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• 01 May 2012 Volume 31 Issue 5

    

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  特约稿
  药物研究
  药物与临床
  药物制剂与药品质量控制
  

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特约稿
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  特约稿

  The Bibliometrical Analysis on Papers Published on Herald of Medicine From 1991－2010

  ZHANG Shijing;LIU Haitong;LI Xiaotao

  2012, 31(5): 551-561.

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  ObjectiveTo acquire detailed knowledge of the development situation of Herald of Medicine in recent 20 years and provide a basis for making improvement of the periodical.MethodsBibliometric methods were adopted to collect subjects in the periodicals from 1991－2010 distribution research，areas，fund，author units，authors，cooperation situation，cited frequency and highfrequency keywords were analyzed.ResultsThere were 10 583 papers published on Herald of Medicine from 1991－2010，which involved with 15 794 authors.Who mainly came from provinces such as Hubei and Zhejiang. Most of funded papers were at the provincial level and in upward trend.ConclusionThe influence of Herald of Medicine has covered all over China，the quality and scholarship of the periodical continued to rise.Integrated measures should be implemented to promote further development of the periodical.
药物研究
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  药物研究

  Antioxidation of Tea Pigment in Vitro

  FU Li;HAN Guozhu;LI Nan;LIN Yuan;TANG Zeyao

  2012, 31(5): 562-564.

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  ObjectiveTo study the antioxidation of tea pigment (TP) in vitro.MethodsThe antioxidation and comparation of TP with VitC as positive control were tested by autooxidation of pyrogallic acid and antihydroxide radical assay in vitro.ResultsThe average inhibition rate per minute of TP at the dose of 0.1%，0.2%，0.3% was 7.022%，13.427%，16.910%，respectively.Whereas，the average inhibition rate per minute of VitC at 0.1%，0.2% was 16.340%，32.850%，respectively.Both TP and VitC inhibited autoxidation of pyrogallol in a dose dependent manner.Moreover，the average suppression rate of TP at 0.1%，0.3%，0.5%，0.7%，1.0% on hydroxy radical（•OH） produced in vitro was（11.00±0.70）%，（20.68±0.60）%，（27.04±0.07）%，（32.70±0.30）%（42.90±0.70）%，respectively，while it was（4.50±0.30）%，（7.40±1.00）%，（11.42±0.23）%，（14.80±0.40）%，（16.80±0.60）% for VitC at different doses，respectively.TP and VitC hindered the generation of hydroxy radical（•OH） dose dependently，especially for TP.There was significant difference between VitC and TP at the same dose（P＜0.01），and betweeen TP at different doses（P＜0.05）.ConclusionTP has an antioxidant effect in vitro，especially on hydroxyl elimination.
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  药物研究

  Determination of Ketoconazole in Skin Penetration Solution by HPLC

  SU Biya;LI Guofeng;LIU Sijia;XIONG Luqi

  2012, 31(5): 565-567.

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  ObjectiveTo establish a method for determination of ketoconazole in skin penetration solution prepared by the Franz experiment with HPLC，providing evidence for pharmacokinetics study of ketoconazole via posttransdermal administration.MethodsHPLC was performed on ECOSIL C18 column（250 mm×4.6 mm，5 μm） at 35 ℃，and the mobile phase was composed of methanol0.02 mol•L－1 KH2PO4 solution（70：30）（pH value being adjusted to 6.8 with 0.1 mol•L－1 NaOH solution ）.The flow rate was 1.0 mL•min－1，and the detection wavelength was 235 nm.ResultsThe linear range of ketoconazole was within 0.05－25.00 μg•mL－1（r＝0.999 3）.The average recovery of the solution at high，middle，and low concentration was 98.109% with RSD as 2.956%，repectively，and both of the intraday and interday precision were＜3.30%.ConclusionThe method is rapid and simple，and can be used for the quality control of ketoconazole cream and research on percutaneous of absorption ketoconazole.
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  药物研究

  Effects of Inositol Triphosphate and Tetramethylpyrazine on Accumulation of Adriamycin in BEL7402/ADM Cells

  DENG Wei;WANG Shanshan;ZHANG Qiufang;LIU Ming;WANG Xianlan;LI Hongliang;WU Hongling;TAN Yan;WANG Xuanbin;

  2012, 31(5): 568-571.

