDA (P＜0.05). The total bilirubin (TBiL) and liver index in the positive control and mixture groups were markedly decreased (P＜0.01 and P＜0.05, respectively) as compared to the total alkaloids and total organic acids groups.ConclusionThe four effective fractions of ganershu compound extract provide liver protection and transaminase reduction to different extents， with the mixture showing more pronounced effects.
• Select
  药物研究

  Effect of Lamotrigine on Sodium Current in Acutely Isolated Hippocampal Neurons of Rats

  GOU Yulan;ZHU Suiqiang;TANG Ming;LUO Lijun;CHEN Guohua

  2013, 32(3): 289-291.

    Knowledge map   Save

  ABSTRACT ObjectiveTo investigate the effect of lamotrigine (LTG) on sodium channel in acutely isolated hippocampal neurons of rats. MethodsThe hippocampal neurons of rats at the age of 7－10 d were prepared by chain wire fungus protease E and blowing. The effects of LTG on voltagedependent sodium channels were determined by using wholecell patch clamp technique. ResultsThe amplitude of voltagedependent sodium currents were decreased （15.35±3.01）% by LTG in a concentrationdependent manner at the dose of 100 μmol·L－1 . Moreover， LTG shifted the activation curve of sodium currents by (3.8±0.9) mV toward depolarization and the steady state inactivation curve of these currents by (1.8±0.9) mV toward hyperpolarization. ConclusionLTG can block voltagedependent sodium channels.
论文
• Select
  论文

  In Vitro Antibiotic Activities of Total Flavonoids from Guangxi Ampelopsis Grossedentata in Combination with βlactam Antibiotics

  ZENG Chunhui;YANG Ke;XU Mingguang;WU Guang;CHEN Yiqing;ZHONG Zhenguo

  2013, 32(3): 292-297.

    Knowledge map   Save
• Select
  论文

  HU Wenjin1，HU Wei2，FANG Yun2

  HU Wenjin;HU Wei;FANG Yun

  2013, 32(3): 297-300.

    Knowledge map   Save

  ABSTRACTObjectiveTo study the excretion of hydroxycamptothecine (HCPT) in urine and feces of mice via aerosol administration.MethodsThe urine and feces samples were collected at baseline and 0－3， 3－6， 6－9， 9－12， 12－24 and 24－48 h after aerosol administration. HPLCFLD was used to determine the concentration of unchanged HCPT and its metabolites in the urine and feces.ResultsThe unchanged drug was mainly excreted in the feces， with most of the drug excreted within the first 12 h. Excretion of HCPT in the urine largely occurred in the first 3 h without renal accumulation.ConclusionHydroxycamptothecine is mainly excreted unchanged after aerosol administration in mice.
药物研究
• Select
  药物研究

  in Vitro Bacteriostatic and Bactericidal Activities of Extracts from Chinese Honeylocust Spine

  LIU Jianjian;SHI Peng;HUANG Tao;ZHANG Kai;WU Dachang

  2013, 32(3): 300-302.

    Knowledge map   Save

  ABSTRACT ObjectiveTo explore bacteriostatic and bactericidal activities of Chinese Honeylocust Spine extracts against common laboratory bacteria (Escherichia coli， Bacillus subtilis， Staphylococcus aureus， Candida albicans， Pseudomonas aeruginosa) .MethodsExtracts from Chinese Honeylocust Spine were prepared with different solvents at various concentrations. The activities and minimum inhibitory concentration (MIC) were tested with filter paper and double dilution methods. ResultsThe extracts from Chinese Honeylocust Spine had little bacteriostatic or bactericidal effect against E. coli， Bacillus subtilis， Candida albicans， and Pseudomonas aeruginosa， but they showed moderate effects on Staphylococcus aureus. The MIC of water and ethanol extracts against Staphylococcus aureus was 25.0 and 12.5 mg·mL－1， respectively. ConclusionExtracts from Chinese Honeylocust Spine have both bacteriostatic and bactericidal actions against Staphylococcus aureus.
• Select
  药物研究

  Effects of Baicalein on the Fibrillation and Cytotoxicity of Amyloid βPeptide

  AI Weipeng;XIE Lixia;LIU Hongle;LIU Yani

  2013, 32(3): 303-306.

