Archive

• 01 February 2009 Volume 28 Issue 2

    

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  特约稿
  药物研究
  神经科用药专栏
  药物与临床
  药物制剂
  

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特约稿
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  特约稿

  The History and Development of Antidepressants

  TONG Xiaoxin;TONG Etang

  2009, 28(2): 135-139.

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  ObjectiveSince the second half of the 20th century, there has been rapid development in the research of antidepressants. This paper presents a concise introduction of their historical, classification of chemical structure and action mechanism. It also gives a comprehensive introduction to the research development of new antipressants, including selective serotonin reuptake inhibitors ( SSRI ) , serotonin reuptake accelerant, selective serotonin and norepinephrine reuptake inhibitors ( SNRI), norepinephrine and special serotonin antidressant (NaSSA), norepinephrine and dopamine reuptake inhibitors ( NDRIs), new reversible monoamine oxidase inhibitor, new tricyclic, nature and herbal antipressants.
药物研究
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  药物研究

  Effect of Ligustrazine Derivative on Cytosolic Free Calcium Concentration in Smooth Muscle Cells from Human Spongy Body of Penis

  ZHANG Lidong;LIU Jihong;LI Sui;LIU Miaona;LIN Zhicheng;YAN Shuchao;YIN Chunping

  2009, 28(2): 148-150.

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  ObjectiveTo study the effects of ligustrazine derivatives（A3A6） on intracellular free calcium (Ca2＋)i in cultured human penis corpus cavernosum smooth muscle cells(PCSMC). MethodsBy using laser scanning confocal microscope(LSCM),the Ca2＋i Fluorescence signal changes was investigated in cultured PCSMC loaded with Ca2＋ indicator Fluo3/AM. Compared with TMP and the classical calcium antagonist Ver, effects of ligustrazine derivatives on Ca2＋i increase induced by NE were observed at the same concentration. ResultsThe peak inhibition rates of ligustrazine derivatives（A3A6） were 49.03%, 54.83%,51.48%,50.31%, respectively induced by NE at the concentration of 0.2 mmol•L-1, which were more potent than ligustrazine（18.96%）, much more than Ver（16.51%）（P＜0.05）.ConclusionLigustrazine derivatives（A3A6） can inhibit Man PCSMC Ca2＋i,significantly by suppressing voltage dependent calcium channel, which is more effective than TMP.
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  药物研究

  Effects of Shenmai Injection on Rat Diaphragmatic Muscle Cell Apoptosis, SOD, MDA and NO after Chronic Hypoxia

  JIANG Dongxia;ZHAO LImin;MA Lijun

  2009, 28(2): 150-152.

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  ObjectiveTo study the effects of shenmai injection(SMI) on rat diaphragmatic muscle cell apoptosis, superoxide dismutase (SOD), malondisldehyde (MDA) and nitric oxide (NO) after chronic hypoxia. MethodsRats were hypoxic for one week. The levels of SOD, MDA and NO were measured by photometry. TUNEL was employed for detecting apoptosis. ResultsThe level of SOD was decreased, while MDA and NO were both increased in rats with chronic hypoxia. Theses changes were all blocked by SMI. After chronic hypoxia, cell apoptosis was increased but which was inhibited by administration of SMI. ConclusionThe apoptosis induced by chronic hypoxia could be blocked by SMI, which might be associated with blocking generation of free radicals.
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  药物研究

  The Lipidlowering Function and Antioxidative Effect of Jiangzhining Granules

  LI Shuwen;WU Qinghe;HUANG Ping

  2009, 28(2): 153-155.

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  ObjectiveTo explore the lipidlowering function and antioxidative effect of jiangzhining granules. MethodsThe hyperlipidemia model in rats was established by feeding rats with high lipid food, and the model rats, were given with jiangzhining. TC、TG、HDLC、MDA、SOD、GSHPx、BUN、TP、ALB in serum were detected after 15 days. ResultsJiangzhining significantly decreased TG、MDA and increased HDLC、GSHPx in serum. ConclusionJiangzhining shows obvious lipidlowering effect which results from improving antioxidative ability, eliminating redundant free radicals and preventing lipid peroxidation.
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  药物研究

  Effects of Amiodarone　Hydrochloride　Injection on the Proliferation of Human Esophageal Carcinoma Cell EC9706

  ZHU Shaoping;MAO Zhifu;HUANG Jie;WANG Junyu

  2009, 28(2): 155-157.

