Archive

• 01 August 2014 Volume 33 Issue 8

    

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  药物研究
  心血管系统用药专栏
  药物与临床
  药物制剂与药品质量控制
  

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药物研究
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  药物研究

  Acute Toxicity Test and Diuresis Effect of Esculentoside A

  CUI Nan-nan;MENG Xiang-long;MA Jun-nan;LI Kun;ZHANG Shuo-sheng

  2014, 33(8): 981-984. https://doi.org/10.3870/yydb.2014.08.001

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  ABSTRACT Objective To understand the intensity and characteristics of acute toxicity of esculentoside A on mice and measure relevant parameters and observe its diuresis effect on rat.Methods After intraperitoneal injection of different concentrations of esculentoside A to mice, toxic reactions were observed.Rats with water load were intraperitoneally injected with different doses of esculentoside A.Total urine volume in six consecutive hours after the injection was determined.Results The LD50 of esculentoside A calculated by Bliss method was 26.19 mg﹒kg-1, and the 95% confidence interval was 23.11-29.85 mg﹒kg-1.The mortality and acute toxicity of esculentoside A appeared to be dose-dependent while the blank control group had no abnormal reaction.The urine volume was significantly different between high dose group and the negative control group.No significant difference in urine volume was found between middle and the negative control group, and between low dose group and the negative control group.Conclusion Esculentoside A is poisonous to mice when single dose was intraperitoneally injected, and high dose of esculentoside A has diuresis effect on rat.
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  药物研究

  Content of Six Compounds in Urine and Feces After Intragastric Administration of Shegan Heji in Rat

  ANG Yue-nian;ZHANG Jian;LU Xiao-tong;CHEN Ting;WEI Xin;JING Liang;SUN Chao-rong;HU Song-hao;YANG Chuan-min;YAN Yun

  2014, 33(8): 985-987. https://doi.org/10.3870/yydb.2014.08.002

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  ABSTRACT Objective To study absorption of shegan heji marker components in blood and their excretion in urine and feces of rats, after intragastric administration of shegan heji.Methods LC-MS/MS was used for determination of marker compounds.Rat metabolic cage technology was employed.Results Excretion of marker components were completed 24 hours after administration.Conclusion Ephedrine can be excreted from rats within 24 hours.The possibility of mutual transformation of flavonoids exists in the body.Taking shegan heji will not cause accumulation of ephedrine and flavonoids in the body.

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  药物研究

  Anti-inflammatory Effect of Compound Cornu Cervi Degelatinatum on Collagen-induced Arthritis Model of Mice

  CHEN La-xia;WANG Yan-yan;SUN Wei-guang;XU Xin

  2014, 33(8): 988-991. https://doi.org/10.3870/yydb.2014.08.003

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  ABSTRACT Objective To investigate the effects of compound cornu cervi degelatinatum on the expression of related inflammatory cytokines and pathological changes of the synovium in mice with collagen-induced arthritis (CIA).Methods The CIA model of Balb/c mice was established.The mice were randomly divided into 5 groups: blank control group, model control group, low-dose group (C1), high-dose group (C2) and glucosidorum tripterygll totorum group D.After the first immunization in mice, we observed the general condition and lesions of the fore and hind jaws.After the second immunization, the mice in groups C1 and C2 were orally administered with compound cornu cervi degelatinatum at the doses of 2.5 and 5 g﹒kg-1 body weight per day for 4 weeks, and meanwhile those in group D were administrated with glucosidorum tripterygll totorum at the dose of 13.6 mg﹒kg-1 body weight per day.The serum of the mice was collected to detect the levels of TNF-α and IL-4 by ELISA.Ankle joints were harvested, and the pathological changes of synovial tissues were observed under light microscope.Results As compared with the model control group, the level of TNF-α in the treatment groups was significantly decreased, while the level of IL-4 was elevated in group C1.Histological pathology of ankle joints demonstrated that the synovium of the CIA mice were hyperplastic and the synovial tissues were markedly ameliorated in treatment groups.Conclusion The compound cornu cervi degelatinatum can relieve redness and swelling in mice with CIA.The mechanism may be related to the inhibition of pro-inflammatory cytokine TNF-α and regulation of anti-inflammatory cytokine IL-4.
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  药物研究