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  ObjectiveTo investigate the effects of inositol triphosphate and tetramethylpyrazine on the accumulation of adriamycin in BEL7402/ADM cells and the potential role of calcium involved.MethodsBEL7402/ADM cells were divided into four groups: blank group，inositol triphosphate（IP3） group，tetramethylpyrazine（TMP） group and verapamil（VRP） group.MTT was used to detect inhibition of cell proliferation， and 50% inhibiting concentration value（IC50） was calculated.The intensity of adriamycin accumulation in the cells was observed by fluorescence microscope.Results①IC50 value of the cells treated with TMP，VRP and IP3 was（65.35±0.24）%，（64.89±0.18）% and（337.60±0.12）%（all P＜0.05） of that in the blank group，respectively.②The fluorescence intensity of the cells treated with TMP or VRP was significantly higher than the blank group，while that of the cells treated with IP3 was significantly lower than the blank group.ConclusionIP3 reduces the accumulation of adriamycin in BEL7402/ADM cells and increases the IC50 of adriamycin，while TMP presents the opposite effect，which suggesting that IP3 could activate Pgp by increasing intracellular calcium, but TMP reverses this process.
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  药物研究

  Effect of Coptis Extracts on Apoptosis of HaCat Cell Line

  PENG Xiaoming;HUO Shixia;GAO Li;LI Zhijian;KAISAIER&#;Abudukeremu;YAN Ming

  2012, 31(5): 571-574.

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  ObjectiveTo investigate the effect of coptis extracts on apoptosis and transcription level of NFκB in HaCat cell line.MethodsThe proliferation of HaCat cells was detected with MTT method after being cultured with different doses of coptis extracts（41.6，20.8，10.4 μg•mL－1）.Apoptosis was assayed by the DNA ladder.The absorbance was measured by semiquantitative RTPCR，and NFκB was analyzed by calculating NFκB /GAPDH.ResultsCoptis extracts inhibited the proliferation in a dosedependant manner，especially for the dose of 41.6 μg•mL－1 with inhibition rate as 66.17%.The scalariform DNA appeared in the cells by coptis extracts，which characterizing as apoptosis.In addition，the coptis extracts at the dose of 41.6 and 20.8 μg•mL－1 significantly reduced the transcription level of NFκB.ConclusionThe coptis extracts could induce HaCat cells apoptosis and downregulate the transcription level of NFκB.
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  药物研究

  Antiinflammatory Effects of Compound Chushi Lotion

  ZHANG Xiaopeng;WANG Yanyan;LIU Hongbing;TAN Nala;

  2012, 31(5): 575-578.

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  ObjectiveTo investigate the antiinflammatory effects and possible mechanisms of compound chushi lotion.MethodsThe antiinflammatory effects of compound chushi lotion were studied on the mice models of ear flaps swollen induced by dimethylbenzene and toes swollen induced by carrageenan，via weighing both earlaps and toes of mice and detecting prostaglandin E2 in the swollen toes with ultraviolet spectrophotometer.ResultsThe weight difference between left and right earlaps in the lowdose group［FL，(0.009 3±0.003 6） g］ of compound chushi lotion，middledose group［FM，（0.011 8±0.003 1） g］，and positive control［C，（0.012 1±0.003 4） g］ was less obvious than that of the model control［M，（0.015 5±0.002 9） g］（P＜0.01 or P＜0.05）.The mass difference between left toes and right ones of FL、FM and FH groups was （0.026 0±0.011 0），（0.024 4±0.013 8），（0.015 6±0.007 5） gram，respectively，which was slighter than that in the model group［（0.039 5±0.019 5），P＜0.01 or P＜0.05］.The prostaglandin E2（absorbance/gram） in swollen toes of these groups was（0.494 0±0.044 5），（0.509 1±0.036 7） and （0.491 0±0.076 6），respectively，which was lower than the model group［（0.575 7±0.069 7），P＜0.01or P＜0.05］.ConclusionCompound chushi lotion has antiinflammatory effect，the mechanism of which is possibly associated with inhibition of prostaglandin E2.
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  药物研究