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  ObjectiveTo explore effects of amiodarone hydrocloride on cell proliferation and cell cycle of human esophageal cancer cell EC9706 in vitro. MethodsEC9706 cells proliferation was detected by MTT test, and parameters of cell cycle distribution was measured by flow cytometry (FCM) after being treated with amiodarone hydrocloride or 5fluorouracil (5Fu). ResultsEC9706 cells proliferation was inhibited dramatically along with the increase of amiodarone hydrocloride added from 0.5 to 4.5 μg•mL-1, which showed obvious concentrationeffect relation and timeeffect relation. There were marked differences in parameters of cell cycle distribution and inhibition rates between amiodarone hydrocloride group and the control group(P＜0.01); however, no statistical significance was observed between amiodarone hydrocloride group and 5Fu group. The characteristics of cell cycle distribution changed markedly when EC9706 cells were interfered with amiodarone hydrocloride of abovementioned concentration in vitro: the percentage of cells in stage G0/G1 and G2/M increased, while that of cells in stage S reduced. The trend is similar to that of 5Fu group. ConclusionAmiodarone hydrocloride can inhibit the proliferation of EC9706 in vitro, which showed concentrationeffect relation and timeeffect relation.
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  药物研究

  Components Analyzing in Essential Oil Extracted with Supercritical Carbon Dioxide from Congbai by GC-MS

  ZHOU Yinbo;ZHANG Changgong;FU Qinqin;WANG Zhong;WANG Wei;WANG Qiong;WEN Rong

  2009, 28(2): 158-159.

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  ObjectiveTo analyze the chemical components of essential oil from Congbai. MethodsThe volatile oil was extracted with supercritical carbon dioxide, the components in which and contents were determined by GCMS and normalization method. Results16 components from Congbai by SFE were separated and identified. The main compounds of volatile oil were diterpenoids, fatty acids, alkanes, organosulfur compounds. ConclusionWe have investigated the low polarity gradients from the volatile part of Congbai, the way of which benefits for further studying of Congbi .
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  药物研究

  Extraction and Antihypoxia Effect of Eucommia Polysaccharides in Mice

  XIN Xiaoming;WANG Yuanli;WANG Hao;FEI Hongrong;ZHU Yuyun;GAO Yunsheng

  2009, 28(2): 160-162.

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  ObjectiveTo study the antihypoxia effect of eucommia polysaccharide in mice, in order to provide the theory basis for further development and use of eucommia. MethodsMice were given orally with different dosages of eucommia polysaccharide continuously for 7 days.1 hour after the last administration, the antianoxia action under normalpressure, acute cerebral ischemia anoxia test and the hemorrhagic shock experiment were carried out. The survival time, the breath after the halt of whole brain blood supply and the heartbeat were observed. Results10.9 g polysaccharides were gained from 500 g of eucommias crudes. The results showed that eucommia polysaccharide prolonged the survival time, maintained the breath and the heartbeats after the whole brain blood supply stopped. ConclusionThe eucommia polysaccharide may protect against hypoxia in mice.
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  药物研究

  Effect of Total Coumarins from Radix Angelicae Dahuricae on Pharmacokinetics of Aminophylline in Rabbits

  LI Chao;WANG Decai;WU Congping

  2009, 28(2): 162-164.

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  ObjectiveTo study the effect of total coumarins from Radix Angelicae Dahurica(TCD) on pharmacokinetics of aminophylline in rabbits. MethodsA selfcontrolled method was used. 9 rabbits were intravenously injected with aminophylline 15.0 mg•kg1. After 6 days, the rabbits were orally administered with TCD 50.0 mg•kg1, qd, for 3 days, and then given animophylline 15.0 mg•kg1 again. The serum concentrations of theophylline were determined with spectrophotometer. ResultsBefore TCD administration, elimination rate constant(K),half life(t1/2), apparent volume of distribution(Vd),clearance(CL) and area under curve(AUC) of theophylline were 0.213 h1, 3.253 h, 1.416 L, 0.302 L•h1 and 134.322 μg•h•mL1 respectively. After TCD administration, K, t1/2, Vd, CL and AUC were 0.139 h-1, 4.993 h, 1.437 L, 0.200 L•h1 and 202.968 μg•h•mL1 respectively.ConclusionThe serum concentrations and AUC of theophylline were significantly increased, t1/2 prolonged, K and CL decreased in the rabbits after administered with TCD. It is concluded that TCD inhibits the normal metabolism of theophylline.
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  药物研究