    Knowledge map   Save

  ABSTRACT ObjectiveTo investigate the effects of baicalein on the fibrillation and cytotoxicity of amyloid βprotein Aβ142. MethodsThe inhibitory effects of baicalein on Aβ142 fibril formation were determined by using thioflavin T fluorescence (ThT). The protective effects against cytotoxicity induced by Aβ142 in PC12 cells were evaluated by MTT assay. ResultsThe data from ThT fluorescence assay showed that baicalein had a dosedependent effect on inhibition of Aβ142 fibril formation and disaggregation of preformed Aβ142 fibril. It also reduced the neurotoxicity of Aβ142 on the cultured PC12 cells in (P＜0.01), as determined by the MTT method.ConclusionThese findings provide evidence that baicalein can effectively inhibit Aβ142 fibril formation and aggregation and significantly lower the neurotoxicity on PC12 cell line， suggesting that baicalein may be a candidate for prevention or treatment of Alzheimer's disease.
• Select
  药物研究

  Bioequivalence of Felodipine Sustainedrelease Tablets in Healthy Volunteers

  LIU Yi;QIU Lin;RAO Zichao;LIU Dong

  2013, 32(3): 306-309.

    Knowledge map   Save

  ABSTRACTObjectiveTo set up a method for determination of felodipine in human plasma by HPLCMS/MS and study the relative bioavailability and bioequivalence of felodipine sustained-release tablets.MethodsTwenty healthy male volunteers were randomized to receive a single dose of tested felodipine sustainedrelease tablet or the reference tablet by a twoway crossover design. Plasma concentration of felodipine was determined by HPLCMS/MS and the bioequivalence between two formulations were evaluated by DAS2.0 program.ResultsThe pharmacokinetic parameters of the tested and the reference felodipine tablet were expressed as follows: Cmax was （2.15±0.63） ng·mL－1 and （2.29±0.63） ng·mL－1，tmax was （6.33±1.57） h and （6.68±1.32） h， t1/2 was （18.22±2.75） h and （19.04±2.27） h， AUC048 were （58.11±5.15） ng·mL－1·h and （61.13±6.31） ng·mL－1·h. The relative bioavailability F was (95.06±8.42) %.ConclusionThe two felodipine sustainedrelease tablets are bioequivalent.
• Select
  药物研究

  Determination of 17 Amino Acids in Human Plasma by High Performance Liquid Chromatography with Precolumn Derivatization

  CHEN Rong;ZHOU Li;DONG Ji;ZHANG Hua;MIAO Liyan

  2013, 32(3): 310-312.

    Knowledge map   Save

  ABSTRACTObjectiveTo detect 17 amino acids in human plasma by HPLC with precolumn derivatization using 6aminoquinolylNhydroxysuccinimidyl carbamate (AQC).MethodsPlasma samples were pretreated with AQC as derivatization agent. The amino acid derivatives were separated on a C18 column with fluorescence detection (λex＝250 nm， λem＝395 nm) after gradient elution. The method was applied to determine the concentration of 17 free amino acids in human plasma from 22 healthy volunteers.ResultsThe analytes displayed a good linearity over the tested concentration range. The average recovery was within the range of (87.7±5.8)%－(117.1±8.4)%. The intra and intervariation coefficients were less than 10.3% and 11.0%， respectively. All tested amino acids in the plasma samples are within the normal reference range.ConclusionThe method is simple and stable with decent separation， which can be generally used to determine amino acids in human plasma.
呼吸系统疾病用药专栏
• Select
  呼吸系统疾病用药专栏

  Antipyretic， Antiinflammatory and Antitussive Effects of Jinchai Kanggan Capsule

  WU Shan;HE Kaiyong;PAN Wangping;LV Xiaojun;ZOU Rui;LIU Zhaoyun

  2013, 32(3): 313-315.

    Knowledge map   Save

  ABSTRACT ObjectiveTo investigate the antipyretic， antiinflammatory and antitussive effects of jinchai kanggan capsules.MethodsThe antipyretic， antiinflammatory and antitussive activities of the preparation were observed in the yeast induced fever in rats， croton oil induced auricular edema in mice, and aqua ammoniae induced cough in mice， respectively.ResultsThe jinchai kanggan capsules reduced body temperature elevation in rats between 3 ~ 6 h， alleviated auricular edema and prolonged cough incubation in mice.ConclusionThe jinchai kanggan capsule has antipyretic， antiinflammatory, and antitussive effects.
• Select
  呼吸系统疾病用药专栏

  Forty Cases of Adult Patients with Acute Asthma Treated with Atorvastatin

  XU Shu;LI Jing;DU Junxian

  2013, 32(3): 316-318.

