Archive

• 01 January 2007 Volume 26 Issue 1

    

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  药物研究
  消化系统用药专栏
  药物与临床
  药物制剂
  药品质量控制
  用药指南
  

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药物研究
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  药物研究

  Experimental Study on Acute Toxicology of Flourouracil Magnetic Albumin Deutomicrosphere

  XU Rong;ZHOU Shun-chang;CHENG Si-xiang;CHEN Hui;ZENG Fan-dian

  2007, 26(1): 6-7.

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  ABSTRACT Objective To investigate the acute toxicology of flourouracil magnetic albumin deutomicrosphere (5-FuMAD) for further use.Methods The acute toxic reaction and the main viscera pathological morphology of mice were evaluated after given 5-FuMAD by intravenous injection via vena caudalis with different doses respectively.Results LD50(median lethal dose) of 5-Fu injection was194.54 mg/kg,and its 95% confident interval was 161.2－234.8 mg/kg.The maximum tolerance dose(MTD) of 5-FuMAD was 1 250 mg/mL. Degeneration and necrosis of viscera were not found in both groups. Conclusion MTD of 5-FuMAD is 5 times the value of the therapeutic dosage. The toxicity is low and it may have potential clinical application．
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  药物研究

  Advanced Glycation Endproduct Induces Fractalkine Expression in Rat Glomerular Mesangial Cell

  WANG Bi-fei;SUN Liao;LIU En-bo;LI Hong-hui;TANG Ping;YANG Jing-xin

  2007, 26(1): 8-11.

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  Objective To explore the effect of advanced glycation endproducts(AGE) on fractalkine expression in rat glomerular mesangial cell. Methods Rat glomerular mesangial cells were cultured in vitro. The study was designed to divided into AGE group: cells were incubated with AGEBSA ( 100 mg·L^-1),control group: BSA（100 mg·L^-1）,antiAGE group:cells were incubated with antiAGE antibody for 2h,then coincubated with AGEBSA ( 100 mg·L^-1),PDTC group: PDTC（100 μmol·L^-1）for 1 h, then AGEBSA ( 100 mg·L^-1). Fractalkine mRNA and protein expression was analyzed by RTPCR and Westernblot. NFκB activation was detected by laser confocal microscope. Results AGEBSA induced fractalkine mRNA and protein expression in mesangial cells abundantly which can be inhibited by PDTC and antiAGE antiboby remarkably. Having stimulated by AGEBSA for 15 min, NFκB/P65 translocated into nucleus, and reached to the peak in 30 min. Conclusion AGEcan induce fractalkine mRNA and protein expression in mesangial cells through activating NFκB.
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  药物研究

  Effects of Kinetin on Expression of MMP-2 and TIMP-1 at the Progression of CCl₄inducing Rat Hepatic Fibrosis

  ZHANG Zhen-gang;TIAN De-ying;ZHOU Jian;MA Xiao-jun;XU Dong;HUANG Yuan-cheng;SONG Pei-hui

  2007, 26(1): 11-14.

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  Objective To probe into the effects of kinetin on expression of MMP-2 and TIMP-1 at the progression of rat hepatic fibrosis induced by CCl₄. Methods 60 male and female Wistar rats were divided into 3 groups. Rats of the model group were injected with 40% CCl₄ 0.3 mL·(100 g)^-1 subcutaneously , twice a week. At the basis of the model group, rats of the trial group were injected with 40% CCl₄ and 0.1% kinetin solution 0.5 mL·(100 g)^-1, rats of the control group were injected with the equal volume of 0.9% sodium chloride solution. After 12 weeks, examination was based on microscopy, and the degrees of inflammation and fibrosis of liver tissues were examined by hematoxylineosinstain. The expression of MMP-2 and TIMP-1 were detected by immunohistochemistry. Results The extent of liver fibrosis improved significantly after kinetin was administrated into rat with liver fibrosis. The expressions of MMP-2 and TIMP-1 in the liver tissues of the treatment group were markedly decreased compared with those of the control group. Conclusion Kinetin can inhibit liver fibrosis. One of the possible antifibrotic mechanisms of Kinetin is to reduce the expression of MMP-2 and TIMP-1 in liver of rat hepatic fibrosis.
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  药物研究

  Inhibition of Cinobufacini on the Production of IL2 from Mouse Spleen Lymphocyte

  CHEN Na;CHEN Xingping

  2007, 26(1): 14-16.

