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    药物研究
  • 药物研究
    WANG Yan;DIAO Bo;ZHENG Guorong;CHEN Huimin;GAO Jinhua
    2013, 32(2): 139-142.
    ObjectiveTo investigate the intervention effect of omega3 polyunsaturated fatty acids (ω3PUFAs) on pressure related tissue injury in aged rat model, and provide theoretical basis for prevention of pressure sores in elderly patients. MethodsA total of 20 aged SD rats were randomly divided into 3 groups, including the control group(n=6), the model group(n=6) and the ω3PUFAs group(n=8). Rats in the ω3PUFAs group were fed on normal diet and intragastrically administed with ω3PUFAs at 1.6 g•kg-1•d-1, and rats in model and control groups were fed on normal diet only. Twenty days later the model group and ω3PUFAs groups were exposed to a 22.47 kPa pressure for 2 h. The control group did not receive pressure intervention. After execution, the color and morphological changes of the pressured skin were observed by nake eyes, Pathological changes of the skin and muscle tissue were observed under the light microscope, and the activity levels and content of creatine phosphokinase (CPK), superoxide dismutase (SOD), myeloperoxidase (MPO) were determined in muscle homogenate. ResultsWe observed persistent redness in the local skin area under pressure in the model group and the ω3PUFAs group. Light microscopy analysis and SOD, CPK, MPO detection results showed that aged rat model developed tissue injury under 22.47 kPa pressure for 2 h. As compared with the model group, tissue injury was significantly alleviated in the ω3PUFAs group (P<0.01). Conclusionω3PUFAs could be used as an effective prevention measure to increase the antioxidant capacity, reduce inflammation reaction and reduce the incidence of pressure ulcers in elderly patients with high risk of pressure ulcers.
  • 药物研究
    WU Di;LIU Hui;PU Jinhui;ZHANG Jing;ZOU Ping;GUO Danfeng
    2013, 32(2): 142-145.
    ObjectiveTo investigate antibacterial activity of self-synthesized O-carboxymethyl chitosan (OCMC). MethodsAntibacterial rates were calculated by colony counting. Effects of different positions of the caboxymethyl group, different concentrations and pH of OCMC on antibacterial activity were compared. ResultsThe antimicrobial test demonstrated that the antibacterial activities of OCMC were better than those of N, OCMC or NCMC. The antibacterial activities of OCMC increased with concentration and decreased with pH over a certain range. It was also found that OCMC showed stronger antibacterial activities against grampositive bacteria than against gramnegative bacteria.ConclusionThe synthesized OCMC possesses a broadspectrum antibacterial property.
  • 药物研究
    PING Li;XU Bingyong;FU Zhijun
    2013, 32(2): 146-149.
    ObjectiveTo study the absorption of phenolic alkaloids from Menispermum Dauricum (PAMD) by rats’ intestines. MethodsAbsorption kinetics was investigated by intestinal perfusion in vivo in rats. The effects of absorption site, pH value and drug concentration on PAMD absorption were studied. ResultsThe absorption rate constant (Ka) of PAMD was ileum>jejunum≈duodenum, in an order from highest to lowest. The concentration of PAMD had no significant effect on Ka. Ka was significantly different at pH value of 5.4, 6.8 and 7.8 ,respectively (P<0.05). ConclusionPAMD is absorbed at all segments of intestine in rats, but the best absorption occurs in ileum; the absorption pathway of PAMD was passive diffusion, and the Ka of PAMD increases as the pH of intestinal solution increases.
  • 中药及天然药物专栏
  • 中药及天然药物专栏
    LIU Hongmiao;LI Yanling;YANG Jizhang;JIANG Shaohao
    2013, 32(2): 159-162.