  Preparation of Monoclonal Antibody of Sodium Estrone Sulfate from Pregnant Mare’s Urine

  AMANGULI&#;Tuohongerbieke;FENG Xiao-hui;GONG Yue-hong;QI Xin-wei;AERZIGULI&#;Tuerxun;GAO Xiao-li

  2014, 33(8): 991-996. https://doi.org/10.3870/yydb.2014.08.004

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  ABSTRACT Objective To establish a method to prepare anti-sodium estrone sulfate monoclonal antibody (ESS-Mab).Methods Balb/c mice were immunized by ESS.Immune Methods were screened.The blood serum potencies were measured by indirect ELISA and the best consistence of antigen and the first antibody were confirmed with method of titration．Cell fusion was carried by using PEG method and McAb hybridoma was screened with the indirect ELISA.Results The best immunization method of mice was subcutaneously multi-point injection in mouse back with the dose of 200/100 μg ESS antigen five times.The fusion rate was 90.2%.Hybridoma positive rate of ELISA screening was 4.4%.Finally two cell lines 2C8 and 8A7 with good specificity and sensitivity were obtained.Conclusion The best immunization way is selected and indirect ELISA is set up effectively and reliably for screening and presenting ESS McAb.the hybridoma technique is able to prepare monoclonal antibody of anti-ESS successfully.
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  药物研究

  Influence of Dexamethasone on IL-25 and IFN-γ in Bronchoalveolar Lavage Fluid of Asthmatic Mice

  LU Wei;WANG Lei;QIAO Ming;WANG Yu;JIANG Ji-fu;WU Zhong-ming

  2014, 33(8): 997-1000. https://doi.org/10.3870/yydb.2014.08.005

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  ABSTRACT Objective To investigate the mechanism of therapeutic action of dexamethasone on asthmatic mice by detecting the levels of IL-25 and IFN-γ in bronchoalveolar lavage fluid (BALF).Methods Balb/c mice with SPF grade were randomly divided into normal control group, asthma group and dexamethasone group.Asthma group and dexamethasone group were sensitized and challenged with ovalbumin (OVA).Dexamethasone group was intraperitoneally injected with dexamethasone one hour before challenging.The mice were executed 24 hours after the last challenge, and the HE stained pathological sections of the right lung were made.Pathological sections of lung were observed.BALF in the left lung was also collected.The total white blood cell count and absolute eosinophile (EOS) count were observed, and the percentage of EOS was calculated.The levels of IL-25 and IFN-γ were measured with ELISA, and correlation analyses were made.Results The counts of total white blood cell and EOS, and the percentage of EOS were significantly higher in the asthma group than in the normal control group and dexamethasone group (P＜0.05).No differences were found between the normal control group and dexamethasone group.The IL-25 level was higher in the asthma group than in the normal control group and dexamethasone group (P＜0.05), and its level in the dexamethasone group was also higher than that in the normal control group.The IFN-γ level was lower in the asthma group than in the normal control group and dexamethasone group (P＜0.05), while there was no significant difference between the normal control group and dexamethasone group.IL-25 was negatively correlated with IFN-γ in each group.Conclusion Part of the mechanisms of dexamethasone acting on asthma are related to its inhibition on the pulmonary inflammation and promotion on the expression of IFN-γ, and possible inhibition of IL-25 expression.
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  药物研究

  Effect of Shuanghuanglian Combined with Levofloxacin on Antibiotic Resistance of Staphylococcus Aureus ATCC29213 in Rabbit Tissue Cage Infection Model

  WANG Guo-jun;YE Yun;FENG Bi-min;LI Hong

  2014, 33(8): 1001-1004. https://doi.org/10.3870/yydb.2014.08.006

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  ABSTRACT Objective To explore effects of shuanghuanglian combined with levofloxacin on antibiotic resistance of Staphylococcus Aureus ATCC29213 to levofloxacin.Methods Tissue cage infection model with Staphylococcus aureus was established in rabbits, and the infected animals were given with levofloxacin alone (group A) or in combination with shuanghuanglian (group B) for 5 days respectively.Steady-state concentration of levofloxacin in tissue cage, bacteria recovery and bacterial resistance in tissue cage infection model were studied.Results Steady-state concentration of levofloxacin in tissue cage was not significantly different between group A and group B.The recovery rate of bacteria was significantly lower in group B than in group A (20.0% vs.100.0%).The minimum inhibitory concentration (MIC) was lower in group B than in group A.Conclusion Shuanghuanglian combined with levofloxacin is helpful to reduce antibiotic resistance of Staphylococcus aureus to levofloxacin,indicating that some Chinese traditional medicine combined with antibiotics can reduce antibiotic resistance.
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  药物研究

