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    药物研究
  • 药物研究
    Optimization of the Separation Conditions of Fingerprint for Plumbago Zeylanica by High Performance Liquid Chromatography
    HUO Shixia;YAN Ming;ZHANG Lanlan;LIU Xiaodong
    2009, 28(11): 1399-1401.
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    ObjectiveTo optimize the separation conditions of fingerprint for Plumbago zeylanica by high performance liquid chromatography. MethodsThe reversedphase high performance liquid chromatographic method was adopted. The samples were extracted by different ethanol (V/V) solution and separated with a linear gradient elution on Shimpack VPODS C18 column(250 mm×4.6 mm , 5 μm), and then, with the acetonitrile0.1% phosphoric acid solution as mobile phase, were detected at UV 270 nm and column temperature 25 ℃. During the linear gradient elution program, the volume fraction of acetonitrile in mobile phase changed as follows: 0～80 min, from 15% to 45%; 80～120 min, from 45% to 69%; 120～125 min, from 69% to 100%; 125～140 min,100%;flow rate was 1 mL•min1. ResultsThe separation conditions described above achieved good result in the aspects of separable effect, stability, sensitivity, and reproducibility. ConclusionThe optimum separation conditions would be useful for establishing the method of fingerprint for Plumbago zeylanica by high performance liquid chromatography.
  • 药物研究
    Dissolution Property and Estrogenic Effects of Asperosaponin Ⅵ with Different Particle Sizes from Radix Dipsaci
    ZHANG Yanqing;ZHANG Chunfeng;YANG Zhonglin
    2009, 28(11): 1402-1404.
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    ObjectiveTo study the dissolution property and estrogenic effects of asperosaponin Ⅵ from Radix Dipsaci with different sizes of particle. MethodsThe contents, dissolution quantity and rate of asperosaponin Ⅵ were determined by HPLC. The estrogenic actions of asperosaponin Ⅵ with coarse, fine and superfine powders were studied on mice. ResultsThe superfine powder had a good dissolution rate and strong estrogenic effects. ConclusionThe superfine powder is better than the others on estrogenic effects.
  • 药物研究
    Antifungal Action of Euphorbia Humifusa Extracts and Effect on Squalene Epoxidase of Trichophyton Rubrum
    GULNAR&#;Dawuti;SILAFU&#;Aibai;LI Zhijian;AN Huixia;GAO li;PENG Xiaoming
    2009, 28(11): 1404-1407.
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    ObjectiveTo study in vitro antifungal activity of Euphorbia humifusa extract(EHE), and its mechanism of action against T.rubrum. MethodsThe MICs of 82 strains of common clinical fungi treated by EHE were measured by the standard approved by the National Committee for Clinical Laboratory Standards (NCCLS): reference method for broth dilution antifungal susceptibility testing of filamentous fungi (M38A). And the effect of EHE on squalence epoxidase activity in T.rubrum membrane was studied by ELISA. ResultsThe mean MIC of EHE against T.rubrum was 446 μg•mL1, against T.mentagrophytes was 652 μg•mL1, against T.violaceum was 1 024 μg•mL1, against T.schoenleinii was 896 μg•mL1, against T.verrucosum was 853 μg•mL1, against M.canis and 4 kinds of Candida, were all higher than 1 024 μg•mL1. And the activity of squalence epoxidase was attenuated by EHE at 256 μg•mL1.ConclusionEHE has remarkable antifungal activity against the dermatophytes than Candida. The mechanism of action may be related to its inhibition on squalene epoxidase activity in fungus.
  • 药物研究
    Study on Supercritical Fluid CO2 Extract of Valeriana Officinalis L.by GCMS
    DENG Xuehua;ZHU Ronghua;ZHOU Ying;FANG Ying;LIU Yanwen
    2009, 28(11): 1408-1410.
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    ObjectiveTo detect the chemical components of supercritical fluid CO2 extract from Valeriana officinalis L.MethodsThe Valeriana officinalis oil was extracted by supercritical fluid CO2 extraction technology and the chemical components were analyzed by GCMS. Results 51 components were identified and composed of 78.4% Valeriana officinalis oil. ConclusionThis method has a good separating effectiveness and can provide a base for the exploitation and application of Valeriana officinalis L.
  • 药物研究
    Effect of Radix Salviae Miltiorrhizae on Apoptosis and CyclinD1 Expression of Spinal Dorsal Horn Neurons in Diabetic Rats
    YANG Yingcong;ZHOU Qingshan;WANG Long
    2009, 28(11): 1410-1413.