  Study on the Relative Bioavailability and Bioequivalence of Lansoprazole Table

  LI Qian;DENG Jungang;QIAO Jian;LI Weiyong

  2009, 28(2): 165-167.

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  ObjectiveTo study the relative bioavailability and bioequivalence of lansoprazole tablets and lansoprazole capsules in human plasma. Methods　19 healthy volunteers in randomized crossover study were given a single oral dose of 30 mg of the test or of the reference. 12 h later,blood was taken out at several time points. The plasma level of lansoprazole was determined by HPLC. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS2.0 program. 　ResultsCmax of the test formulation and the reference one were , (662.14±360.85) and (649.85±356.29) μg•L1; tmax were (2.82±0.53) and (2.26±0.63) h; AUC0→12 were (1 788.12±1 078.25) and (1 857.72 ±1 136.34) μg•h•L1; AUC0→∞ , (1 892.97±1 108.87) and (1 938.03±1 160.68) μg•h•L1 , respectively. The 90% confidential interval of Cmax , AUC0→12 and AUC0→∞ of the test were 97.8%～104.8%, 90.0%～101.9% and 92.0%～103.2% , respectively. The relative bioavailability was (96.8±15.1) % for the test and reference preparation. ConclusionThe two formulations are bioequivalent.
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  药物研究

  Pharmacokinetics and Bioequivalence of Cefdinir Dispersible Tablet in Healthy Volunteers

  REN Ping;ZHAO Gang;KE Xu;GU Shi-fen;CHEN Hui

  2009, 28(2): 168-170.

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  ObjectiveTo study the relative bioavailability and bioequivalence of cefdinir dispersible tablet in healthy volunteers. Methods In a randomized crossover study, 20 healthy male volunteers were given a single oral dose of 100 mg test and reference dispersible tablet. A reversed-phase high performance liquid chromatography was employed for determining cefdinir in plasma, for which pharmacokinetic parameters were calculated and the relative bioavailability of two formulations was evaluated by using DAS 2.0 software.ResultsThe main pharmacokinetic parameters of the test and reference dispersible tablets were as follow: Cmax were (0.920±0.236) and (0.907±0.216) μg•mL-1; tmax were (3.375±0.944) and (3.625±0.825) h; t1/ 2 were (1.826±0.600) and (1.910±0.597) h; AUC0-10 were (4.305±1.080) and (4.392±1.224) μg• h•mL-1; AUC0-∞ were (4.632±1.147) and (4.803±1.325) μg• h•mL-1; The relative bioavailability of the test preparation was (101.0±23.2)%. ConclusionThe test and reference dispersible tablets were bioequivalent.
神经科用药专栏
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  神经科用药专栏

  Improvement of Learning and Memory Function by Aqueous Extract of Salvia Miltiorrhiza Bge．F．alba．C．Y．wu．et H•W •Li in Mice

  WANG Hao;GAO Yunsheng;ZHANG Qingle;XU Xiaoyan;CHEN Wei;ZHU Yuyun

  2009, 28(2): 173-175.

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  ObjectiveTo study the effects of aqueous extract of Salvia miltiorrhiza Bge．F．al ba．C．Y．wu．et H•W•Li on learning and memory function of mice. MethodsThe mice were ig aqueous extract of Salvia miltiorrhiza Bge．F．alba．C．Y．wu．et H•W •Li for one week continuously. Effect of the aqueous extract on learning and memory function of normal and dysmnesia mice was observed by using Y shape labyrinth. ResultsThe aqueous extract improved the learning and memory function of normal and dysmnesia mice. ConclusionIt is suggested that aqueous extract of Salvia miltiorrhiza Bge．F．al ba．C．Y．wu．et H•W •Li could markedly enhance the learning and memory ability, which could prevent and cure the senile dementia.
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  神经科用药专栏

  Effects of Minocycline on Activity and Expression of Caspase3 Induced by Focal Cerebral Ischemia Following Reperfusion

  SHEN Xiaoyan;WANG Xuejun

  2009, 28(2): 175-178.