  Effect and Underlying Mechanism of Nocodazole on Inhibition of Rat Vascular Smooth Muscle Cell Proliferation

  LI Dan;GUO Xiao-mei

  2014, 33(8): 1004-1008. https://doi.org/10.3870/yydb.2014.08.007

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  ABSTRACT Objective To investigate the effect and underlying mechanism of nocodazole on the inhibition of rVSMCs proliferation.Methods rVSMCs were divided into four groups, group A (normal culture), group B (serum-free culture for 24 h), group C (18 h normal culture after 48 h of serum-free culture), and group D (nocodazole treatment for 12 h after thymidine treatment for 12 h). Flow cytometry, transmission electron microscopy, and metabolism measurements were performed and mitofusin-2(Mfn-2)expression was detected.Results Flow cytometry analysis showed rVSMCs of group B,C,D were arrested to G0/G1, S and G2/M phases, respectively. Less and smaller mitochondria were observed in group D by transmission electron microscopy in nocodazole-treated rVSMCs. Compared with groups A and C, there were significant decreases in glucose and L-amino acid metabolism, levels of ATP, and marked increase in NADH in group D(P＜0.05). Western Blot showed that G2/M cell cycle arrest and nocodazole could induce up-regulation of Mfn-2 in rVSMCs(P＜0.05).Conclusion Nocodazole can block the energy metabolism and proliferation in rVSMCs, which is probably associated with the role of Mfn-2 on anti-atherosclerosis.
心血管系统用药专栏
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  心血管系统用药专栏

  Determination of Landiolol Concentration in Human Blood by LC-MS/MS

  YU Yun-li;ZHANG Quan-ying;HUA Wen-yan;HUANG Ming;WANG Meng

  2014, 33(8): 1009-1012. https://doi.org/10.3870/yydb.2014.08.008

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  ABSTRACT Objective To establish an LC-MS/MS method for the detection of landiolol concentration in human blood.Methods After pretreatment with neostigmine and a deproteinization procedure,landiolol and the internal standard venlafaxine were eluted isocratically using a mobile phase consisting of acetonitrile and 10 mmoL﹒L-1 ammonium acetate with 0.1% formic acid in a ratio of 36:64 (V/V).Separation of the respective compounds was achieved on a Waters XTerra RP18 column (150 mm×4.6 mm,5 μm).Quantitative analysis of landiolol was conducted by a triple-quadrupole mass spectrometer with positive-electrospray ionization source,monitored under a multiple reaction monitoring (MRM) mode.The extracted ions monitored following MRM transitions were m/z 510.5→423.1 for landiolol and m/z 278.2→215.1 for the internal standard venlafaxine.Results The calibration curve of landiolol in human blood showed good linear relationship in the range of 1.010-2 020 μg﹒L-1.The lower limit of quantitation was 1.010 μg﹒L-1.The RSD of within-day and between-day precision was less than 6.5% and 4.8%,respectively.The recovery rate was 92.6%-100.9%.Conclusion The method is proven to be simple,rapid and reliable,and can be applied to study the pharmacokinetics of landiolol hydrochloride in healthy Chinese volunteers.

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  心血管系统用药专栏

  Effects and Mechanism of Atherosclerosis Prevention by DMARDs in Patients with Rheumatoid Arthritis