  Hemostatic Effect of Thrombin -Chitosan Sodium Loaded Alginate Microspheres

  WANG Qiang;LANG Yiyong;Li Zheng;DAI Hua

  2012, 31(5): 579-580.

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  ObjectiveTo investigate the hemostatic effect of alginate microspheres with thrombinchitosan sodium.MethodsThe hemostatic microspheres were prepared by emulsioncrosslinking method，with chitosan sodium and alginate as excipients，thrombin as model drug.The models of trauma caused femoral artery bleeding in rats，blood oozing from the back of rats and bleeding from broken tails of mice were created，the model animals were treated with thrombin microspheres and compared with Yunnan Baiyao and tampons.The hemostatic time and bleeding volume were recorded to assess the hemostatic effect of thrombin microspheres.ResultsThe thrombin microspheres at a high，middle and low dose obviously shortened hemorrhage time（P＜0.01）and reduced bleeding volume（P＜0.05）of rat femoral artery.The hemostasis was enhanced with dose，but without conspicuous doseeffect relationship.The hemorrhage time（P＜0.01）of broken tails in mice was significantly curtailed by thrombin microspheres in a dosedependant manner.The hemorrhage time（P＜0.05）was obviously shortened and bleeding volume（P＜0.01）was lowered by thrombin microspheres at the high，middle and low dose，especially for the high dose.ConclusionThrombinchitosan sodium loaded alginate microspheres have obvious hemostasis effects.
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  药物研究

  Effects of Sevoflurane on Arrhythmia Induced by Myocardial Ischemia/reperfusion in Rabbits and Expression of NADPH Oxidase Subunit p22phox

  ZHANG Junfeng;ZHOU Wu;WANG Tao

  2012, 31(5): 581-583.

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  ObjectiveTo explore the effects of sevoflurane on arrhythmia induced by myocardial ischemia/reperfusion in rabbits and expression of NADPH oxidase subunit p22phox.MethodsThe model of myocardial ischemia/reperfusion was established in rabbits，and which were randomly divided into 3 groups: shamoperated group，ischemiareperfusion（I/R） group and sevofluranepretreatment group.The level of lipid peroxidate（LPO） was detected by spectrophotometry with thiobarbituric acid reaction products（TBARS）.The expression of NADPH oxidase subunit p22phox was assayed by western blotting.ResultsThe incidence of ventricular arrhythmias in the model group was 90%，with duration as ［（158.82±18.86）s］，both of which were markbly upregulated in comparison with the shamoperated group.The level of myocardial LPO in the model group was ［（2.12±0.36） μg•g－1］，which was significantly higher than that of the shamoperated group ［（0.89±0.11） μg•g－1，P＜0.01］.The expression of p22phox subunit was obviously upregulated.Compared with the model control，the incidence of ventricular arrhythmias（70%），duration［（39.65±5.27） s］，myocardial LPO ［（1.35±0.20） μg•g－1］ and p22phox expression in the sevofluranepretreatment group were significant downregulated.ConclusionSevoflurane could suppress arrhythmia induced by myocardial I/R in rabbits，the mechanism of which involved with downregulating p22phox expression and therefore dropping the level of LPO in tissues.
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  药物研究

  Determination of Nifedipine in Human Plasma by High Performance Liquid Chromatography Tandem Mass Spectrometry

  REN Xiuhua;YUAN Chunping;ZHANG Donglin;LIU Yu;CHEN Qian;LIU Dong

  2012, 31(5): 584-588.