    ObjectiveTo investigate possible acute and chronic toxicities of xianggui huazhuo capsules for clinical reference. MethodsMaximal tolerated dose (MTD) was established in mice for acute toxicity evaluation. In the chronic toxicological study, rats were treated with intragastrical gavage (i.g) administration for 12 weeks, and then two thirds of the the animals were sacrificed and the others were kept for observation in recovery phase for additional 2 weeks. Activity, body weights, excretion, foodintake, and external appearance of the treated animals were observed and recorded. Haematological and blood biochemical parameters were detected, and pathological examinations performed. ResultsNo evident toxicity was observed in mouse acute toxicity test. The MTD was 48 g•kg-1, equivalent to 480 times of the clinically recommended dose (0.1 g•kg-1 ). No severe toxicity was found in high, middle, or low dose group in the longterm evaluation. No organic changes were observed in pathological tests. ConclusionXianggui huazhuo capsules is safe for i.g. administration in rats at the recommended clinical dose.
  • 中药及天然药物专栏
    PAN Xiaojiao;YANG Xiufen;CHEN Liping;TANG Lu
    2013, 32(2): 163-165.
    ObjectiveTo study anticoagulant and fibrinolytic activities of polysaccharides from Curcuma kwangsiensis. MethodsThe mice were administered by gavage with low, medium and high concentrations of polysaccharides for 3 days. Clotting time (CT), prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (Fbg) of mice were detected. Fibrin plate method was performed to determine the fibrinolytic activiy of medicated serum in vitro.Results The CT, APTT and TT were prolonged significantly (P<0.05), but the PT and Fbg did not change. ConclusionThe polysaccharides from Curcuma kwangsiensis have anticoagulant activities and exert their anticoagulant activities through intrinsic pathway and common pathway of coagulation.
  • 中药及天然药物专栏
    YANG Zhongliang;YANG Xiuyun;QU Xiaolu;HU Qingxi;LI Jian;LIU Weidong
    2013, 32(2): 166-167.
    ObjectiveTo explore the analgesic effect of jinwei lithiasiseliminating granules on mice with intraperitoneal injection of acetic acid. MethodsSixty healthy male ICR mice were randomly divided into 5 groups: treatment groups (low, middle and highdose groups), positive control group and negative control group, with each group having 12 mice. Jinwei lithiasiseliminating granules (1.33, 2.66 and 5.32 g•kg-1), diclofenac sodium and isovolemic distilled water were administered by gavage in the mice of abovementioned groups, respectively, once daily, for 7 days. Each mouse was injected intraperitoneally with 0.2 mL of 0.7% acetic acid 1 h just after the final perfusion, and the writhing times of all mice was counted within 20 mins after injection. ResultsThe mean writhing times was significantly less in the treatment groups than in the negative control group (P<0.01). There was no significant difference between the treatment groups and the positive control group.ConclusionJinwei lithiasiseliminating granules are shown to have considerable analgesic effect.
  • 中药及天然药物专栏
    YU Hongsong;LING Lin;XIE Jun;JIANG Hong;SHI Guangfei
    2013, 32(2): 168-171.
    ObjectiveTo investigate the effect of salviae miltiorrhizae on hypoxic mouse cardiomyocytes.MethodsMouse cardiomyocytes were isolated from neonatal mouse heart and the cells were divided into 3 groups: high dose salviae miltiorrhizae (300 μg•mL-1) group, low dose salviae miltiorrhizae (75 μg•mL-1) group and control group, respectively. Cell viability was assessed was also evaluated using CCK8 assay. After the cells were cultured under hypoxic condition (5% CO2 and 95% N2) for 12 h, cell apoptosis was assessed by Annexin VPI and Caspase3 assay. Gene expression of Akt, Bad and FGF after cell harvest using realtime PCR. ResultsHigh dose salviae miltiorrhizae significantly increased the cell viability as compared with the other two groups (both P<0.05). Low dose also increased cell viability significantly as compared with the control group (P<0.05). High dose salviae miltiorrhizae significantly reduced cell apoptosis detected by Annexin VPI as compared with the low dose group and the control group (both P<0.05). The Caspase3 activities in both salviae miltiorrhizae groups were significantly decreased as compared with the control group (both P<0.05). There was no significant difference between high dose group and low dose group in Caspase3 activity. Realtime PCR showed that high dose salviae miltiorrhizae treatment significantly upregulated the expression of Akt and FGF (P<0.05) and reduced the expression of BAD (P<0.05) as compared with the control group. The gene expression was significantly higer for FGF (P<0.05) and lower for BAD (P<0.05) in the high dose salviae miltiorrhizae group as compared with the low dose group. ConclusionSalviae miltiorrhizae treatment increases cardiomyocyte viability and decreases cell apoptosis, mainly through the elevated gene expression of Akt, FGF and decreased gene expression of BAD.