  RAO Li;CUI Liu-fu

  2014, 33(8): 1012-1017. https://doi.org/10.3870/yydb.2014.08.009

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  ABSTRACT Objective To investigate the effect of DMARDs on the prevention of early-onset atherosclerosis in rheumatoid arthritis (RA) patients for exploring an appropriate schedule to reduce cardiovascular events.Methods Seventy-two patients with early RA were included in this study.Erythrocyte sedimentation rate (ESR) and high sensitivity C reactive protein (hs-CRP) were detected before and after treatment to evaluate inflammation.Carotid intima-media thickness (cIMT) and endothelium-dependent flow-mediated vasodilatation (ED-FMD) were monitored.Disease Activity Score in 28 Joints (DAS28) and health assessment questionnaire-disability index (HAQ-DI) was used to assess severity degree of RA and life quality of the patients, respectively.The patients were treated with methotrexate (MTX), hydroxychloroquine (HCQ) and sulfasalazine (SSZ) alone or combined based on severity of RA.Results After 1 year of treatment, ESR, hs-CRP, DAS28 and HAQ-DI were significantly improved (all P＜0.01).At the same time, the serum lipid levels also had obvious changes.However, there was no obvious difference in body mass index (BMI) after 1 year.The cIMT ratio value was significantly decreased compared to baseline (0.43±0.08 mm vs.0.50±0.16 mm, P＝0.002), and FMD% also significantly improved from basic value of 5.26 to 7.57 after treatment (P＝0.041).Conclusion Early intervention of RA by using DMARDs can effectively control the disease and slow the progression of atherosclerosis, but also reduce cardiovascular mortality.
药物与临床
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  药物与临床

  Application of Small Dose of Dexmedetomidine Under the Guidance of Narcotrend During Combined Spinal-Epidural Anesthesia for Elderly Patients

  LU Zeng-ting;YANG Gang-hua;HE Qi-tao;MA Jun-yang;ZENG Li-rong;LIN Ai-ting

  2014, 33(8): 1035-1038. https://doi.org/10.3870/yydb.2014.08.014

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  ABSTRACT Objective To investigate the feasibility of Narcotrend-guided application of small dose of dexmedetomidine (DEX) for sedation during combined spinal-epidural anesthesia for elderly patients.Methods Fifty cases of ASA Ⅱ or Ⅲ elderly patients were randomly divided into treatment group and control group (25 patients of each group).After combined spinal-epidural anesthesia, both groups received continuous intravenous infusion of DEX, at 0.4 μg﹒kg-1 in 10 min, and then the rate was lowered to 0.4 μg﹒kg-1 per hour.For the treatment group, infusion rate was adjusted to reach a Narcotrend Index (NTI) of 75-85, and for the control group, infusion rate was adjusted to reach an OAA/S score of level 3-4.MAP, HR, RR, SpO2, NTI and OAA/S score were recorded at the beginning of DEX treatment (t0), 10 min (t1), 20 min (t2), 30 min (t3), and 60 min (t4) after the beginning of DEX treatment, and at the end of surgery (t5).The incidence rates of adverse events including bradycardia, hypotension, low oxygenation, and respiratory depression were also recorded.The patients were followed up until 24 h after surgery to record loss of memory about the surgical events.Results In comparison with t0, NTI and MAP of both groups significantly decreased at t1-t5 (P＜0.01).Comparison between the two groups showed no difference in MAP at each time point, and NTI of treatment group was higher than that of control group at t2-t5 (P＜0.05).In comparison with t0, OAA/S of both groups significantly decreased at t1-t5 (for t1, P＜0.05;for t2-t5, P＜0.01).Comparison between the two groups showed no difference in OAA/S at each time point (P＞0.05).Follow-up at 24 h after surgery observed total amnesia in 72.0% of DEX group patients and in 76.0% of the control group, without significant difference (P＞0.05).Conclusion Sedating elderly patients undergoing spinal-epidural anesthesia with DEX under the guidance of Narcotrend is safe and feasible, and the patients can be sedated properly.
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  药物与临床

  Clinical Application of Etomidate Combined with Remifentanil by Target Controlled Infusion Anesthesia During Painless Bronchofiberscopy