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    ObjectiveTo investigate the effect of Radix salviae miltiorrhizae on apoptosis and cyclinD1 expression of spinal dorsal horn neurons in diabetic rats. MethodsThirty male Wistar rats weighing 180～220 g were randomly divided into 3 groups (n=10 each): group A (diabetes mellitus) ， group B (diabetes mellitus + radix salviae miltiorrhizae) and group C (normal control) . Diabetes mellitus was induced by intraperitoneal injection with streptozotocin (STZ) 60 mg•kg1 in rats. 3 mL•kg1 Radix salviae miltiorrhizae was given intraperitoneally 1 week after STZ injection, q.d. for 4 weeks in group B. Paw withdraw threshold (PWT) was calculated by von Frey filaments before and 1, 2, 3, 4 and 5 w after STZ injection. All rats were killed 5 weeks after STZ injection and lumbar segment of spinal cord was removed for detection of apoptosis in spinal dorsal horn neurons (TUNEL) and determination of cyclinD1 expression by immunohistochemistry. ResultsCompared with group C, PWT was lower, the histopathological damage in spinal dorsal horn was visible, apoptotic index and cyclinD1 expression were increased significantly in group A and B (P＜0.05). While compared with group A, PWT was increased, the histopathological damage was attenuated, apoptotic index and level of cyclinD1 were decreased significantly in group B(P＜0.05).ConclusionRadix salviae miltiorrhizae can attenuate the spinal dorsal horn neuronal apoptosis through downregulation of cyclinD1 expression in diabetic rats
  • 药物研究
    The Effect of Sodium TanshinoneⅡA on Connective Tissue Growth Factor in Cultured Peritoneal Mesothelial Cell
    DING Hong;WANG Zongqian;MA Jianfei;FAN Yi
    2009, 28(11): 1414-1416.
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    ObjectiveTo investigate the effect of sodium tanshinoneⅡA on connective tissue growth factor(CTGF) of mesothelial cells (PMCs) cultured in high concentration of glucose. MethodsPrimary PMCs of male Wistar rats were cultured in different concentration of glucose, and interfered by Sodium tanshinoneⅡA later.Extracellular CTGF level was detected by ELISA; expression of CTGF mRNA was assessed by using reverse transcription polymerase chain reaction (RTPCR). ResultsHigh concentration of glucose stimulated the expression of CTGF (P＜0.01), which was suppressed by sodium tanshinoneⅡA (P＜0.01) in a dose dependent manner. ConclusionSodium tanshinoneⅡA can decrease the expression of CTGF stimulated by high concentration of glucose in a dose dependent manner. Sodium tanshinoneⅡA might be an effective agent to reduce extracellular matrix accumulation and inhibit peritoneal fibrosis of peritoneal membrane.
  • 药物研究
    The Effects of Iptakalim on Plasma Endothelin1 and Its mRNA Expression in Rats with Hypoxic Pulmonary Hypertension
    SHEN Hong;XIE Weiping;WANG Hong;JIN Yu;CAI Jiankang
    2009, 28(11): 1416-1419.
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    ObjectiveTo explore the effects of Iptakalim on endothelin1(ET1) and its mRNA expression in the lung of rats with chronic hypoxic pulmonary hypertension(HPH). MethodsSD rats were randomly divided into normalcontrolled group, HPHmodel group, and Ipt treated group(treated with Ipt 1.5mg•kg1•d1 prior to hypoxia),the HPHmodel group and Ipt treated group were bred in normal baric and hypoxic condition, 8 hour a day ,6 days a week, for 4 weeks. Radioimmunoassay was used to test the plasma ET1 concentration of rats. The expression of ET1 and endothelin converting enzyme(ECE) was detected by reverse transcription polymerase chain reaction（RTPCR）. ResultsCompared with control group, the plasma ET1 concentration, ET1 mRNA and ECE mRNA markedly increased in HPH group (P＜0.01);Plasma ET1 concentration, ET1 mRNA and ECE mRNA were significantly lower in Ipt group than those in HPH group(P＜0.01).ConclusionIptakalim may prevent the hypoxic pulmonary hypertension by inhibiting the upregulated expression of ET1, ECE induced by hypoxia, reversing the increased plasma levels of ET1 under pathological condition.
  • 药物研究
    Influence of Chronic Ethanol Intake on the Cardiovascular System and Liver in Rats
    HUO Jiping;TANG Qiang;HU Benrong;ZHANG Qiufang;LIU Yuyan;FENG Mei;XIANG Jizhou
    2009, 28(11): 1420-1423.