  • 中药及天然药物专栏
    LIANG Qinglong;WEN Yangmin;XIE Yonghua;LUO Cailin
    2013, 32(2): 171-173.
    ObjectiveTo study the antioxidative activities of the polysaccharides from Panope generosa in vitro.MethodsThe capability to scavenge DPPH radical of polysaccharides from polysaccharides from Panope generosa was measured. Furthermore, the effects of polysaccharides on contents of H2O2, malondialdehyde (MDA) and nitric oxide synthase (NOS) in liver homogenate were studied. ResultsThe polysaccharides from Panope generosa scavenged DPPH radical. When the concentration of polysaccharides was 4 mg•mL-1, the inhibition rate of DPPH reached 94.50%. The polysaccharides from Panope generosa decreased the contents of H2O2, MDA and NOS in liver homogenate. ConclusionThe polysaccharides from Panope generosa can markedly enhance antioxidative capacity in vitro.
  • 药物与临床
  • 药物与临床
    HUANG Yu;GE Wei;TANG Tian;LI Changhu;ZHENG Yongfa
    2013, 32(2): 178-185.
    ObjectiveTo evaluate the efficacy and safety of threedimensional conformal radiation therapy synchronized with chemotherapy in patients with locally advanced nonsmall cell lung cancer.MethodsThe literature related to evaluation of the threedimensional conformal radiation therapy plus chemotherapy for the patients with locally advanced nonsmall cell lung cancer were retrieved from Cochrane Database of Systematic Reviews,MEDLINE,EMbase,OpenSIGLE, National Technical Information Service (NTIS),CNKI,VIP,Wanfang database and CBM from the day of database establishment till the october 2011.Two authors independently appraised the quality of the reference research, extracted the data, and performed Meta analysis to the RCTs which met the quality standards. The extracted data were analyzed by RevMan5.0.25 . ResultsA total of 12 trials were included. Meta analysis of five key outcome indicators showed that threedimensional conformal radiation therapy with concurrent chemotherapy had significantly improved the treatment efficiency and local symptoms [OR = 2.52, 95% CI (1.41,4.52) and OR = 3.22,95% CI (1.32,7.83) respectively]. But, no conspicuously difference was found in radiation esophagitis, radiation pneumonitis and bone marrow suppression degree. ConclusionThe current evidence shows that threedimensional conformal radiotherapy combined with chemotherapy can significantly improve local symptoms and treatment efficiency in patients with locally advanced nonsmall cell lung cancer, and most patients can tolerate the side effects. clinicians may recommend the combination therapy over radiation alone. Due to the limitations of the included studies,more largescale,highquality RCTs are required.
  • 药物与临床
    ZHU Jing;FU Zhen;FANG Huijuan;ZHAO Jianping;XIONG Shengdao;ZHANG Zhenxiang;XU Yongjian;XIONG Weining
    2013, 32(2): 185-188.
    ObjectiveTo explore the effect of the relevant factors and different interventions on tobacco cessation and provide evidence-based strategies for smoking intervention. MethodsQuestionnaires were collected to record the basic information of patients who agreed to quit smoking, and comprehensive interventions as giving smoking cessation drugs were performed. Then the patients were followed for 48 weeks by telephone regularly. The different interventions for the successful smoking cessation programs were collected and analyzed. ResultsThe total percentage of patients who remained tobaccofree clinic after 12, 24 and 48 weeks was 35.9%, 33.3%, and 31.0%,respectively. The success rate was significantly higher in patients treated with varenicline benefits than those without treatment after 12 and 24 weeks (P<0.01). However, there was no statistical difference in quitting smoking after 48 weeks. Patients who were previously enrolled in the smoking cessation programs had higher success rate 12 and 24 weeks later, as compared to first-time quitters. (P<0.01). Patients who left the clinic 12 weeks after treatment has very similar success rate as compared to those who left the clinic 24 and 48 weeks later(P<0.01). ConclusionPatients who have previous attempts of tobacco cessation supposed to be easier to quit smoking. The first 12 weeks is the most critical period for smoking cessation and varenicline may provide additional benefits.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    MA Chao;SU Mujun;ZANG Kexin
    2013, 32(2): 208-212.

