Archive

• 01 January 2012 Volume 31 Issue 1

    

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  药物研究
  肿瘤科用药专栏
  药物与临床
  药物制剂与药品质量控制
  用药指南
  药物不良反应
  

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药物研究
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  药物研究

  Experimental Research of Anluohuaxian Pill Plus Interferon-γ on Schistosomal Liver Fibrosis in Mice

  XIAO Fei;MA Ke;HUANG Hai-yan;AI Guo;JIAO Yun-tao;NING Qin;HUANG Jia-quan

  2012, 31(1): 1-4. https://doi.org/10.3870/yydb.2012.01.001

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  Objective To compare the effects of anluohuaxian pill plus interferon-γ against schistosomal liver fibrosis with anluohuaxian pill used alone.Methods Fifty Kunming mice were divided into 5 groups.Except 10 mice in the normal control, the other 40 were infected with 40 Schistosoma japonicum per mouse.Six weeks later, the model of schistosomal liver fibrosis was successfully induced, and the model mice were randomly divided into 4 groups evenly.① The model control mice were treated by intragastric administration of 0.75 mL normal saline at each time point;②In the anluohuaxian pill group, mice were i.g.treated with anluohuaxian pill mixed with normal saline at the same volume as above;③In the interferon-γ group, mice were hypodermically injected with 0.1 mL mixture of interferon-γ (2×106 U) and pyrogenfree water(4 mL);④In the twodrug combination group, mice were treated with halfandhalf anluohuaxian pill and interferon-γ one time per day for 8 weeks.By the end of therapy, the liver tissues were taken for pathological examination and expression of typeⅠ,Ⅲ collagen and TIMP-1(tissue inhibitor of metalloproteinases 1) was detected. Results The apparently diminished size of schistosomal egg nodules of the anluohuaxian pill group, the interferon-γ group,the two-drug group, the model control were (460.406 5±36.276 8),(443.927 6±44.209 5),(433.430 0±64.928 4),(533.765 8±88.102 2)μm,respectively. Compared with the model control, the hepatic injury was attenuated in all therapeutic groups with apparently diminished size of schistosomal egg nodules, P<0.05.Further, the expression of typeⅠ,Ⅲ collagen as well as TIMP-1 were all conspicuously reduced, especially in the two-drug combined group(P<0.05). Conclusion Combination of anluohuaxian pill with interferon-γ shows more effective on treating schistosomal liver fibrosis, which is possibly associated with inhibition of hepatic stellate cell activation and diminished expression of TIMP-1.
  
  
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  药物研究

  5-aza-2’-Deoxycytidine Induces Demethylation and Expression of CDH13 Gene in Human Lung Cancer Cell Lines

  LIAO Wan-min;WANG Dao-wen

  2012, 31(1): 5-8. https://doi.org/10.3870/yydb.2012.01.002

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  ObjectiveTo investigate the effects of 5-aza-2’-deoxycytidine (5-Aza-dC) on methylation state and expression of CDH13 gene in human lung cancer cell lines A549 and LTEP-a2, and elucidate its underlying mechanisms.Methods The methylation specific PCR(MSP) and RT-PCR was used to detect the changes of promoter methylation and mRNA expression of CDH13 gene in A549,LTEP-a2 and HFL1 cells before and after being incubated with DNA methyltransferase inhibitor 5-Aza-dC, respectively. Results The promoter of CDH13 gene methylation was not detected in normal lung cell lines, but in both A549 and LTEP-a2 cells.Treatment with 5-Aza-dC induced the demethylation of CpG islands in the promoter region.The mRNA expression of CDH13 gene was found in A549 and LTEP-a2 cells, but was weaker than that in normal cells.CDH13 mRNA expression was obviously enhanced in cancer cells treated with medicines. Conclusion Promoter abnormal methylation is a main cause of CDH13 gene inactivation in human lung cancer cell lines, which could be completely reversed by the demethylation agent 5-Aza-dC.
  