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  ObjectiveTo establish a high performance liquid chromatography tandem mass spectrometry（HPLCMS/MS） method for determinng nifedipine in human plasma.MethodsPlasma samples were precipitated with acetonitrile and detected by HPLCMS/MS using midazolam as internal standard.The separation was carried out on a Diamonsil C18 column（2.1 mm×150 mm，5 μm）with a mobile phase of methanolH2O（77.7：23.3） and the flow rate was 0.3 mL•min－1.Electrospray ionization（ESI） was performed，and the multireaction monitoring mode（MRM） was used to monitor positive ion and the quantitative analysis of ion pairs for nifedipine and internal standard midazolam was at m/z 369.1→224.2 and m/z 325.9→291.0，respectively.ResultsThe linear range of nifedipine in plasma was within 1.205－241.000 ng•mL－1，r＝0.996 9.The LLOQ of nifedipine in plasma was 1.205 ng•mL－1.The relative recovery of the method was 85%115% and the intra and inter day RSDs were less than 9%.ConclusionThis method is sensitive，accurate，reliable and is suitable for pharmacokinetic studies of nifedipine in human.
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  药物研究

  Bioequivalence of Cetirizine Hydrochloride Chewable Tablets in Chinese Healthy Volunteers

  SHU Chengren;WEI Lele

  2012, 31(5): 588-591.

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  ObjectiveTo study the relative bioavailability and evaluate the bioequivalence of cetirizine hydrochloride chewable tablets in Chinese volunteers.MethodsThe concentrations of cetirizine hydrochloride in plasma following oral administration at a single dose in a randomized crossover study were detected by a HPLCUV method and the pharmacokinetic parameters were calculated by DAS2.0 software for assessing the bioequivalence.ResultsAfter oral administration of 20 mg preparations of the test and reference，respectively，the obtained pharmacokinetic parameters were as follows: AUC0→t were（5.814±1.454） and（5.802±1.028） μg•mL－1•h，respectively;AUC0→∞were（6.358±1.617）and（6.236±1.186） μg•mL－1•h，respectively;Cmax were（0.749±0.149）and（0.716±0.153） μg•mL－1，respectively; tmax were（0.819±0.391）and（1.000±0.429） h，respectively；t1/2 were（7.332±0.199）and（7.375±1.420） h，respectively.The relative bioavailability of the test tablet was（99.9±17.5）%.ConclusionThe method established for content detection of cetirizine hydrochloride in plasma is in consistent with the requirements for relative bioavailability study.The test preparations and the reference ones are bioequivalent.

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  药物研究

  Determine the Influence of Solvents on Conjugation between Antibiotics with Human Serum Albumins by Fluorescence Spectrometry

  LIN Jiale;DAI Gexin;ZHANG Zhennan;WANG Xuebao

  2012, 31(5): 591-595.

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  ObjectiveTo investigate the influence of different solvents on conjugation of ceftazidime，ceftriaxone，cefminox and moxalactam with human serum albumins（HSA） under physiological condition.MethodsThe apparent quenching constant（Kq） and binding constant（KA） between drugs and HSA were calculated by detecting the fluorescence values with fluorescence spectrometry.ResultsThe interaction of ceftazidime，ceftriaxone，cefminox and moxalactam with HSA was a kind of static quenching procedure.The binding capacity with albumin of ceftazidime，ceftriaxone and cefminox in 5% GS was lower than that in 0.9% NS，while that of moxalactam increased to some extent.ConclusionThe drug efficacy of ceftazidime, ceftriaxone and cefminox is more durable when taking 0.9% NS as solvent than 5% GS; while the drug effiacy of moxalactam is more durable when taking 5% GS as solvent than 0.9% NS.
药物与临床
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  药物与临床

  Analgesic Effect of Oxycodone and Acetaminophen Tablets for Total Hip Arthroplasty

  FANG Zhong;XIAO Jun;LI Feng;XIONG Wei;LI Guanghui

  2012, 31(5): 608-611.