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  ObjectiveTo investigate the underlying neurobiological mechanism of the protective effect by minocycline after temporary middle cerebral artery occlusion (tMCAO) in rats. MethodsRats underwent 90 min of MCAO. Minocycline or saline placebo was administered intraperitoneally starting at reperfusion. Neurofunctional tests, drywet ratio and apoptosis rate for brain edema were carried out at 24 h after tMCAO and the expression of caspase3 were detected by Western Blot. ResultsThe severe neuronic deficits, the drywet ratio and apoptosis rate induced by tMCAO were significantly improved after treated with minocycline (P＜0.05); meanwhile, the expression and activity of caspase3 were significantly decreased (P＜0.01). ConclusionMinocycline can decrease the expression and activity of caspase3 and therefore protect against tMCAO.
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  神经科用药专栏

  The Effect of Resveratrol on Expression of Interleukin-6 Induced by Fibrin in Rat Brain Vascular Endothelial Cells

  XUE Zheng;CHENG Mingzhen;HU Xiaoqing;ZHANG Suming

  2009, 28(2): 178-181.

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  ObjectiveTo investigate the effect of Resveratrol on expression of interleukin6(IL6) induced by fibrin in rat brain vascular endothelial cells . MethodsThe concentration of IL6 was measured by Elisa kit and the mRNA of IL6 was measured by RTPCR after cultured with 1.0 mg•mL-1 fibrin polymerization on rat brain vascular endothelial cells in the presence or absence of different concentration of resveratrol（0－50 μmol•L-1）. ResultsAfter 24 h of incubation,25 and 50 μmol•L-1 of resveratrol could significantly reduce IL6 protein expression（P＜0.01）and IL6 mRNA level （P＜0.01）induced by fibrin compared to the control group. ConclusionResveratrol is potent inflammatory cytokine inhibitor which could reduce IL6 expression in the coculture of rat brain vascular endothelial cells with fibrin.
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  神经科用药专栏

  Effects of Tongxinluo on VEGF Expression and Angiogenesis of Rats with Cerebral Infarction

  YANG Yexin;YE Lianzhen;HE Gang;LIANG Xinyu;MEI Yuanwu

  2009, 28(2): 182-184.

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  ObjectiveTo evaluate the effects of tongxinluo on VEGF expression and angiogenesis and functional outcome after cerebral infarction in rats. Methods55 male SD rats were divided into control group, model group and tongxinluo(TXL) group randomly. The rat model of focal cerebral infarction was established with unilateral middle cerebral artery (MCA) suture occlusion in the model group and TXL group. The rats in TXL group were given by gavage with TXL (1 g•kg1•d1) for 14d, while those in other groups were reared in their original living state. VEGF expression and angiogenesis were measured in the boundary zone to brain infarction at 1, 3, 7, 14 and 28 d. Results It was found that VEGF expression started at 1 d, subsequently increased, and reached peak value at the 3 d, failed away until 7 d in model group and TXL group. VEGF expression was mainly detected in the boundary zone of the infarcts at every timepoint. To compare with the model group, VEGF expression of TXL group was significantly increased in 3 and 7 d after MCAO. Compared with the control group, the microvessel density (MVD) in model group and TXL group were significantly increased at 14 and 28 d after MCAO, especially in TXL group. ConclusionTongxinluo may increase the VEGF expression and promote the blood vessel proliferation in rats with cerebral infarction.
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  神经科用药专栏

  Protective Effect of Etomidate on Ischemic Spinal Cord Injury of Rabbits

  YU Qijing;ZHOU Qingshan;HUANG Haibo

  2009, 28(2): 185-188.