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  药物研究

  Preliminary Pharmacodynamic Study of Xingsu Zhike Syrup

  ZHANG Shi-yong;CHENG Jun;PENG Dai-yin;GAO Jia-rong

  2012, 31(1): 8-10. https://doi.org/10.3870/yydb.2012.01.003

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  ObjectiveTo study the expectorant, anti-tussive, anti-asthmatic and anti-inflammatory effects of xingsu zhike syrup.Methods Mice were divided into five groups at random, including normal control, kechuanning group(3.0 mL.kg^-1), and three groups received with low dose, middle dose and high dose of xingsu zhike syrup(1.5,3.0,6.0 mL.kg^-1), respectively．The rat model with cough by ammonia, mouse model for testing phenol red excretion, mouse model of histamine-acetylcholine induced asthma and that with celiac capillary permeation by acetic acid were created to explore effect of xingsu zhike syrup. Results Cough frequency within 2 minutes of the medium,low dose groups of xingsu zhike syrup,and blank control were(40.50±9.53),(36.73±10.40),(36.54±7.24),(28.07±4.83),(44.72±6.97)times, respectively.The latent period of cough induced was(24.56±10.83),(26.22±9.17),(26.92±8.69),(28.62±11.58),(18.49±5.56) s, respectively.The latent period of incubation induced was(64.8±17.9),(68.4±18.3),(75.8±20.7),(73.6±17.8),(49.8±15.4) s , respectively.The absorbency reflecting phenol red discharge was(0.096±0.025),(0.103±0.021),(0.110±0.035),(0.110±0.032),(0.083±0.022), respectively, that for capillary permeability was(0.107±0.034),(0.103±0.027),(0.090±0.024),(0.099±0.031),(0.121±0.037), respectively. Conclusion Xingsu zhike syrup has significant expectorant, anti-tussive, anti-asthmatic and anti-inflammatory effects.
  
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  药物研究

  Inhibitory Effects of Trichostatin A on Human Renal Carcinoma Cell Line GRC-1

  WANG Tao;LUO Hao;QIN Qian-bo

  2012, 31(1): 11-14. https://doi.org/10.3870/yydb.2012.01.004

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  ObjectiveTo investigate the influence of histone deacetylase inhibitor (trichostatin A, TSA) on the human renal cancer line GRC-1 and its mechanism.Methods The proliferating activity of GRC-1 by TSA was observed by MTT assay.The cell apoptosis and cell cycle distribution were detected with Flow cytometry.Western blot was used to assess the expression levels of apoptosis gene bcl-2 and cell cycle regulation gene p21. Results A dose dependent inhibition was remarkably confirmed in GRC-1 cells treated with TSA.As compared with that in the control group, apoptosis rate of GRC-1 cells in TSA group was increased obviously (P<0.05).The percentage of G0/G1 phase increased markedly, while the percentage of S phase decreased significantly by TSA (P<0.05).Furthermore, the expression level of bcl-2 protein in TSA group was significantly lower, while p21 protein was significantly higher than those in the control group (P<0.05).However, the expression level of p53 protein in TSA group shows no significant difference from that in the control group (P＞0.05). Conclusion The data demonstrate that TSA induce growth arrest by G0/G1 phase blocking, and apoptosis eliciting, the mechanism of which may occur through down-regulating the expression of apoptosis gene bcl-2 and upregulating cell cycle regulation gene p21.
  