    ObjectiveTo establish high performance liquid chromatography (HPLC) methods for determination of related substances in candesartan cilexetil tablets. MethodsAccording to the quality standard of candesartan cilexetil tablets announced by State Food and Drug Administration (SFDA), the related substances were determined on a Hypersil C18 column (250 mm×4.6 mm, 5 μm) with the mobile phase of Methanolacetonitrile0.05 mol•L-1 sodium dihydrogen phosphate solution (adjusted to pH 3.2 with phosphoric acid) (55:30:20) at a flow rate of 0.9 mL•min-1, detected at 254 nm wavelength. According to the standard of candesartan cilexetil tablets established by the Japanese Pharmacopoeia 16th Edition, the related substances were determined on a Waters C18 column (150 mm×4.6 mm, 5 μm) with gradient elution of mobile phase A and B [A: acetonitrilewateracetic acid (57:43:1), B: acetonitrilewateracetic acid (90:10:1)] at a flow rate of 0.9 mL•min-1, detected at 254 nm. ResultsFive related substances of candesartan cilexetil could be determined by the method referred to SFDA. A good linear relationship was observed in the concentration range of 0.25-25.00 μg•mL-1. The detection limit was 1 ng. Eight related substances of candesartan cilexetil could be determined by the method referred to Japanese Pharmacopoeia. A good linear relationship was observed in the concentration range of 0.40-40.00 μg•mL-1. The detection limit was 0.8 ng. ConclusionBoth of the determination methods could be used for the determination of related substances in candesartan cilexetil tablets. The method referred to Japanese Pharmacopoeia was proved to be more sensitive, specific, and accurate.

  • 药物制剂与药品质量控制
    LOU Yongjun
    2013, 32(2): 212-214.
    ObjectiveTo develop a thinlayer chromatography (TLC) method for determination of related substances in methylene blue and investigate the stability of it. MethodsFive uL of test solution was applied to a suitable thinlayer chromatographic plate coated with a layer of chromatographic silica gel. The chromatogram was developed in a chromatographic chamber with a solvent system consisting of the upper layer separated from a wellshaken mixture of water, nbutanol and glacial acetic acid (100:80:20), and examined under ultraviolet light at 254 nm and natural light. ResultsMethylene blue underwent extensive degradation under thermal stress (60 ℃). It was found to degrade under thermal stress (40 ℃) and photolytic conditions. It possessed hygroscopicity and degraded under high humidity conditions (RH 92.5% and 75%). ConclusionThe studies show that methylene blue is hygroscopic and unstable.
  • 药物制剂与药品质量控制
    LI Dan;YAN Shu
    2013, 32(2): 215-218.
    ObjectiveTo establish a high performance liquid chromatography (HPLC) method for simultaneous determination of 7 effective components in different forms of yinchenhao decoction. MethodsThe Inertex C18 reversedphase column (4.6 mm × 250 mm, 5 μm) was adopted as stationary phase. The mobile phase was methanol0.001% phosphoric acid with gradient elution. The injection volume was 20 μL. The flow rate was 1.0 mL•min-1. Detection was performed at wavelength of 254 nm at 30 ℃. ResultsThe contents of the effective components in one dose of the traditional decoction were: chlorogenic acid 18.120 6 mg, geniposide 21.898 8 mg, rhein 13.035 7 mg, aloeemodin 6.261 6 mg, emodin 1.385 4 mg, chrysophanol 2.878 0 mg, and rheochrysidin 0.880 2 mg. The contents of the effective components in one dose of refined granule decoction were: chlorogenic acid 0 mg, geniposide 34.470 5 mg, rhein 1.291 2 mg, aloeemodin 1.625 2 mg, emodin 1.636 6 mg, chrysophanol 2.314 6 mg, and rheochrysidin 1.166 8 mg. ConclusionThis method is accurate and rapid. The contents of the effective components in the different forms of yinchenhao decoction are different, so drug compatibility is one of the main causes for the change of effective components. Although refined granule decoction of yinchenhao is feasible for clinical application, the concentrations of effective components are not comparable to traditional decoction.
