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2009 Vol. 27, No. 5

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2009, 27(5): 321-323,344.
Abstract(1992) PDF (226KB)(589)
Abstract:
Inhibition research of three commonly-used anti-tumor drugs against HepG2 cell line
JIA Jing, LI Yue-yue, ZHU Zhen-yu, CHAI Yi-feng, ZHANG Guo-qing
2009, 27(5): 323-333,361.
Abstract(2327) PDF (578KB)(1413)
Abstract:
Objective :To establish an inhibition research method of three commonly-used anti-tumor drugs against HepG2 cell line. Methods : The determination was performed on a 96-well plate.The drugs were administrated in a series of concentrations,and each concentration was triplicate.Cells without drugs were set as a negative control.Followed by determination of MTT method,the inhibition ratio was plotted to concentration. Results :The inhibition ability of 3 drugs were different when the concentration were in different range.On the whole,the inhibition ability of 5-Fu was the weakest one. Conclusion :The method evaluates and compares the inhibition ability of 3 commonly-used anti-tumor drugs against HepG2 cell line,and could be a reference in positive control of drug screening experiment.
Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluoro-phenyl)-3-(N-isoproyl-N-substituted amino)-2-propanols
WEI Ning, ZHANG Song-wei, DAN Zhi-gang, CHAI Xiao-yun, YU Shi-chong, WU Qiu-ye
2009, 27(5): 324-327,392.
Abstract:
Objective :Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole. Methods : A isopropyl and substituted amino group were introduced and a series of title compounds were synthesized.All of them were confirmed by MS,1H-NMR,etal.The antifungal activities were also evaluated against the eight common pathogenic fungi. Results :Fifteen compounds were synthesized.All title compounds exhibited activity against fungi tested to some extent.Compounds(6c),(6d),(6e),(6f) and(6g) exhibited strong antifungal activities against eight test fungi comparable to the control drug itraconazole except Aspergillus fumigatus. Conclusion :A benzyl moiety with a group of shorter length substituted on 4-position is required for high activity.
Studies on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV
FENG Ji-lu, WU Guang, YU Jian-xin, LIU Jia, NIU Chun-juan, LI Ke
2009, 27(5): 328-331.
Abstract(2539) PDF (659KB)(564)
Abstract:
Objective :To study on synthesis and antiviral activities of 5-substituted pyrimidine acyclic nucleoside phosphonate compounds on HBV. Methods : Starting with substituted pyrimidine,we synthesized 8 firstly reported compounds 1a~1h.Preliminary pharmacological test was made on HBV. Results :TThe test results show the inhibitory rate of targeted compounds on HBsAg and HBeAg is normal,but 1d is higher than lamivudine. Conclusion :5-substituted pyrimidine acyclic nucleoside phosphonate compounds keep the normal activities on HBV and introduce long chain of chloroformate at N6 of pyrimidine shows better activity.
Therapeutical effects of Danhong for injection on myocardial infarction in dogs
WANG Ke-bing, ZOU Li-hua, ZHANG Zhi-qiang
2009, 27(5): 334-336,352.
Abstract(2382) PDF (356KB)(781)
Abstract:
Objective :To investigate the therapeutical effects of Danhong for injection on myocardial infarction model induced by coronary artery ligation in dogs. Methods : The models of myocardial infarction were produced by ligation of the left anterior descending coronary artery in the anaesthetized dogs.The extent of myocardial ischemia and infarction was determined by means of epicardial mapping and N-BT staining.The parameters of lactate dehydrogenase and creatine kinase were also determined in the serums of dogs. Results :Danhong for injection(2、6 and 12mg/kg) by the way of intravenous injection obviously reduced the extent of myocardial infarction and the myocardial ischemia level at a dose-dependent manner.Increase of ∑-ST and N-ST,and the range of myocardial infarction caused by ligating coronary artery in dogs were obviously reduced by Danhong for injection.The level of LDH and CK in the serum of dogs were also decreased by Danhong for injection.Conclusions:The results show that Danhong for injection has significant protective effects on myocardial infarction in dogs.
Studies on glycolic acid injection resulting in local necrosis of rat livers
LI Ying, YANG Qiu-xia, SUN Jing, ZHENG Wei-qiang, CHEN Jian-ming
2009, 27(5): 337-339,372.
Abstract(2403) PDF (385KB)(485)
Abstract:
Objective :To observe local necrosis of rat livers resulted from glycolic acid injection and compare necrosis effects resulted from glycolic acid injection and ethanol injection. Methods :After injections of a series of concentrations of glycolic acid and ethanol into rat livers,the mean diameters and the pathologic histology examinations of coagulation necrosis in rat livers were detected. Results :Necrosis occurred around the injection site of glycolic acid.The mean diameter of the necrotic area caused by 5%、10%、15%、20%、30%、40%and 50%glycolic acid was significantly larger than that caused by ethanol(P< 0.05),and pathohistology confirmed that the necrosis was more serious in the former group. Conclusion :Glycolic acid could cause local necrosis of liver,and might be used in clinical practices in the future as a substitute of ethanol for the treatment of liver cancer.