  LI Wei;LI Guo-ling;ZENG Wen-qiang;SHI Ming;CHENG Li

  2014, 33(8): 1039-1042. https://doi.org/10.3870/yydb.2014.08.015

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  ABSTRACT Objective To discuss the safety of using etomidate combined with remifentanil by target controlled infusion (TCI) for painless bronchofibroscopy.Methods Sixty patients were divided into two groups: painless bronchoscopy group (treatment group, 24 patients) and the routine bronchoscopy group (control group, 36 patients).Treatment group received TCI of remifentanil and intravenous injection of etomidate fat emulsion.Control group was subjected to surface anesthesia with 2% lidocaine.SpO2, blood pressure, heart rate and breath changes during examination and complete awakening were continuously monitored.Bronchofiberscopy time, body movement during examination, bucking and satisfaction degree after examination were also recorded.Results Treatment group patients felt senseless and painless during bronchoscopy, without memory of bronchoscopy and pain.Patients in control group had discomfort, body movement and acute bucking, and most of them had painful memory.There were significant differences between the two groups (P＜0.01).In treatment group, after examination, blood pressure, respiratory frequency, heart rate and SpO2 were significantly decreased (P＜0.01).During examination, the blood pressure, respiratory frequency and heart rate were increased, and SpO2 decreased in control group compared to the baseline (P＜0.01).There was no significant difference in SpO2 between treatment group and control group during examination (P＞0.05).Conclusion TCI etomidate combined with remifentanil during bronchoscopy achieved satisfying anesthetic effect.
药物制剂与药品质量控制
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  药物制剂与药品质量控制

  Formulation and Stability Studies on Paclitaxel Self-microemulsifying Drug Delivery System

  ZHOU Li-juan;CHEN Xi;LIU Qing-fei;WANG Yi-ming;LUO Guo-an

  2014, 33(8): 1063-1067. https://doi.org/10.3870/yydb.2014.08.023

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  ABSTRACT Objective To study the preparation and stability of paclitaxel self-microemulsifying drug delivery system (PTX-SMEDDS).Methods The formulation of the PTX-SMEDDS was optimized by monitoring the appearance, particle size, concentration, relative substance, and bacterial endotoxin.Influence of different pH and different dosage of activated carbon on PTX-SMEDDS was investigated.Subsequently it was subjected to stability studies.Results The PTX-SMEDDS was a translucent diluted-yellow solution with a mean diameter of 19.6 nm.High speed centrifugal test indicated PTX-SMEDDS was stable.The result of the influential factor tests showed PTX-SMEDDS was unstable to high temperature and light.In the accelerated tests for 6 months, the quality of PTX-SMEDDS was stable.The samples should be sealed and stored at low temperature and shady place.Conclusion Easily prepared and stable formulation of PTX-SMEDDS is achieved, and further investigation is warranted to develop self-microemulsifying drug delivery system for injection.
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  药物制剂与药品质量控制

  High Performance Liquid Chromatograph Fingerprint of Liqi Xiaoying Tablets

  HU Jun-jie;XIAO Yi;WANG Gui-hong;ZHENG Guo-hua

  2014, 33(8): 1067-1070. https://doi.org/10.3870/yydb.2014.08.024

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  ABSTRACT Objective To establish high performance liquid chromatograph (HPLC) fingerprint of liqi xiaoying tablets,and to provide reference for quality control of the herbal medication.Methods The chromatography conditions consisted of Aichrom Bond-AQ C18 (250 mm×4.6 mm,5 μm) column with mobile phase of acetonitrile-0.1% phosphoric acid (gradient elution), column temperature of 30 ℃,flow rate of 1 mL•min-1,injection volume of 20 μL,and UV detection wavelength of 226 nm.Results HPLC fingerprint was established with 13 common peaks,4 of which were identified.The similarity of the HPLC fingerprints of liqi xiaoying tablets from 10 batches was greater than 0.95.Conclusion The method is accurate, reliable, and can reflect complete information for the quality of liqi xiaoying tablets.
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  药物制剂与药品质量控制

  Determination of Content of Nutmeg Lignan and Dehydrodiisoeugenol in Nutmeg by HPLC

  LIU Huan;CHEN Jian-feng;WANG Jing;YUAN Zi-min

  2014, 33(8): 1070-1072. https://doi.org/10.3870/yydb.2014.08.025

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  ABSTRACT Objective To develope a high performance liquid chromatograph(HPLC)method for simultaneous determination of nutmeg lignan and dehydrodiisoeugenol before and after processing of nutmeg.Methods The column was Diamonsil C18 (250 mm× 4.6 mm, 5 μm).The mobile phase was methanol-water in a gradient elution mode.The UV detection wave length was 274 nm.The column temperature was 25 ℃ . The flow rate was 1.0 mL•min-1.Results Nutmeg lignan and dehydrodiisoeugenol had a good linear correlation in ranges of 10.24-61.44 μg•mL-1 (r＝0.999 6) and 3.0-18.0 μg•mL-1 (r＝0.999 8), respectively.The average recovery rates were 97.94% (RSD=2.17%) and 97.11% (RSD=2.17%).Conclusion The method is simple, accurate, reproducible, and can be used for the simultaneous determination of nutmeg lignan and dehydrodiisoeugenol before and after the processing of nutmeg.
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  药物制剂与药品质量控制