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  ObjectiveTo investigate the analgesic effect of oxycodone and acetaminophen tablets for total hip arthroplasty（THA）.MethodsSixtyfour patients who undergone unilateral THA surgery were randomly divided into two groups evenly.The treatment group took one tablet of oxycodone and acetaminophen（containing oxycodone hydrochloride 5 mg and paracetamol 325 mg）tid and the control group took celecoxib 200 mg bid.Both treatment lasted for 5 days.Resting visual simulation pain score（RVAS），initiative visual simulation pain score（IVAS），perisistent visual simulation pain score（PVAS），the time for active leg lifting up to 30° and for limbs outreaching up to 45° after surgery and the overall hospital satisfaction with analgesia and complications were recorded.ResultsThe RVAS，IVAS and PVAS of the treatment group at 24 h，48 h，and 72 h postoperation were significantly lower than those in the control group（P＜0.01）.The duration for leg lifting at 30° and for limbs outreaching at 45° of the treatment group［（1.9±0.8） h，（2.9±1.1） d ］were significantly shorter than those of the control ［（3.8±1.2） h，（4.5±1.4） d ］（P＜0.01）.The overall satisfaction with analgesia in the treatment group （83.1%）was significantly better than that in the control group（43.8%）.Three cases of adverse reactions occurred in the treatment group.ConclusionThe oxycodone and acetaminophen tablets show good analgesic effect for THA，which promote early functional recovery，improve the patients’ degree of satisfaction with surgery and develop fewer side effects.It could be an ideal postoperative analgesia for THA.
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

  Determination of Paeonol in Mingmu Dihuang Pills（Concentrated Pills） by HPLC

  CHENG Qiaoyuan;CHEN Bilian

  2012, 31(5): 630-632.

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  ObjectiveTo establish a method for the determination of paeonol in mingmu dihuang pills（concentrated pills）by RPHPLC.MethodsThe analysis was performed on a Agilent Zorbax SBC18 column（250 mm×4.6 mm，5 μm） with methanolwater（48：52） as mobile phase，at a flow rate of 1.0 mL•min－1.The detection wavelength was at 274 nm.The content was calculated with external standard.ResultsThe linear range of paeonol was good within 32.06－1 282.40 ng（r＝1.000 0）.The average recovery was 96.38%，with RSD as 0.80%（n＝6）.ConclusionThis method is simple，accurate，sensitive，repeatable and can be used for quality control of the preparation.
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  药物制剂与药品质量控制

  Determination of Resveratrol and Polydatin in Polygonum cuspidatum from Different Habitats

  ZHOU Yaqin;FAN Xiyuan;ZHOU Xiaolei;WANG Shuo;YUAN Jingquan;ZHANG Rongting;WEI Fan;MIAO Jianhua

  2012, 31(5): 632-634.

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  ObjectiveTo create a method for content determination of resveratrol and polydatin in Polygonum cuspidatum from different habitats of Guangxi by HPLC.MethodsThe determination of resveratrol and polydatin was performed with HPLC by using a C18（4.6 mm×250 mm，5 μm）column.Acetonitrile and 0.3% phosphoric acid were used as mobile phase，which flowing at 1.0 mL•min－1(with the gradient elution at15%－40%，0 to 25 min).The detection wavelength was 254 nm，and column temperature was at 25 ℃.ResultsThe maximum content of resveratrol and polydatin in Polygonum cuspidatum of Guangxi was 1.998 3% and 2.776 1%，respectively，and the minimum one of which was 0.356 1% and 0.370 5%，respectively.ConclusionThe established HPLC method is simple，reliable，fast，repeatable and stable，which is suitable for evaluating the quality of Polygonum cuspidatum.There is great difference between Polygonum cuspidatum from different habitats of Guangxi due to various factors.
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  药物制剂与药品质量控制

  Determination of the Content Related Substances of Mesna Injection

  ZHOU Zheng;ZHANG Yan

  2012, 31(5): 635-637.