  • 药物制剂与药品质量控制
    ZHANG Wenting;HUANG Wei;WANG Weisheng;CHENG Xiaqian;XU Lijun;LOU Jinfang;WANG Chunfu
    2013, 32(2): 218-220.
    ObjectiveTo compare the contents of stachydrine and leonurine of young Leonurus heterophyllus (YLH) in different harvest time for the further scientific guidance for implantation and harvest of YLH. MethodsA high performance liquid chromatography (HPLC) method was established for the simultaneous determination of stachydrine and leonurine in YLH. The contents of these two alkaloids in different places of production and harvest time were determined. ResultsThe contents of the two alkaloids increased over time in both two places of production, reached a peak at about the 5th month after implantation, and then decreased. ConclusionThe method is stable with good resolution, and suitable for the quality control of YLH. The data obtained can provide research base for the implantation and harvest of YLH.
  • 药物制剂与药品质量控制
    HU Bei;MA Hongda;SHI Guobing;HOU Mingxiao
    2013, 32(2): 221-222.
    ObjectiveTo establish a method to determine matrine content in shenqiyangxin dropping pills.MethodsHigh performance liquid chromatography (HPLC) was used to directly determine matrine on DiamonsilC18 (200 mm ×4.6 mm,5 μm) column. Acetonitril0.1% phosphoric acid (20:80) (adjusted to pH 8.0 by triethylamine) served as mobile phase. The flow rate was 1.0 mL•min-1. The detection wavelength was set at 220 nm and the temperature was 35 ℃. ResultsThere was a good linearity within the range of 0.31-9.92 μg•mL-1, r=0.999 9. The average recovery of matrine was 98.28%, and RSD was 1.66% (n=6). ConclusionThe method is simple, accurate and reproducible. It can be used as a quality control method for shenqiyangxin dropping pills.
  • 药物制剂与药品质量控制
    ZHANG Yuanyuan;LI Yinfeng;WANG Jiejing;LI Pei;JIN Chaodong
    2013, 32(2): 223-225.
    ObjectiveTo determine the related substances in lurasidone hydrochloride by reversed phase high performance liquid chromatography (RPHPLC) method. MethodsYMCPack Pro C18 Column (150 mm×6.0 mm, 5 μm) was used. The mobile phase consisted of methanol5 mmol•L-1 diammonium phosphate [adjusted to pH 7.0 by phosphoric acid] (85:15). The detection wavelength was 230 nm, and the flow rate was 1.0 mL•min-1.ResultsLurasidone hydrochloride was effectively isolated from all of the intermediates and degradation products under this condition. The calibration curve of lurasidone hydrochloride was linear over the range of 2.772-1 108.8 μg•mL-1(r=0.999 9). ConclusionThe method was accurate, simple, rapid and exclusive, and could be applied for examination of related substances in lurasidone hydrochloride.
  • 药物制剂与药品质量控制
    RUAN Hongsheng;CAO Ling;CHEN Zhibao;JIA Guiyan;ZHENG XiaoLiang;QIN Xuegong
    2013, 32(2): 226-229.

    ObjectiveTo optimize the extraction technology of epicatechin from Fagopyrum dibotrys (D. Don) Hara. MethodsCentral composite design and response surface methodology were adopted to optimize the process of extraction. The independent variables were microwave power,ethanol concentration,sample/solvent ratio and extraction time. The dependent variable was extraction rate of epicatechin which was used to estimate the relationship between independent and dependent variables. The prediction was evaluated by comparing the observed and predicted values. ResultsThe optimum technological parameters were as follows: microwave power 211.89 W,ethanol concentration 55.11%, ratio of sample/solvent 1:11.43,and extraction time 6.16 min. The highest extraction rate of epicatechin was 2.041 4%, which coincided with the model predicted values.ConclusionThe extraction technology is simple,reliable and highly predictive.