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  Objective To study the effect of cinobufacini on the IL-2 production from mouse spleen lymphocyte. Methods After the separation and purification of spleen lymphocytes from mice, spleen lymphocytes, induced by PHA-P, was co-cultured with cinobufacini. ELISA was used to detect the level of IL-2 production. Results Cinobufacini , 0.20－0.40 mg·mL^-1 ,enhanced IL-2 production from mouse spleen lymphocytes. There was significant difference (P＜0.05) between cinobufacini and control groups. ConclusionCinobufacini can enhance IL-2 production from spleen lymphocytes.
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  药物研究

  An Experimental Study of the Neuroprotective Effect of Uric Acid after Spinal Cord Injury in Rats

  LIU Tie;ZHOU Song;ZHANG Fan;GUAN Han-feng;CHEN Chao;LI Feng

  2007, 26(1): 16-19.

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  Objective To study the neuroprotective effect of uric acid (UA) after acute spinal cord injury(SCI) in rats. Methods Fortyfive female adult SD rats were randomly divided into 3 groups: the control group(n=5), spinal cord injury group with saline treatment ,and a group using UA treatment. All spinal cord injury models were made in Allen’s way. In UA treatment group,UA 500 mg·kg^-1 (prepared into suspension by 0.9% sodium chloride solution)was injected into peritoneal cavity 1 hour before and 4 hours after SCI. In other groups the same volumes of saline were injected at the same time spots. The level of malondialdehyde(MDA) and superoxidedismutase(SOD) in the injured spinal cord tissue were detected and the tissue sections of the injured spinal cord were stained with hematoxylin and eosin, and terminal deoxynucleotidyl transferasemediated dUTP nick end labeling methods(TUNEL) were adopted to label the apoptotic cells at 8,24,72 h , 7 d after the injury. ResultsAs compared with the spinalcord injury group, the MDA levels in tissues of spinal cord was reduced and SOD levels increased significantly in UA treatment group. The pathological changes of spinal cord were improved in the UA group, the apoptotic cells were decreased in the UA group than those in the SCI group. ConclusionThe results suggest that UA has neuroprotective effects on the injured spinal cord by inhibiting free radical induced injury and decreasing apoptosis after acute spinal cord injury in rats.

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  药物研究

  Study on Adsorption Process of Total Flavonoids in Drynaria Fortunei with Macropore Resin

  CHEN Shun;GUAN Yan-bin

  2007, 26(1): 19-21.

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  Objective To study the absorptions process of total flavonoids in Drynaria fortunei with macropore resin. Methods AB-8 resin was selected to investigate its static adsorption and adsorption kinetics, and the absorption isotherm curve with Freundich and Langmuir equations was simulated in 25 ℃. Different concentrations of alcohol for the absorptions were also studied, and the throughout curve was made for judging the end of elution. Results Both of Freundich and Langmuir equations fit the absorption isotherm curve very well. The 50% alcohol was the best concertration for elution. Conclusion The properties of AB-8 resin is good for absorption and desorption of total flavonoids, and the parameters can reflect the inner properties of absorption.
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  药物研究

  Determination of Clarithromycin in Human Plasma by Liquid Chromatographymass Spectrometry(LC-MS)

  ZHENG Heng;CHEN Ya-li;WANG Li;FANG Shu-xian

  2007, 26(1): 22-23.

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  Objective To develop a LC-MS method for the determination of clarithromycin concentration in human plasma. Methods 20 mL of roxithromycin solution(10 μg·mL^-1,internal standard)were added to 0.20 mL of plasma. The plasma samples were extracted with 4 mL ether after alkalizing using 0.1 mol·L^-1 Na₂CO₃. 3 mL of organic layer were transferred to a clean tube and evaporated to dryness under N2. The residue was reconstituted in 1 mL acetonitrile and 10 μL were injected into an ODS C18 (5.0 μm,250 mm×2.0 mm)column. The mobile phase consisted of acetonitrile:0.05% acetic acid(60：40)at flow rate of 0.2 mL·min^-1 . The eluate from the HPLC column was plumbed directly into ESI probe. Analysis in the mass spectrometer was operated in the selectedion monitoring model. Results The standard curve was linear in the range of 0.010－5.00 μg·mL^-1.The detection limit was 0.010 μg·mL^-1. The interday, intraday variability and relative recovery rate were suitable for biological analysis. Conclusion The method of LCMS is suitable for pharmacokinetic study of clarithromycin in human plasma.
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  药物研究

  Studies on Non-alkaloid Constituents from the Stem and Leaf of Fritillaria Hupehensis

  ZHANG Jiu-liang;PI Hui-fang;RUAN Han-li;ZHANG Yong-hui;WU Ji-zhou

  2007, 26(1): 23-25.