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  ObjectiveTo establish a method for determining content and related substances of mesna injection by HPLC.MethodsA CAPCELL PAK C18（4.6 mm×250 mm，5 μm） column was used with methanolphosphate buffered solution（2.94 g of potassium dihydrogen phosphate，2.94 g of dipotassium hydrogen phosphate and 2.6 g of tetrabutylammonium hydrogen sulfate dissolved in about 660 mL water；pH adjusted to 2.3 with phosphoric acid）（35：65） as mobile phase.The flow rate was 1.0 mL•min－1 and the detection wavelength was at 235 nm.ResultsThe linear ranges of mesna and dimlsna were within 0.002－7.4 mg•mL－1（r＝1.000 0）and 0.003－0.300 mg•mL－1（r＝1.000 0），respectively.The average recoveries of mesna and dimlsna were 99.8%（RSD＝0.6%）and 99.8%（RSD＝0.7%）（n＝6），respectively.ConclusionThe method is simple，reliable，accurate and can be applied to the quality control of the preparation.
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  药物制剂与药品质量控制

  Determination of Camphor，Menthol and Borneolum Syntheticum in Cataplamat Devices by GC

  YAN Min;LIU Yuanyuan;YI Bixin

  2012, 31(5): 637-639.

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  ObjectiveTo establish a method for determination of camphor，menthol and borneolum syntheticum in cataplamat devices by GC.MethodsThe Alltech ECWAX column（30 m ×0.53 mm，1.2 μm）was applied in the analysis with nitrogen as carrier gas and FID as detector.The temperature was programmed from initial column temperature at 85 ℃ for 1 minute，rose to 140 ℃ at the rate of 10 ℃•min－1 for 13 minutes and from 140 ℃ to 210 ℃ at the rate of 50 ℃•min－1 for 3 minutes.The detector temperature was 280 ℃ and injector temperature was 250 ℃.ResultsThe linear relationship was good within the range of 8.7－4 355.0 μg•mL－1 for camphor （r＝0.999 9），9.9－4 956.0 μg•mL－1 for menthol（r＝0.999 9），and 10.0－4 998.0 μg•mL－1 for borneolum syntheticum（r＝0.999 8）.The average recoveries of camphor，menthol and borneolum syntheticum were 104.1%（RSD＝2.7%），100.6%（RSD＝2.4%） and 99.8%（RSD＝2.6%），respectively.ConclusionThe method is simple，sensitive，accurate，rapid，and can be applied to the determination of camphor，menthol and borneolum syntheticum in cataplamat devices.
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  药物制剂与药品质量控制

  Ultrasonic Extraction Technique for the Total Favonoids from Hedyotis diffusa Willd.

  XIE Jing;CHEN Yonggang

  2012, 31(5): 640-642.

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  ObjectiveTo study the ultrasonic extraction technique for the total favonoids from Hedyotis diffusa Willd.MethodsTo extract the total favonoids with an ultrasonic method，optimize the extraction process with the orthogonal experiment and purify them by chromatography with polyamide（PA） column using rutin as standard.The content of total favonoids was calculated by NaNO2Al（NO3）3NaOH.chromogenic method.ResultsThe optimized extraction technique was that extracting Hedyotis diffusa Willd 30 min once for three times with 70% ethanol（raw material：solvent＝1：20） as solvent，and the yield of which reached 2.38%.ConclusionThe best extraction technique is easy and practical，which assuring the complete extraction of the total favonoids from Hedyotis diffusa Willd.
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  药物制剂与药品质量控制

  Effect of Different Drug Processing on Contents of the Total Flavonoids in Bergamot

  LI Yong;YAO Xi

  2012, 31(5): 643-645.

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  ObjectiveTo investigate the effect of different drug processing on contents of the total flavonoids in Bergamot.MethodsThe NaNO2AlCl3NaOH method and UVvisible spectrophotometry were applied to determine total flavonoids in different processed products of Bergamot. ResultsThe highest extraction rate for total flavonoids was obtained with 50% ethanol as extracting media，and the total flavonoids in Bergamot before and after being processed showed no significant change，except for those processed via microwave were more.ConclusionThe Bergamot herbs can be processed by frying，steaming and microwaving.