    Knowledge map   Save

  ABSTRACT Objective To evaluate the shortterm relief and longterm control of acute moderate asthma in adult patients by atorvastatin.MethodsA total of 80 adult patients with acute moderate asthma were randomly divided into treatment and control groups， 40 cases in each. Both groups were administrated with fluticasone/salmeterol composite dry powder inhaler at the dose of 250 μg/50 μg twice a day in the acute phase and once daily in remission. The treatment group was also given 40 mg atorvastatin for the first day， followed by 20 mg daily for long term maintenance. We observed asthma symptoms， wheezing disappearance， length of hospital stay， forced expiratory volume in the first second (FEV1)， peak expiratory flow (PEF)， asthma control level within the following 3 months as well as adverse events in the two experimental groups.ResultsThe duration of asthma remission， wheezing disappearance， and length of hospital stay (4.60±0.18，5.28±0.18，and 7.50±0.20 d, respectively) in the treatment group were shorter than those (5.52±0.20，6.45±0.23，and 8.63±0.20 d, respectively) in the control group (P＜0.01). The experimental group had significantly better improvements of FEV1 (0.312±0.076 vs. 0.276±0.069 L，P＜0.05) and PEF (52.6±10.8 vs. 42.6±11.5 mL·min－1, P＜0.01) as compared to the control group. Asthma control within 3 months in the experimental group was better than that of the control group（92.5% vs. 70.0%，P＜0.05）. The two groups presented similar safety profile.ConclusionAstorvastatin is safe and effective for relieving symptoms of acute phase and the providing long term management of the disease in adult patients with asthma.
药物与临床
• Select
  药物与临床

  Relationship Between Aspirin Resistance and Gene Polymorphism of Platelet Membrane Glycoprotein Ⅱb/Ⅲa Receptor

  LIU Ju;HUANG Ting;MEI Qunchao

  2013, 32(3): 328-331.

    Knowledge map   Save
• Select
  药物与临床

  Escitalopram for Treating 116 Patients with Depressive Disorder

  WANG Qi;ZHANG Zhongdong;YU Haiyan

  2013, 32(3): 331-334.

    Knowledge map   Save

  ABSTRACT ObjectiveTo evaluate the efficacy and safety of escitalopram on depressive disorder in comparison with duloxetine and paroxetine . Methods A total of 297 patients with depressive disorder were divided into three groups: 116 cases in escitalopram group(20 mg·d－1)， 105 cases in duloxetine group (60 mg·d－1) and 76 cases in paroxetine group (20 mg·d－1). All of the patients treated for 6 weeks. The main efficacy was evaluated by 17 items on Hamilton Depression Scale (HAMD) at baseline and the end of 1， 2， 4，and 6 weeks after therapy. Moreover， the adverse effects were assessed with treatment emergent symptom scale (TESS). ResultsThe efficacy of the three drugs was 81.7% (escitalopram)， 77.8% (duloxetine) and 79.4% (paroxetine)， respectively， with showed no significant difference. The incidence of adverse reaction in the escitalopram group was higher than that of the other two groups， presenting no statistical significance. ConclusionEscitalopram is a newgeneration drug for depression with rapid onset of action and moderate adverse reaction.
药物制剂与药品质量控制
• Select
  药物制剂与药品质量控制

  Comparison of Dissolubility of the Active Ingredients in Ligusticum wallichii and Rhizoma cyperi with Different Extraction Approaches

  ZHANG Xinying;GUO Shuyun;ZHANG Wenjuan;WANG Qingwei;XU Yuan;ZHANG Tingting

  2013, 32(3): 350-353.

    Knowledge map   Save
• Select
  药物制剂与药品质量控制

  Effects of Cinnamon and Coptis in Different Compatibility Proportion on Content of Berberine in Jiaotai Bolus

  CHEN Guang;LU Fuer;LI Lingli;XU Lijun;ZOU Xin;WANG Kaifu;DONG Hui;HUANG Zhaoyi;HU Yayun

  2013, 32(3): 353-355.