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  药物研究

  Inhibition of Snail Polysaccharide on Human Hepatic Cancer Cell Line SMMC-7721

  LV Gang-fei

  2012, 31(1): 14-16. https://doi.org/10.3870/yydb.2012.01.005

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  ObjectiveTo study the suppressive effect of snail polysaccharide on human hepatocellular carcinoma cell line SMMC-7721.Methods Human hepatocellular carcinoma cells SMMC-7721 were co-cultured with different dose of snail polysaccharide for 24, 48 and 72 h, respectively.The multiplication restrain on hepatic cancer cells by snail polysaccharide was determined by MTT method;and the cell cycle was detected by using flow cytometry. Results The absorbent value of cells affected under different concentrations of snail polysaccharide after 24, 48 and 72 h showed significant difference compared with the control at corresponding periods, (P<0.05 or P<0.01 ) , and which presented time and dose related manner.The half inhibitory concentration (IC50) of snail polysaccharide on SMMC-7721 cell strain was 0.293, 0.032 and 0.011 mg.mL^-1, respectively.The result indicated that snail polysaccharide arrested SMMC-7721 the cell strain to G2/M by flow cytometry. Conclusion The snail polysaccharide inhibits proliferation of cell strain SMMC-7721.
  
肿瘤科用药专栏
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  肿瘤科用药专栏

  Clinical Observation of Treating 20 Elderly Patients with Advanced Colorectal Cancer in the Regimen of Cetuximab plus XELOX

  SUN Jie;JIANG Li-na;PAN Sai-ying

  2012, 31(1): 17-19. https://doi.org/10.3870/yydb.2012.01.006

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  ObjectiveTo evaluate the safety and efficacy of cetuximab combined with capecitabine plus oxaliplatin(XELOX) in treatment of elderly patients with advanced colorectal cancer(ACC) .Methods Fourty elderly patients histologically diagnosed as ACC were randomly divided into two groups, 20 in the trial group (cetuximab plus XELOX) and 20 in the control group(XELOX regimen) .Treatment was capecitabine 2 000 mg.(m²)^-1 (1 000 mg.(m²)^-1 orally twice a day on days 1-14 for 3 weeks, oxaliplatin 130 mg.(m²)^-1 intravenously (I.V.) on day 1 every 3 weeks, and cetuximab [initially 400 mg.(m²)^-1 I.V.(120 min) , subsequently 250 mg.(m²)^-1 (60 min)] .All patients were assessable for the efficacy and toxicity test. Results The overall response was 12 in the trial group and 7 in the control group, the disease control was 18 vs 14 ,and the median time to progression(TTP) was 7.7 months vs.5.4 months, there were statistically significant differences between two groups (P<0.05).The most frequent grade I/II treatmentrelated adverse events including diarrhea, nausea/vomiting, neurotoxicity, neutropenia and handfoot syndrome .Skin rash was observed in 55.0% of the patients in the trial group. Conclusion Cetuximab combined with XELOX regimen is effective, safe and well tolerated in treatment of elderly patients with ACC, and is worth for further study of ACC.
  
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  Effective Observation of Erlotinib for Recurrence/Progression in Patients with Nonsmall Cell Lung Cancer with Brain Metastases After Radiotherapy

  LIU Yong;ZHAO Jing;YU Shi-ying;XI Qing-song

  2012, 31(1): 20-23. https://doi.org/10.3870/yydb.2012.01.007

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  ObjectiveTo evaluate the antitumor efficacy and adverse reaction of erlotinib for recurrence/progression in patients with non-small cell lung cancer (NSCLC) with brain metastases after radiotherapy.Methods The clinical data of 37 NSCLC patients with previously irradiated and recurrent/progressive brain metastases was analyzed retrospectively.They were treated orally with erlotinib at 150 mg&#8226;d-1.The efficacy and adverse reaction were evaluated after 8 weeks’ treatment. Results Thirteen patients had EGFR gene exon 19/21 mutations and 24 patients with unknown EGFR mutational status.The overall disease control rate (DCR) for all patients with intracranial brain metastases was 56.7%, including 5 patients (13.5%) with partial response (PR) and 16 patients (43.3%) under stable disease (SD) condition.The PR and SD in the mutational group were 3 and 8 cases, those were 2 and 8 cases in the unspecified mutational group, respectively.As for systemic disease, DCR was 40.5% including PR in 3 patients (8.1%), SD in 12 ones (32.4%);The PR and SD in the mutational group were 2 and 7 cases, and which were 1 case and 5 cases in the unspecified mutational group, respectively.Erlotinib showed significantly more effective in the mutational group than that in the unspecified mutational group (P<0.05).The major adverse reactions were grade 1/2 fatigue 64.9%, skin rash and diarrhea with 43.2% and 21.6%, respectively.The incidence of rash was conspicuously higher in mutational group than that in the unspecified mutational group (P<0.05). Conclusion Erlotinib is effective and safe on treating NSCLC patients with previously irradiated, recurrent/progressive brain metastases, especially for those with EGFR mutations, which should be considered as a new therapeutic option.
  