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    ObjectiveTo study that whether moderate ethanol intake could or not protect the cardiovascular system and do harm to the liver. MethodsFifty male healthy adult SD rats were randomly assigned into five groups: control group(sodium chloride, 1 mL•kg1•d1)，sucrose group(5% sucrose, 1 mL•kg1•d1) and three ethanol groups (50% ethanol, 2.5 mL•kg1•d1; 50% ethanol, 5 mL•kg1•d1; 50% ethanol, 10 mL•kg1•d1).All the rats were treated with intragastric administration for 12 weeks. By the end of the 12th week, the heart weight index and left ventricle weight index were calculated; the tissues from the heart, liver and thoracic aorta were stained with HE. ResultsThe plasma cholesterol level in sucrose group and ethanol groups were higher than that of control group (P＜0.05 or P＜0.01).The triglyceride level in 50%ethanol 5 mL•kg1•d1 and 10 mL•kg1•d1 were higher than that of control group and sucrose one (P＜0.05 or P＜0.01). Blood pressure in 50%ethanol 5 mL•kg1•d1 and 10 mL•kg1•d1 were higher than that of control group (P＜0.05). With HE staining, the blood vessel endothelium were not smooth in sucrose and three ethanol groups, and slight fatty degeneration in the liver was found in these groups. Hepatic cord arranged in disorder in 50%ethanol 5 mL•kg1•d1 group. Connective tissue hyperplasia in the liver portal area and spotty necrosis were observed in 50%ethanol 10 mL•kg1•d1 group. Myocardial fiber disarranged in the three ethanol groups. ConclusionChronic mild ethanol ingestion can cause the increase of plasma cholesterol and triglyceride and lead to different degrees of damage in liver, heart and blood vessel, which may do harm to the health.
  • 药物研究
    The Effects of Pretreatment with Ambroxol on Airway Inflammation in Rats with Chronic Bronchitis Induced by Smoking
    YANG Rongshi;PENG Hongxing;ZENG Yulan
    2009, 28(11): 1423-1426.
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    ObjectiveTo explore the role of intercelluar adhesion molecule1(ICAM1) on airway inflammation in rats with chronic bronchitis induced by smoking and study the effect of pretreatment with ambroxol and possible mechanism. MethodsMale Wistar rats were randomly divided into three groups: the control group, smoking group, ambroxol intervention group. The rat model of chronic bronchitis was established by smoking only. For ambroxol intervention group, rats were pretreated with ambroxol through peritoneal injection at 35 mg•kg1•d1 for 75 days, six days each week. The histopathologic changes in hemotoxylin and eosin (HE) stained bronchopulmonary tissues were observed under optical microscope; total cell counts and differential analysis were performed in bronchoalveolar lavage fluid (BALF); the expression of ICAM1 was detected by immunohistochemistry. ResultsThe pathological change of model group was in consistent with that of human chronic bronchitis. The expression of ICAM1 on bronchi and alveolar epithelial and bronchopulmonary capillary endothelial cells were positively correlated with the leukocyte numbers and neutrophil in BALF in the model group (P＜0.01). The expression of ICAM1 in the model group significantly increased as compared with the control group（P＜0.01）; which significantly decreased in ambroxol intervention group compared with the model group（P＜0.01）. ConclusionICAM1 may be involved in the process of airway inflammation in rats with chronic bronchitis induced by smoking; ambroxol might have some effects on ameliorating airway inflammation by downregulating the expression of ICAM1 and inhibiting the aggregation of neutrophil.
  • 药物研究
    Preparation of SustainedRelease PLGA Microspheres Containing Ropicavaine and Dexamethasone and Release Property in Vitro
    XU Yan;CHEN Zhongqing;YU Ranghui;LI Guofeng;WANG Xiaoqiao
    2009, 28(11): 1427-1431.