    Knowledge map   Save

  ABSTRACTObjectiveTo explore the effects of cinnamon and coptis in different compatibility proportion on the dissolution rate of berberine from jiaotai bolus.MethodsAll the drugs were decocted and berberine content was determined on HPLC with a UV detector based on the following parameters: XTerra P18 (4.6 mm×250 mm， 5 μm) column， acetonitrile－0.05 mmol·L－1 potassium dihydrogenphosphate (30：70， pH 3.5 adjusted by phosphoric acid) as mobile phase， detection wavelength 346 nm， column temperature 40 ℃， flow rate 0.9 mL·min－1 and loading sample volume 10 μL.ResultsThere was marked difference in the extraction ratio of berberine between cinnamon combined with coptis in the proportion of 1：0.25, 1：0.5, and coptis single decoction. Moreover， the decoction rate of berberine decreased with cinnamon proportion increasing.ConclusionCinnamon has inhibitory effect on dissolution of berberine from coptis.
• Select
  药物制剂与药品质量控制

  Determination of Paeoniflorin and Baicalin in Biejiajian Pill by HPLC

  ZHANG Qing;MA Jun;XIN Lihua

  2013, 32(3): 356-359.

    Knowledge map   Save

  ABSTRACTObjectiveAn HPLC method was established for the determination of paeoniflorin and baicalin in biejiajian pill. MethodsPaeoniflorin was separated on a C18 column with gradient elution using the mobile phase of acetonitrile 0.05 mol·L－1 potassium dihydrogen phosphate solution，and detected at the wavelength of 230 nm. Baicalin was separated on the same column with methanolwaterphosphoric acid (42：58：0.5) as mobile phase，and detected at the wavelength of 280 nm.ResultsThe calibration curves were linear in the ranges of 0.076 6－1.532 8 μg and 0.061 4－0.770 4 μg，the average recovery was 98.0% and 96.5% （n＝6)，with RSDs of 0.7% and 1.1%，respectively.ConclusionTwo analytical methods were established to determine the two active ingredients for quality control of the biejiajian Pill.
• Select
  药物制剂与药品质量控制

  Separation， Purification and Determination of Total Flavonoids from Compound Qianyu

  MENG Junhua;LI Juyi;WU Jinhu;CHEN Yonggang;ZOU Jili;HE Yang

  2013, 32(3): 359-362.

    Knowledge map   Save

  ABSTRACT ObjectiveTo extract and separate total flavonoids from the Chinese herbal compound qianyu and establish a method for determination of total flavonoids and icariin. MethodsThe solvent combined with the polyamide resin column chromatography was adopted to separate and purify the total flavonoids. The content of total flavonoids and icariin in the extracts was determined by ultraviolet spectrophotometry and HPLC. ResultsThe contents of total flavonoids and icariine were 8.86% and 0.14% after extraction，and were 28.36% and 3.19% after purification， respectively.ConclusionThis extraction and purification approach is simple and reasonable， which can evidently improve the content of total flavonoids and icariin extracted from compound qianyu.
• Select
  药物制剂与药品质量控制

  EnzymeAssisted Impregnation Extraction of Nitidine Chloride from Zanthoxylum nitidum (Roxb.) DC.

  LU Shihui;LI Xiuxia

  2013, 32(3): 363-366.

    Knowledge map   Save

  ABSTRACT ObjectiveTo optimize a process for the impregnated extraction of nitidine chloride from Zanthoxylum nitidum (Roxb.)DC. after enzymatic pretreatment. MethodsThe orthogonal experiment was adopted to study the effect of pretreatment factors including pH， temperature and enzymolysis duration, and extraction factors such as solvents and extraction times on the extract rate of nitidine chloride.ResultsThe optimal process was as following: enzymolysis with substrates mass ratio (cellulose: pectinase) of 1：250， incubation with 4 times the buffer at pH 5 for 30 min at ambient temperature (30 ℃). Impregnated extraction was carried out for 3 times, 2 h each, with 60% alcohol containing 5 g·L－1 hydrochloric acid at the volume of 10， 4， and 3 times of the substrates. The extract rate of nitidine chloride was 85.96%.ConclusionThis process is costeffective， energysaving and environmental friendly， and provides an experimental basis for industrial production.