药物与临床
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  药物与临床

  Effect of Lacidipine on Serum Homocysteine Level of Patients with Hypertention Complicated with Coronary Heart Disease

  WANG Ping

  2012, 31(1): 38-40. https://doi.org/10.3870/yydb.2012.01.014

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  ObjectiveTo investigate the effect of lacidipine on serum homocysteine level of patients with hypertention and coronary heart disease.Methods One hundred eightyfour eligible patients were randomly divided into treatment group(93 patients) and control group(91 patients).The patients in the treatment group were given with lacidipine 4 mg once a day and those in the control were treated with nifedpineines 10 mg twice a day.The duration of therapy was 3 month.The blood pressure and serum homocysteine level pre and posttreatment were measured. Results The serum Hcy level of treatment group was (17.3±5.1) μmol.L^-1 before treatment, and the control group was (16.9±4.8) μmol.L^-1;the three months later, which in the treatment group was (12.5±4.2) μmol.L^-1, in the control group was (14.6±4.4) μmol.L^-1, and the difference was remarkable(P<0.01). Lacidipine was better in decreasing the Hcy level than nifedpineines(P<0.01). Conclusion Comparing with other calcium antagonists, the effect of lacidipine on reduction serum homocysteine level in hypertensive patient with coronary heart disease is much better and is independent of hypertensionlowering, which may be one of the unique mechanisms of its anti-arteriosclerosis.
  
  
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  药物与临床

  Dexmedetomidine for Sedation During Low Epidural Anesthesia in 22 Elderly Patients

  LIAO Ming-feng;CHI Xiao-hui;DENG Yu-chun;ZHANG Xue;YANG Hui;LUO Ai-lin

  2012, 31(1): 40-42. https://doi.org/10.3870/yydb.2012.01.015

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  Objective To assess the security and optimal dosage of using dexmedetomidine for sedation during low epidural anesthesia in the elderly patients.Methods A total of 48 elderly patients undergoing transurethral resection prostate were randomly divided into two groups: dexmedetomidine group and control one, 24 patients in each group.All patients received low epidural anesthesia with 1.5% lidocaine.Infusion of dexmedetomidine started 10 minutes before operation at a loading dose of 0.5 μg.kg^-1 in the test group, with a reduction of 0.1 μg.kg^-1.h^-1 once to a maintenance dose of 0.2 μg.kg^-1.h^-1 for keeping the Richmond AgitationSedation Scale (RASS) to at level -2.Patients in the control received no sedative treatment.The sedation assessment, vital signs and postoperation complication were observed. Results Twentytwo patients in the dexmedetomidine group completed evaluation, and they were in a stable sedation state.Moreover, lower heart rate, more satisfaction and less shivering were observed (P<0.05).The optimal dose of dexmedetomidine for sedation during low epidural anesthesia in elderly patients was proposed at 0.2-0.3 μg.kg^-1.h^-1. Conclusion Loading 0.5 μg.kg^-1 dexmedetomidine followed by maintaining infusion at 0.2-0.3 μg.kg^-1.h^-1 could provide a good and stable sedative effect during low epidural anesthesia in elderly patients.
  