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  Objective To study the chemical constituents from the stem and leaf of Fritillaria hupehensis. Methods The stem and leaf of Fritillaria hupehensis were divided into two parts: alkaloids parts and nonalkaloids parts. Several chemical fractions were prepared from the nonalkaloids parts, and five compounds were purified from the acetic ether parts by the methods of the silica gel column. The five compounds were identified by the modern spectral technology such as MS, ¹H-NMR, ¹³C-NMR. Results Five compounds were isolated from the nonalkaloid parts of the stem and leaf of Fritillaria hupehensis. There were CH₃(CH₂)₂₆CH₃ 、CH₃(CH₂)₂₄OH、CH₃(CH₂)₂₀COOH, β-sitosterol and daucosterol. Conclusion These compounds were all obtained from the stem and leaf of Fritillaria hupehensis for the first time. And the first three compounds were got for the first time from Fritillaria.
消化系统用药专栏
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  消化系统用药专栏

  Effect on Hyperammonaemia after Eradication Therapy of Helicobacter Pylori Infection in 42 Patients with Liver Cirrhosis

  LUAN Shuang-mei;WANG Wang-yue;LI Hong-guang;ZHANG Xiao-jun;ZHU Ya-bi;HUANG Lan;ZHANG Li-ping

  2007, 26(1): 27-28.

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  Objective To study the effects on hyperammonaemia after eradication therapy of Helicobacter pylori(Hp) infection in patients with liver cirrhosis. Methods Ammonia concentrations in blood were examined. Among 65 patients with liver cirrhosis,42 cases were positive of helicobacter pylori and 23 negative. The cases of Hp positive were divided into group A and B. Patients in group A were treated with antiHp drugs. Data of ammonia were analysed after eradication of Hp. Results Ammonia in patients with Hp positive liver cirrhosis was significantly higher than that in patients with Hp negative liver cirrhosis. Ammonia after eradication of Hp in group A was significantly lower than that in group B. Conclusion Helicobacter pylori infection could induce hyperammonia in patients with liver cirrhosis which may be one of the factors to induce hepatic encephalopathy. The eradication of helicobacter pylori is effective to lower blood ammonia in patients with liver cirrhosis hyperammonia.
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  消化系统用药专栏

  Observation Study on Paclitaxel/Oxaliplatin/Capecitabine Regimen as Firstline Therapy for Patients with Advanced Gastric Cancer

  HU Guo-yong;YANG Jian-guo;DING Yan-bing;WU Jian;XIAO Wei-ming

  2007, 26(1): 29-31.

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  Objective To evaluate the objective response rate and toxicity of paclitaxel/oxaliplatin/capecitabine regimen as firstline therapy for patients with advanced gastric cancer. Methods Thirty six patients with advanced gastric cancer were administrated with intravenous paclitaxel 90 mg·（m2）^-1·d^-1 (d1 , d8) , intravenous oxaliplatin 100 mg·（m2）^-1·d^-1 (d1 , d8) , and oral capecitabine 1 250 mg·（m2）^-1·d^-1 (d1～14) in a 21day cycle of therapy for 2－6 cycles. ResultsThirtyfour patients were assessable for efficacy and toxicity. One patient achieved a complete response and 24 patients had partial responses, with an overall response rate of 69.5 %.The median TTP for all was 9 months(range 2-17 months).The median overall survival was 16 months(range 2-38 months). The most common adverse effects were myelosuppression and gastrointestinal response. There was no chemotherapyrelated death. Conclusion The combination of capecitabine and oxaliplatin/paclitaxel is effective and well tolerated as firstline therapy for patients with advanced gastric cancer.
药物与临床
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  药物与临床

  Clinical Evaluation of Transdermal Fentanyl in Preventing the Pain after Portion Splenic Artery Embolism Operation

  LIU Zhong-min;FU Jia-ping;FENG Wei-ying

  2007, 26(1): 39-40.

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  Objective To evaluate the efficacy of transdermal fentanyl in postoperative analgesia after portion splenic artery embolism. Methods 43 cases of hematic disease received portion splenic artery embolism operation, 29 of them were treated by transdermal fentanyl 5 mg , 10-12 hours before the operation, and 14 cases of them were included in control group (retrospetive analysis). Therapeutic response and toxicity were studied. ResultsWith the use of transdermal fentanyl，9 cases (31.03%)had complete remission of pain, 16 cases(55.17%)had partial remission of pain, and 4 cases(13.8%)had no remission. The total gratification rate of analgesia was 86.2%,with a scale of VAS 1.93±1.77 in the treatment group and 6.43±2.90 in the control group. There was a very significant difference between the two groups (P<0.01). The toxicity was mild, some patients had nausea, vomiting, anorexia, constipation,etc., one case had enteroplegia and abdominal distension. ConclusionTransdermal fentanyl is an effective and convenient drug in postoperative analgesia after portion splenic artery embolism with slight sideeffects. It can be used as a usual drug before the treatment of portion splenic artery embolism．
药物制剂
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  药物制剂

  Research on Extract Technology of Huangqi Zhechong Decoction with Orthogonal Design Methods

  XI Zhi-xia;DANG Shuang-suo;WANG Mei-na;ZOU Jing

  2007, 26(1): 55-56.