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  ObjectiveTo study the effect of etomidate on spinal cord injury induced by ischemia/reperfusion (I/R) .MethodsTwenty four white adult Japanese rabbits were randomly assigned to 3 groups: groupA, shamoperation group (n=8); group B, ischemic reperfusion group; group C, ischemiareperfusion with etomidate. Spinal cord ischemia was induced by infrarenal aortic crossclamp for 40 minutes in groupB and group C. Etomidate 0.5 mg•kg-1 was intravenously injected 10min before clamping and then infused at a rate of 3 mg•kg-1•h-1 until unclamping in group C,0.9% saline was used as control in other groups. After surgical operation, postoperative neurological function, electromyography of rear limbs, histopathology, malondialdehyde (MDA) levels and superoxide dismutase (SOD) activities in the spinal cord were assessed for all animals. ResultsCompared with group A, group B showed significant I/R injuryinduced changes in the neurological function scores, histopathology and electromyography (P＜0.01). However, groups C treated with etomidate significantly reversed these changes of all parameters (P＜0.01). Meanwhile, I/Rinduced increase in MDA content observed in group B were also significantly reduced in group C (P＜0.01), and I/Rinduced decrease in the SOD activities were also significantly prevented in etomidate treated group (P＜0.01). ConclusionEtomidate showed potent protective effects against spinal cord I/R injury in the rabbit model, and protected loss of antioxidant activities of the spinal cord as well.
药物与临床
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  药物与临床

  Clinical Study of Hydroxycamptothecin Inravesical Instillation for Preventing Postoperative Recurrence of Bladder Carcinoma

  ZENG Wenli;XIA Yue

  2009, 28(2): 200-201.

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  ObjectiveTo investigate the clinical effect of hydroxycamptothecin inravesical instillation for preventing postoperative recurrence of bladder carcinoma. Methods72cases of bladder carcinoma were treated by conservative bladder operation. Clinical effect and recurrence rate of bladder carcinoma were evaluated by followup. ResultsFollowup showed that the total recurrence rate of bladder carcinoma was 18.1% and the rate of superficial carcinoma was 14.3% with lower side effect. ConclusionInravesical instillation of hydroxycamptothecin is a safe and effective treatment for preventing postoperative recurrence of bladder carcinoma.
药物制剂
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  药物制剂

  Determination of the Prescription and Evaluation of Characters for Amphotericin B Liposomes Dry Powder Inhalation

  GUO Huili;MEI Xingguo;LI Gao

  2009, 28(2): 225-228.

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  ObjectiveTo investigate the in vitro characters of Amphotericin B liposomes dry powder, select a suitable carrier and determ the best formulation of inhalation powders. MethodsAmphotericin B liposomes dry powder was dehydrated by freeze drying and spray drying method;the particle size of the two kinds of powders was compared by determining the deposition rate of active parts. ResultsThe particle size of the powder prepared by freeze drying was larger than that by spray drying. The higher deposition rate was found at the ratio of dry powder to the lactose carrier as Inhalac230 being 1：1, which were 11.95% for freeze drying particles and 20.08% for spray drying powder . ConclusionThe particles of dry powder prepared by spray drying method is smaller, and the deposition rate of active part is higher than that of freeze drying powders.
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  药物制剂

  Comparison of Liposoluble Constituents Extracted by SFE-CO2 and Percolation from Salvia Miltiorrhiza

  HAN Xiaoke;LIU Hanqing;ZHANG Ming;MA Junhua;MA Jiyong

  2009, 28(2): 228-230.

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  ObjectiveTo seek the optimal method and conditions for extracting liposoluble components from salvia miltiorrhiza, in order to develop comprehensive utilization of salvia miltiorrhiza. Methods The optimal extraction technology was chosen out by comparing and testing as contents of tanshinoneⅡA. ResultsThe optimized conditions for SFECO2 extraction were as follows: pressure 35 MPa, 100% ethanol as modifier, the temperature 40 ℃, the operation time 2 h, with the content reached 3.87 mg•g-1. The optimized conditions for Percolation were that 95%alcohol, 16fold solvent amount, flow rate 1.0 mL•min-1, 20 meshes drug powder, with the content reached 3.28 mg•g-1.ConclusionSFECO2 is better than percolation with the higher extraction content, which shows that the comprehensive utilization of salvia miltiorrhiza could be feasible.