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

  Isolation,Purification,Determination of Relative Molecular Mass and Content in Polysaccharide from Aloe barbadensis Miller

  DANG Xiu-li;LIU Xue-ying;WANG Qing-wei;ZHANG Sheng-yong;Gai Shou-chang

  2012, 31(1): 67-70. https://doi.org/10.3870/yydb.2012.01.0.026

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  ObjectiveTo isolate and purify the polysaccharide from Aloe barbadensis, determine relative molecular mass, total sugar content and protein content of the purified fraction (PSA2).Methods To adopt the method of water lifts and the alcohol immerse to extract the rude polysaccharides from Aloe barbadensis Miller.Rude polysaccharide was deproteinized by repeated freezethaw method,purified by DEAE–cellulose 52 and Sephadex G-100 columns,and the purified polysaccharide was termed as PSA2.HPGPC was used to determined the molecular weight of PSA2, the contents of the total soluble sugar and protein of PSA2 were determined by the phenolsulfuric acid method and coomassie brilliant blue method, respectively. Results The HPGPC showed relative molecular mass of PSA2 was 8 457.4.The contents of total sugar and protein were 61.0% and 0.7%, respectively. Conclusion The extraction technology is simple and feasible, the HPGPC, phenolsulfuric acid and coomassie brilliant blue are precise and rapid.
  
  
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  药物制剂与药品质量控制

  Content Determination of Toddaline in Xiao’er Xiaoke Tablets by HPLC

  ZHAO Lei;LIU Jia-le;LI Yan;SUN Yan-tao;

  2012, 31(1): 70-72. https://doi.org/10.3870/yydb.2012.01.027

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  ObjectiveTo establish a HPLC method for determination of toddaline in xiao’er xiaoke bablets.Methods Zorbax SBC18(250 mm×4.6 mm,5 μm)was used.The mobile phase was acetonitrile 1% triethylamine (pH 3.0 adjusted by phosphoric acid)(22:78).The flow rate was 1.0 mL.min^-1 and detection wavelength was set at 269 nm. Results The linear range of gastrodin was 8.25-825.00 μg.mL^-1 (r ＝ 0.999 8).The average recovery was 96.80% (n＝6) (RSD＝1.11%). Conclusion This method is simple, accurate and reproductive,which can be used for the quality control of xiao’er xiaoke bablets.
  
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  药物制剂与药品质量控制

  Optimization of Screening Disintegrants for Azithromycin Dispersible Tablets

  ZONG Yong-bing;WAN Yuan-song;JIN Chun;QIN Yong;

  2012, 31(1): 72-74. https://doi.org/10.3870/yydb.2012.01.028

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  ObjectiveTo study impact of disintegrants on the uniformity of tablets’ disperse for improving the quality of azithromycin dispersible tablets.Methods Sodium carboxymethyl starch,crosslinked polyvinylpyrrolidone and other suitable ingredients were used to prepare the tablets. Results The sodium carboxymethyl starch and proper preparation significantly enhanced the quality of azithromycin dispersible tablets. Conclusion The preparation is reasonable and stable, which is evenly dispersed and well dissolved.
  
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  药物制剂与药品质量控制

  Content Determination of Muscone in Xiaojin Capsules by Gas Chromatography

  LU Min;HU Zhen-bo;WANG Ying-feng;XIANG Yang

  2012, 31(1): 75-76. https://doi.org/10.3870/yydb.2012.01.029

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  ObjectiveTo establish a method for content determination of muscone in xiaojin capsules.Methods AT.OV-1301 column (30 m×0.25 mm,0.25 μm) was applied, the initial temperature of oven was set at 200 ℃ for 10 minutes, then it was raised to 250 ℃ for 10 minutes at rate of 30 ℃ per minute.The temperature of injection port was 200 ℃.The detector was FID, which was at 280 ℃. Results The calibration curves were linear in the range of 46-736 ng for muscone(r=0.999 8).The average recovery was 100.10%(RSD＝1.61%). Conclusion The method is simple, rapid, accurate, which can be used for the quality control of xiaojin capsules.
  