  Quality Analysis of Three Components in Shuanghuanglian Powder for Injection Before and After Ultrasonic Atomization

  HAN Fei;XIAO Xiong;WANG Qing;CHEN Shi-cheng;LUO Xiao-jian

  2014, 33(8): 1073-1076. https://doi.org/10.3870/yydb.2014.08.026

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  ABSTRACT Objective To establish a new RP-HPLC method for simultaneous determination of chlorogenic acid,forsythin, and baicalin in shuanghuanglian powder for injection after ultrasonic atomization.Methods Hypersil ODS2 C18 (250 mm×4.6 mm,5 μm) was used as the chromatographic column.The mobile phase was methanol-0.2% phosphate acid solution (40:60).Flow rate was 1.0 mL•min-1.Sample volume was 5 μL.Column temperature was 30 ℃.Detection wavelength was 324 nm at 0-10 min and 277 nm at 10-25 min.Results Contents of chlorogenic acid,forsythin, and baicalin had good linear relationship with the respective peak area (r≥0.999 7) within the scope of the sample volume.The RSD was ＜2% for precision, reproducibility, and stability.Recovery rate was 98.50%-101.12% (n=6).Conclusion The method is rapid, accurate and reproducible, with high resolution.It can determine the content of three kinds of components at the same time.The three components in shuanghuanglian powder for injection did not change significantly before and after ultrasonic atomization.
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  药物制剂与药品质量控制

  Influence of Climate and Geographical Environment on Quality of Desmodium Styracifolium Herba Harvested at Different Time

  WANG Hai-xia;LIN ping;ZHOU Weng-ting;JI Sheng-guo

  2014, 33(8): 1077-1079. https://doi.org/10.3870/yydb.2014.08.027

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  ABSTRACT Objective To study the influence of climate, geographical environment and harvesting time on contents of schaftoside in Desmodium styracifolium Herba.Methods Content of schaftoside in Desmodium styracifolium Herba was determined by using HPLC.ODS-C18 column (4.6 mm×250 mm,5 μm) was used, the mobile phase was methanol-water (32:68), the detection wavelength was 272 nm, the flow rate was 0.5 mL•min-1, and the column temperature was 35 ℃.Results The climate type, amount of precipitation, average temperature, duration of sunshine, geographical environment of different province had significant impacts on the content of schaftoside in Desmodium styracifolium Herba.Conclusion Subtropical monsoon climate, temperature from 25 ℃ to 32 ℃, sunshine time of 10 h per day and the average annual rainfall of 1 942 mm are suitable for growth of Desmodium styracifolium.The content of schaftoside in samples cultivated from Guangxi Province is higher than that cultivated from Guangdong Province and Hainan Province.The schaftoside content of sample cultivated in July is higher than that cultivated in other months.
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  药物制剂与药品质量控制

  Optimization of Extraction Technology for Total Saponins of Ardisia Crenata by Singlefactor Experiment Combined with Response Surface Methodology

  WU Qin;CHEN Xun

  2014, 33(8): 1080-1082. https://doi.org/10.3870/yydb.2014.08.028

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  ABSTRACT Objective To optimize the extraction process of Ardisia crenata based on the content of total saponins and to provide a basis for the Ardisia crenata study.Methods Based on the Results of the single-factor tests and the Box-Behnken central composite experimental design principles, a response surface methodology which has three factors and three levels was designed to optimize the extraction process of Ardisia crenata based on the content of saponins.Results A maximal extraction yield of total saponins reached 2.29% under the optimal conditions as follows: 70% alcohol was used as extraction solvent with the material to liquid ratio of 1:16, the extraction time was 3 h at 70 ℃.Conclusion The optimized extraction process is accurate, reliable and practically valuable.