Synergistic protective effect of Fructus Schisandrae chinensis with Astragalus polysaccharides on paracetamol-induced acute liver injury in mice
YAN Fei, ZHANG Qiao-yan, ZHANG Hong, HAN Ting, JIAO Lei, QIN Lu-ping
2009, 27(5): 340-344.
Abstract:
Objective : To study the synergistic protective effect and mechanism of extracts from Fructus Schisandrae chinensis(EFS) with astragalus polysaccharides(APS) on paracetamol-induced liver injury in mice. Methods :Mice liver injury was induced by peritoneal injection paracetamol physiologic saline solution at a dose of 500 mg/kg.The activities of serum alanine aminotransferase(ALT) and asparate aminotransferase(AST),the contents of malondialdehyde(MDA) and glutathione(GSH) in the liver tissue,and the liver histopathological changes were observed to evaluate the effects of EFS,APS and their combination on liver injury. Results : The EFS(270 mg/kg) or APS(900 mg/kg) alone did not produce any effect on liver injury induced by paracetamol in mice.The combination of EFS at dose of 30、90 and 270 mg/kg respectively with APS at dose of 100、300 and 900 mg/kg significantly decreased the activities of ALT and AST in serum and MAD level in liver tissue(P<0.05 or P<0.01),increased the GSH content in liver tissue(P<0.05 or P<0.01),and improved liver histopathological changes.The coefficients drug interaction(CDI) of related parameters between EFS(270 mg/kg) and APS(900 mg/kg) were all less than 0.7. Conclusion :The combination of EFS and APS reduced the ALT and AST level in serum,improved the liver histopathological changes of liver injury mice through synergistically increasing GSH content and antioxidant ability of liver.
Optimized preparation of oridonin-loaded nanoparticles by central composite design and response surface method
XU Jie, WANG Ju, FENG Nian-ping, ZHAO Ji-hui, YU Yan-yan, TAN Rong
2009, 27(5): 345-348,369.
Abstract:
Objective : To optimize the formulation of oridonin-loaded PLA nanoparticles with modified spontaneous emulsification solvent diffusion method. Methods :Applying central composite design and response surface method,choose the concentration of drug in organic phase,the concentration of PLA in organic phase and the ratio of water phase to organic phase as the influence factors.The evaluation parameters included entrapment efficiency,drug loading rate and particle size.Experiments were done on the theory of central composite design.The data were simulated using multi-linear equation and second-order polynomial equation.The possibly optimal formulation was predicted by response surface method. Results : TThe range of the optimal conditions were the concentration of drug in organic phase 0.5~0.8 mg/mL,the concentration of PLA in organic phase 1.6~2.6 mg/mL,the ratio of water phase to organic phase 1~1.5 According to the optimal conditions,the mean particle size,entrapment efficiency and drug loading rate were 98.5 nm,(28.86 ±0.93) % and(8.23 ±0.35) %,respectively. Conclusion :The central composite design and response surface method are useful for the optimization of preparing oridonin-loaded PLA nanoparticles.The established model could predict the parameter of the formulations exactly and properly.
Research on constituents of Radix Aconiti and its processing by electrospray ionization trap mass spectrometry
DONG Xin, LIU Min, ZHAO Jing-xia, ZHANG Wei, LOU Zi-yang
2009, 27(5): 349-352.
Abstract(2202) PDF (607KB)(974)
Abstract:
Objective : To reveal the processing principleg of preparation of Radix Aconiti by electrospray ionization trap mass spectrometry. Methods : The three reference standars were made MSn analysis and elucidating the fragmentation pathways.The rapid analysis by HPLC-ESI-MS had been used for identification of contituents in Radix Aconiti. Results :The comparison of mass spectra and liquid chromatographic information revealed the differences of Radix Aconiti and its process product. Conclusion : It is necessary to make quality control of process product of traditional Chinese herbal medicines by HPLC-ESI-MS.
Effects of 20 Chinese patent medicines on the catalytic activities of five main cytochrome P450s of human liver microsome
XU Bin, ZHAO Gang, WEI Hua, QIAN Xiao-feng, LI Jing-xian, XU Wen
2009, 27(5): 353-356.