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  Objective To seek out the optimum extract technology of huangqi zhechong decoction. Methods Three levels in each of three factors( amount of water, decoction frequency and duration of decoction) were selected with orthogonal design. The conteats of astragaloside Ⅳ and polysaccharides served as indexes. Results The optimum extracting conditions were as follows. The amount of water was twenty times that of the drug, the decoction frequency was two ,and the duration of decoction was two hours. Conclusion This method of optimum design can guarantee the quality of huangqi zhechong decoction.
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  药物制剂

  Preparation of Racecadotril Suspension and Preliminary Study on Its Stability

  SONG Tian;HE Zai-an;LIU Yan-wen

  2007, 26(1): 57-59.

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  Objective To prepare racecadotril suspension. Methods The suspending effects of the following hydrophilic polymers were investigated: HPMC, CMC-Na, PVP K90, Xanthan gum and MC. Two percent of HPMC appeared to be a satisfying suspending agent by evaluating the sedimentation rate and the redispersion of racecadotril. The stability of suspension was studied by detecting the rheology property, suspension viscosity, and microscopic morphology and the stability of particle morphology under accelerated experiment of drugs was also detected. ResultsThe obtained racecadotril suspension comformed with the quality standard. Conclusion The suspension meets the requirements of suspension preparation with stable quality
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  药物制剂

  Preparation of a Laminaran Liposomes and Its Quality Evaluation

  XU Yong-hua;YANG Ya-ling;PENG Hai-long;FAN Rui-mei

  2007, 26(1): 60-62.

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  Objective To prepare laminaran liposomes with its quality evaluation. Methods The liposomes were prepared by the reverse evaporating method, and the morphology of laminaran liposomes, the drug loading, the entrapment efficiency, the invitro release, the stability and the particle size distribution were studied. Results More than 35.00% of initial laminaran content were entrapped into laminaran liposomes, and the results of transmission electron micrograph showed that the Laminaran liposomes were evenly distributed small spherical or similar to spherical vesicles, with a mean diameter of 75 nm. The liposomes exhibit a better sustainedrelease effect than the commercial preparation. Conclusion Laminaran liposomes are consistent with the experimental design supposition, and provide reference for laminaran liposomes preparation.
药品质量控制
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  药品质量控制

  Direct Determination by FTIR Spectroscopy Combined with PCA for the Identification of Paeonia lactiflora Pall. and Their Confusable Varieties

  LI Bin-lan;CHENG Ze-feng;SHOU Wen-hong;CHENG Cun-gui

  2007, 26(1): 71-73.

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  Objective To identify Paeonia lactiflora Pall. and its confusable varieties by Fourier transform infrared(FTIR) spectroscopy assisted with OMNI sampler. Methods IR was obtained by FTIR Spectroscopy with direct mensuration , principal component analysis (PCA) was progressed by taking xylem as comparing standard, selecting thirtysix groups representative absorbency data as a basis, and taking samples as analysis objective. The degree of difference between Paeonia lactiflora Pall. and its confusable varieties was compared by principal factors analysis. Results Principal component analysis of FTIR Spectroscopy exhibited practical value on reflecting the degree of difference in chemical compositions among different species from the same genera. Conclusion This is a direct, quick and accurate method to obtain the sample FTIR atlas.
用药指南
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  用药指南

  Estimating Method of the Pharmacokinetic Parameters of Drug Obeying Parallel the First Order and MichaelisMenten Elimination

  SU Yin-fa;BAI Xue-min

  2007, 26(1): 78-80.

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  Objective To estimate the pharmacokinetic parameters of drug obeying parallel one order and Michaelis-Menten elimination with bolus intravenous administration. Methods Concentration-time data from the simulation by four order Runge-Kutta algorism were converted into ⊿C/⊿t. The differential dC/dt was replaced by ⊿C/⊿t,and concentration C was replaced by harmonious C_iC_i+1 or arithmetic mean(C_i+C_i+1)/2. ⊿C/⊿t with C_iC_i+1 or (C_i+C_i+1)/2 data were fitted by nonlinear regression in SPSS software. Results The pharmacokinetic parameters obtained from SPSS were exact and reliable. Conclusion SPSS is suitable for estimating the pharmacokinetic parameters of drug obeying parallel one order and MichaelisMenten elimination with bolus intravenous administration.