  
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  药物制剂与药品质量控制

  Content Determination of Cobamamide in Cobamamide Gel

  WU Yan;LIU Yuan;ZHANG Fu-cheng;WANG Ming-lei

  2012, 31(1): 77-79. https://doi.org/10.3870/yydb.2012.01.030

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  ObjectiveTo establish a high performance liquid chromatography method for determining cobamamide in cobamamide gel.Methods A XBC18 Uitimate column(4.6 mm ×250 mm , 5 μm)was used;the mobile phase was consisted of 0.05 mol.L^-1 monobasic potassium phosphate buffer solution (adjusted to pH 3.2 with phosphoric acid):acetonitrile(83:17);loading volume was 10 μL;the flow rate was 1.0 mL.min^-1;and the UV detection wavelength was set at 260 nm. Results The linear range for cobamamide was 10-50 μg.mL^-1, r＝ 0.999 9.The average recovery was 99.49%,with a RSD as 0.60%(n＝9). Conclusion The method is specific and accurate, which is suitable for the content determination of cobamamide in the gel.
  
  
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  药物制剂与药品质量控制

  Research of Quality Standard for Jinju Xiaozhi Suppository

  CHEN Jin

  2012, 31(1): 79-81. https://doi.org/10.3870/yydb.2012.01.031

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  Objective To establish the quality standard for jinju xiaozhi suppository.Methods Radix et Rhizoma Rhei and Borneolum in jinju xiaozhi suppository were identified by TLC(thin layer chromatograph).Chlorogenic acid was determined by HPLC. Results The characteristic identification by TLC was distinct and highly specific.The Results of quantitative evaluation showed that chlorogenic acid had the linear range of 5.4-108.8 μg (r＝0.999 9,n＝6),and the average recovery was 99.03% (RSD＝1.61%,n＝6). Conclusion The method is reliable,accurate and specific, which is benefit for the quality control of jinju xiaozhi suppository.
  
  
用药指南
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  用药指南

  Meta-analysis of Cinepazide Maleate Injection for Treatment of Unstable Angina Pectoris

  QING Yu-fen;JI Hong-liang;LIU Yong-yong

  2012, 31(1): 93-96. https://doi.org/10.3870/yydb.2012.01.037

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  Objective To evaluate the efficacy of cinepazide maleate injection for treatment of unstable angina pectoris(UAP).Methods The national and international literatures related to random control clinical trials on cinepazide maleate injection for treating UAP were retrieved.The Jadad score was used to evaluate the quality.The data were statistically analyzed by Metaanalysis. Results It was showed that cinepazide maleate injection was better in reducing frequency of angina attacks and improving ischemic ECG than the control from seven studies by Metaanalysis. Conclusion It’s manifested that cinepazide maleate injection has certain curative effect on unstable angina pectoris and lower occurrence of adverse reaction by Meta-analysis, which needs further verifying by randomized control trial with strict design and large sample.
  
  
药物不良反应
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  药物不良反应

  Analysis of 121 Adverse Drug Reaction Reports

  TANG Jie;LIU Dong;JIANG Han-ying

  2012, 31(1): 110-113. https://doi.org/10.3870/yydb.2012.01.044

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  Objective To investigate the characteristics of adverse drug reactions(ADRs) in Tongji hospital, and know well ADR monitoring and assessment for avoiding risk of drug use in clinic.Methods ADR reports in our hospital from September 1, 2008 to August 31, 2010 were downloaded from the national and municipal ADR monitoring network.The related data were converted and analyzed statistically. Results Among the 121 ADR cases of medication, antimicrobial agents ranked firstly and followed by the antitumor agents and drugs on circulation system.The main ADRs involved systemic disorders, skin and its appendage damages, and digestive system disorders.Ninety ADR cases(74.4%) were induced by intravenous drip.There were 19 new and serious ADR reports, which related to 16 kinds of medicines. Conclusion It should be paid more attention to establishing highlevel ADR monitoring system, carrying out the analysis, tracking high risk medicines, expanding safe research and promulgating precaution to deminish the drug risk.