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    ObjectiveTo prepare sustainedrelease PLGA microspheres containing ropicavaine and dexamethasone (RopDexPLGAMS) and study drug release in vitro. MethodsRopDexPLGAMS was prepared with PLGA as carrier by a waterinoilinwater(W1/O/W2) dubleemulsion solvent evaporation method. Effects of various preparation parameters, such as polymer concentration, continuous phase/organic phase(CP/OP) ratio, volume of internal water phase and stabilizer PVA concentration on the properties of microspheres, such as particle size, morphology, drug loading, encapsulation efficiency and burst release in vitro were examined. ResultsPLGA levels was a critical factor for preparing microspheres and particle size; drug loading, encapsulation efficiency were increased significantly with increasing PLGA accompanied by a remarkably decreased burst release. The particles size, drug loading, encapsulation efficiency increased considerably, the surface of microspheres was smoother and burst release decreased as the volume ratio of CP/OP increased. Porous matrix in microspheres augmented, burst release increased and drug loading, encapsulation efficiency decreased with the higher volume of internal water phase. Particle size decreased and burst release increased as PVA concentration in the continuous phase was increased from 0.5% to 2%.By optimizing the prepare technology, RopDexPLGAMs were achieved with spherical shape, smooth surface and evenly distributed. Approximately 90% of microspheres were within the range of 20～70 μm in size. The drug loading of ropivacaine and dexamethasone were （7.48±0.33）% and （1.52±0.16）%, and encapsulation efficiencies were （70.97±2.36）% and （57.30±1.17）%, respectively. ConclusionThe duble emulsion solvent evaporation method is applicable for preparation of RopDexPLGAMs. The microspheres have a good appearance and significant in vitro sustainedrelease characteristics as a typical Sshaped and threephase.
  • 药物研究
    Protective Effects of dlTetrahydropalmatine on Focal Cerebral Ischemiareperfusion Injury in Rats
    MA Xiao ya;WANG Meina;DENG Xiuling;CAI Yingmin;LIANG Weiwei;WANG Yuhu
    2009, 28(11): 1432-1436.
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    ObjectiveTo study the protective effects of dltetrahydropalmatine (THP) on focal cerebral ischemiareperfusion injure in rats. MethodsThe modified LONGA method was used to make the model of focal cerebral ischemiareperfusion injury in rats. THP was ip injected at 10.0,5.0,2.5 mg•kg1 15 min before ischemia. The influence of THP were observed after ischemia for 3 h followed by reperfusion for 3 h on neurological deficits, size of cerebral infarction, lactate dehydrogenase (LDH) and creatine kinase (CK) activities in serum, contents of water, calcium, malondialdehyde (MDA) and superoxide dismutase (SOD) activity in brain tissue, and injure of brain ultrastructure in the model rats. ResultsTHP dosedependently reduced neurological deficit scores, decreased the size of cerebral infarction and inhibited LDH and CK in serum. THP 10.0 mg•kg1 markedly lowered the water contents of injured brain, improved the damaged brain ultrastructure. THP also increased the activity of SOD, reduced the content of MDA and inhibited intracellular calcium accumulation in the cerebrum. ConclusionTHP has protective effects against cerebral ischemiareperfusion injury in rats, and mechanism of which might be related to inhibiting the lipid peroxides and reducing calcium accumulation.
    • 代谢性疾病用药专栏
  • 代谢性疾病用药专栏
    The Effect of Malt Extracts on Prolactin Levels in HPRL Mice
    WEI Anhua;CAI Yaling;WU Jinhu;RUAN Jinlan
    2009, 28(11): 1441-1443.
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    ObjectiveTo investigate the effect of malt extracts on prolactin level in female HPRL mice, and preliminary analyze the chemical constituents , in order to determine the active fraction.MethodsThe content of polysaccharide in malt extracts was determined by phenolsulfuric acid method and flavonoids were detected by UV spectrophotometer.The female HPRL mice model was induced by metoclopramide, and then the malt extracts were given intragastrically.ResultsThe content of polysaccharides and flavonoids were 7.60%, 0.17%, with RSD as 0.70%, 1.70%, respectively.The serum PRL in the model mice was significantly increased (P＜0.05); that in the malt extracts treated groups were significantly decreased（P＜0.05）.No significant difference between treatment groups and the bromocriptine group was found.ConclusionThe malt extract could decrease the prolactin level in female HPRL mice which induced by metoclopramide, with the similar action as bromocriptine.
  • 代谢性疾病用药专栏
    Hypoglycemic Effect of the Extracts from a Chinese Traditional Compound FormulaHuangqi in Mice
    HONG Ge;LI Songnian;MA Shitang;YU Jie
    2009, 28(11): 1444-1446.
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    ObjectiveTo investigate the hypoglycemic effect of the extracts from a Chinese traditional compound formulahuangqi on normal mice and alloxaninduced diabetic mice. MethodsThe diabetic mice were induced by alloxan in Kunming mice. Then they were administrated with the extracts continuously for 30 days, and the changes of the blood glucose value were observed. Blood glucose was measured at 0, 0.5, 2 hours after oral administration with glucose liquid, and the change of area under the blood glucose curve (AUC) was calculated. The same method was used to evaluate the influence of extracts on body weight, blood glucose value and glucose tolerance in normal mice. ResultsThe extracts had no influence on body weight, blood glucose value and the AUC induced by the glucose loading in normal mice. The descending rates of blood glucose were 2.85%，10.76% and 12.99%, respectively in the three extracts treated groups of diabetic model. Both the blood glucose value of 0, 0.5, 2 hours and the AUC induced by the glucose loading were decreased as well. ConclusionThe extracts from Chinese traditional compound formulahuangqi have the functions of lowering the blood glucose and regulating glucose tolerance on alloxancaused diabetic mice.