Abstract(2130) PDF (782KB)(905)
Abstract:
Objective :The effects of the 20 Chinese Patent Medicines on the catalytic activities of five main drug metabolism enzymes of human liver microsome,CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP 3A4,were assessed. Methods : Human liver microsome incubation experiment was carried out to assay the injection on the catalytic activities of the enzymes.Phenacetin,tolbutamide,S-mephenytoin,dextromethorphane and midazolam were used as the substrates of the enzymes.After the incubation,the five metabolites of the substrates were quantified by HPLC-MS/MS method.The inhibition was calculated by comparing the formation velocities of metabolites with or without test drug. Results : Liu Shen Pill showed obvious inhibitory effect on CYP1A2 with an IC50 of 28.75 μg/mL;Gan Su Granule showed obvious inhibitory effect on CYP2C19 with an IC50 of 29.80 μg/mL;Dan Shen Tablet showed obvious inhibitory effect on CYP1A2 with an IC50 of 48.55 μg/mL;Bei Ling Capsule showed obvious inhibitory effect on CYP1A2 with an IC50 of 17.45 μg/mL;Xia Tian Wu Compound Tablet showed obvious inhibitory effect on CYP2D6 with an IC50 of 40.26 μg/mL;Tanshinone Capsule showed obvious inhibitory effects on CYP1A2,CYP2C9,CYP2C19,CYP2D6 and CYP3A4 with IC50s of 7.04,13.97,55.77,33.90 and 34.57 μg/mL.Tong Feng Ding Capsule showed obvious inhibitory effect on CYP2D6 with an IC50 of 37.56 μg/mL. Conclusion :Most test drugs showed obvious inhibitory effect on the catalytic activities of drug metabolism enzymes.The result indicated that Chinese Patent Medicine had the potential to induce drug-drug interactions and special attention should be paid when they are used in combined with other drugs.
Studies on cefazolin sodium pentahydrate in the treatment of COPD
XU Li, LI Chun-long, FANG fei-bo
2009, 27(5): 357-358.
Abstract(2405) PDF (163KB)(545)
Abstract:
Objective :To evaluate the efficacy and safety of cefazolin sodium pentahydrate in the treatment of acute stage of COPD. Methods : A randomized,controlled clinical trail was carried.A total of 65 patients of COPD were randomly divided into three groups(trial:25 cases,controlⅠ21 cases,controlⅡ19 cases),were administered intravenously at a dose of 2 g,bid,for 7 to 14 days. Results :At the end of the treatment,the cure rate and effective rate of three group were 80.00%(trial),71.43%(controlⅠ),47.37%(controlⅡ) amd 92.00%(trial),85.71%(controlⅠ),63.16%(controlⅡ) respectively.The incidence of adverse drug reaction were 4.00%,4.76%,5.26% respectively. Conclusion : The cefazolin sodium pentahydrate had an excellent clinical efficacy and good safety in treating patients with CODP.
Determination of illegal ingredient diclofenacpotassium in TCM by capillary electrophoresis
LIU Min, GU Zhuo-liang, ZHANG Xiao-dan, ZHOU Guo-hua
2009, 27(5): 359-361.
Abstract(3190) PDF (506KB)(673)
Abstract:
Objective :To establish a capillary electrophoresis(CE) method for determining the illegally added ingredient diclofenac potassium in TCM,Shuguning tablet. Methods : CE was used for the separation by using the uncoaded capillary(75 μm×50 cm) and buffer of 25 mmol/L Na2HPO4(pH 6.50±0.02).The applied voltage was 25 kV at 25℃.The sample was injected for 5s at 0.5psi and the detection wavelength was at 275 nm. Results :Linear range was from 0.010 g/L to 0.200 g/L(r=0.998 4),the average recovery was 100.6% with the RSD of 4.39%. Conclusion : This method is simple,rapid,reliable and accurate for quantifying the illegally added diclofenac potassium in Shuguning tablets.
Analysis of the essential oil from fresh leaves of Artemisia argyi cultivated in Shanghai by GC-MS
MENG Hui, XU Yong
2009, 27(5): 362-364.
Abstract(2277) PDF (574KB)(465)
Abstract:
Objective :To analyze the chemical constituents of essential oil extracted from fresh leaves of Artemisia argyi cultivated in Shanghai,so that to provide valuable information for use of fresh leaves of Artemisia argyi. Methods : Hydrodistillation was employed to prepare essential oil from fresh leaves of Artemisia argyi cultivated in Shanghai,and GC-MS was used to analyze the constituents of the essential oil. Results :Fresh leaves of Artemisia argyi contains rich essential oil,and sixty-eight compounds were identified,the main constituents are D-germacrene,cineole,caryophyllenene and thujone. Conclusion :Essential oil from fresh leaves of Artemisia argyi have different chemical composition compared with the dried medicinal material.The main constituents are D-germacrene,cineole,caryophyllenene and thujone,and of which thujone is the richest.This is should be considered when use the fresh leaves of Artemisia argyi.