  • 代谢性疾病用药专栏
    The Effect of Total Flavones of Buckwheat Flower and Leaf on Ultrastructural Organization in Diabetic Rats
    JIA Hongjuan;HAN Shuying;WANG Xizhu;SONG Qiaofeng;ZHU Yanhui
    2009, 28(11): 1447-1449.
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    ObjectiveTo study the protection of total flavones of buckwheat flower and leaf (TFBFL) on ultrastructural organization in diabetic rats and probe its mechanism. MethodsT2DM was induced by intraperitoneal injection of streptozotocin (STZ) and i.g. fat milk in rats. At the end of the experiment, blood fat and blood glucose were measured and the pathology tissue slices were made to observe the ultrastructural alteration under electron microscope. ResultsFBG, TC, TG, FFA in TFBFL group was significantly lower than those in the experimental control group. TFBFL improved the heart construction. ConclusionTFBFL could ameliorate myocardial damage in STZ induced T2DM model.
  • 代谢性疾病用药专栏
    Impacts of Yinning Tablets on ThyroidInduced Hyperthyroidism YinDeficiency Model of Rats
    LIU Ting;HOU Lianbing;ZHONG Yansong
    2009, 28(11): 1450-1452.
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    ObjectiveTo establish a hyperthyroidism Yindeficiency model on rats and study the major pharmacodynamics role of yinning tablets. MethodsThe hyperthyroidism Yindeficiency model was set up by feeding rats with the suspension of thyroid tablets. The T3, T4, FT3, FT4, TSH in rats were detected by RIA and the body weight, rectal temperature, behavior and appearance were tested. The thyroid and adrenal tissue indexes were caculated and WBC and neutripluls were also counted. ResultsCompared with the model rats, serum T3, T4, FT3, FT4 values and rectal temperature were significantly lower (P＜0.05) serum TSH values, weight, WBC and neutripluls increased significantly (P＜0.05) in drugs treated rats. ConclusionYinning tablets not only help hyperthyroidism Yindeficiency rat return to normal, but also can increase body weight, lower rectal temperature, improve appearance and performance, which have the similar effect of jiakangling tablets.
    • 药物与临床
  • 药物与临床
    Amlodipine Combined with Bisoprolol for the Treatment of Renal Hypertension
    PENG Cheng;HE Xiaofeng;LIU Shenwei
    2009, 28(11): 1456-1458.
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    ObjectiveTo evaluate the effects and safety of amlodipine combined with bisoprololin for the treatment of renal hypertension. MethodsFiftyone patients with renal hypertension were randomly divided into two groups. 28 Patients in the control group were treated with amlodipine 5.0 mg q12 h，while 23 in the treatment group were treated with amlodipine 5 mg qd and bisoprolol 2.5－5.0 mg qd for eight weeks. Blood pressure, heart rate and renal function were monitored before and after treatment. ResultsThe total antihypertensive effective rates were 67.9% and 82.6% in the control and treatment group, respectively. There were no significant changes in heart rate and renal function before and after treatment in both groups and no obvious adverse events occurred. ConclusionAmlodipine combined with bisoprolol was efficient and safe for the treatment of renal hypertension, and was more effective than amlodipine used alone.
    • 药品质量控制
  • 药品质量控制
    Content Determination of Principal Agent in Armillarisin Amber Acid Ester Injection by RPHPLC
    LI Peng;LI Chungang;ZHU Yu;CHEN Qinhua;HU Wenji;WANG Zhongqin
    2009, 28(11): 1493-1494.
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    ObjectiveTo establish a RPHPLC method for detecting the principal agent in armillarisin amber acid ester (AAAE) injection. MethodsRPHPLC was performed on DLC18 column(4.6 mm×150 mm，5 μm) with methanol：1% phosphoric acid：triethylamine (45：55：0.05) as mobile phase at a flow rate of 0.8 mL•min1. The detection wavelength was 366 nm. ResultsThe liner range of AAAE injection was 1~100 μg•mL1, r=0.999 9. The relative standard deviation (RSD) for the method was 0.46% and 1.97%, respectively and the mean extraction recovery was 102.25%. ConclusionThe method is proved to be accurate, sensitive and reliable, which is suitable for the determination of AAAE in the injection.
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