Determination of residual solvents in gatifloxacin by headspace capillary gas chromatography
CAI Lin, YAN Ju-jiao, LI Heng
2009, 27(5): 365-366,387.
Abstract(2180) PDF (212KB)(711)
Abstract:
Objective :To establish a method for determination of five residual solvents in gatifloxacin. Methods : The residual organic solvents which are ethanol,acetonitrile,dichloromethane,ethyl acetate,toluene were quantitatively determined by headspace GC on DM-624 column,90%DMF as solvent media,with FID detector,high purity nitrogen as the carrier gas. Results : Five residual solvents were completely separated.There was a good linearity(r=0.999 7~0.999 9).The detection limit of ethanol,acetonitrile,Dichloromethane,ethyl acetate,toluene were all less than 3μg/g;the RSD of precision was less than 5%;the average recovery rate of the preparation was in the range of 94.8%~98.6%. Conclusion :The method is simple,rapid,sensitive and can be used for the quality control of gatifloxacin.
Studies on preparation and skin penetration in vitro of cetirizine hydrochloride gel
GAO Xiang, ZHANG Chen-Xi, YANG Ming, LIU Ji-Yong
2009, 27(5): 367-369.
Abstract(2678) PDF (504KB)(577)
Abstract:
Objective :To prepare cetirizine hydrochloride gel and study its skin penetration in vitro. Methods : Cetirizine gel was prepared with carbopol 940 as base material.Using Franz diffusion cell and excised rat skin in vitro as transdermal barrier.The cumulative permeation quantity of cetirizine was determined by HPLC. Results :The penetration equation of cetirizine gel was Q=110.03t+17.17(r=0.99). Conclusion :The penetration of cetirizine from the gel through the rat skin followed first-order kinetics.
Stability of Medilox electrolyzed oxidizing water and its disinfection effect on hand and on article surface
HUANG Tao-yang, ZHAO Shu-jin, WENG Yan-jun, DENG Zhao-hui
2009, 27(5): 370-372.
Abstract(2732) PDF (179KB)(689)
Abstract:
Objective :To assess the stability of electrolyzed oxidizing water and its disinfection effect on hand and on article surface. Methods : Electrolyzed oxidizing water was stored for 90 days under the room temperature and its effective chlorine content,pH value and redox potential(ORP) value were measured and disinfection effect on hands and article surface was tested. Results :Its chlorine content decreased by 36% and pH value by 17%,ORP value showed no significant changes.The average disinfection effect of the electrolyzed oxidizing water on hands and on article surface was over 90%. Conclusion :The quality of the water during 90 days storage meets the quality standards,and effective chlorine content during storage significantly decline,we suggests that the water should be stored in proper conditions and used before date of expiry.
Joint application of 2D barcode and RFID technology in medical logistics tracking system
LUAN Zhi-peng, KUAI Li-ping, SHU Li-xin, CHEN Shen-xin
2009, 27(5): 373-374,389.
Abstract(1959) PDF (436KB)(986)
Abstract:
Objective :To discuss ideas and practices of joint applying 2D barcode and RFID technology in medical logistics tracking system. Methods :Analysis the technology features of 2D barcode and RFID technology,with the features of medical logistics industries,and design joint applications of these technologies in medical logistics tracking system. Results : Joint application of 2D barcode and RFID technology is an economical and efficient option which can achieve the functions of pharmaceutical logistics tracking.But there are some problems,such as standard non-uniform and hardly be extended.
Safety of biomedicine and it's countermeasures
ZHANG Zhi-ran, DIAO Tian-xi, GAO Yun-hua
2009, 27(5): 375-377.
Abstract(2910) PDF (492KB)(363)
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Biomedical industry is a new emerging high-tech industry,coupled with risk factors,and more and more attentions have been taken on the safety of biomedicine.After the appearance of some safety issues,both the pharmaceutical industry and the public have begun to realize that the safety of biomedicine is very complex and it is different from traditional medicines.Various developed countries in the world are active in the research on biomedical safety.In this paper,the various security issues in biomedicine have been summarized,the response to the safety of the key biological drug has been discussed and some countermeasures on the safety of biomedicine in our country have been suggested.
2009, 27(5): 378-379,395.
Abstract(2043) PDF (148KB)(669)
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2009, 27(5): 380-381,400.
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2009, 27(5): 382-383.
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2009, 27(5): 384-385,394.
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2009, 27(5): 386-387.
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2009, 27(5): 388-389.
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2009, 27(5): 390-392.
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2009, 27(5): 393-393.
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2009, 27(5): 394-394.
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2009, 27(5): 395-395.
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2009, 27(5): 396-398.
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