中国科技论文统计源期刊　中文核心期刊  
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    药物研究
  • 药物研究
    Establishment of Insulin Resistant HepG2 Cell Model and Its Application in Screening Bioactive Components of Mulberry Leaves
    FANG Fei;WU Xinrong;LUO Mingli;LV Huan
    2012, 31(6): 691-694. https://doi.org/10.3870/yydb.2012.06.001
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    ObjectiveTo establish an insulin resistant HepG2 cell model in vitro to screen bioactive components of mulberry leaves. MethodsThe insulin resistant HepG2 cell model was induced by high concentration of insulin. Glucose consumption of the cells was detected after administration with the bioactive components of the mulberry leaves. ResultsAfter the HepG2 cells were cultured with insulin (10 μg·mL－1) for 48 h, insulin resistance of the cells was the most apparent and maintained for 48 h. The bioactive components of mulberry leaves could promote glucose consumption of insulin resistant HepG2 cell model.ConclusionThe insulin resistant HepG2 cell model was successfully established in vitro by high concentration of insulin. Extracts, polysaccharides and flavonoids of the mulberry leaves enhance glucose absorption.
  • 药物研究
    Experimental Study on Reducing the Adverse Effects of Oxcarbazepine in Pregnancy Mice
    LI Yunxia;ZHENG Lina;KAN Shujuan;YANG Jianchun
    2012, 31(6): 695-697. https://doi.org/10.3870/yydb.2012.06.002
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    ABSTRACTObjectiveTo study the influence of oxcarbazepine administration at single or repetitive (multiple) dose in pregnant mice and the interference effects of folic acid on the unexpected adverse event induced by oxcarbazepine in pregnant mice, and to investigate the measures to reduce the adverse effects of oxcarbazepine in pregnant mice. MethodsOne hundred and fifty mice were randomly divided into 5 groups (n＝30 of each group, ratio of female to male was 2：1). In control group, the mice were perfused with distilled water (10 mL•kg－1) in stomach; in singledose oxcarbazepine group, the mice were perfused with oxcarbazepine (150 mg•kg－1) in stomach; in singledose oxcarbazepine ＋ folic acid group, the mice were perfused with oxcarbazepine (150 mg•kg－1) and folic acid (0.07 mg•kg－1) in stomach; in repetitive dose oxcarbazepine group, the mice were perfused with oxcarbazepine (75 mg•kg－1) in stomach in the morning and afternoon, respectively; in repetitive dose oxcarbazepine ＋ folic acid group, the mice were perfused with oxcarbazepine (75 mg•kg－1) and folic acid (0.07 mg•kg－1) in stomach in the morning and afternoon. Conception rate, abortion rate, the absorptions and dead rate, aberration rate, number of normal newborn mice, weight increment during pregnancy, the content of serum folic acid were detected. ResultsThe pregnancy rates of mice in oxcarbazepine singledose group, oxcarbazepine singledose ＋ folic acid group, repetitive dose oxcarbazepine group, and repetitive dose oxcarbazepine ＋ folic acid group were 20%, 30%, 40%, and 50%, respectively. The absorptions and dead rates were 18.8%, 9.8%, 11.6% and 9.2%, respectively. The weight increment during pregnancy and the contents of serum folic acid were increased in these groups in turn. No significant teratogenic effects caused by oxcarbazepine were found. ConclusionOxcarbazepine can lead to unexpected adverse events in mice during pregnancy without significant teratogenic effects; multiple small dose of oxcarbazepine and supplement of folic acid can reduce the adverse effects.
  • 药物研究
    Effect of Fenofibrate on the Expression of Acyl-CoA Synthetase in Aged Rat Liver
    WANG Zhaojun;LI Tianchang;YANG Ye;LI Xianfeng;HUANG Huogao;QIU Yigang
    2012, 31(6): 698-700. https://doi.org/10.3870/yydb.2012.06.003
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    ABSTRACTObjectiveTo investigate effect of fenofibrate on acylCoA synthetase (ACS) expression in aged rat liver and explore the molecular mechanism of lipid metabolism and regulation effect of fenofibrate on lipid metabolism during aging. MethodsSixteen young (46 weeks) and 16 aged (24 months) male SD rats were involved in this study. Both groups of rats were randomly divided into two subgroups: control group, fed with routine food for 2 weeks; experimental group, fed with fenofibrate for 2 weeks. Levels of triglyceride (TG) and total cholesterol (TC) were detected. The level of liver ACS mRNA was determined by reverse transcriptionpolymerse chain reaction (RTPCR). ResultsIn the control group, the TG and TC levels of the aged rats were significantly increased and the ACS mRNA level of the aged rats was significantly decreased as compared with the young rats. Fenofibrate reduced serum TG and TC in aged rats of the experimental group. The ACS mRNA level of both groups was increased by fenofibrate. ConclusionThe mechanism of lipid dysfunction during aging is probably associated with the decreased expression of ACS. Fenofibrate can regulate lipid metabolism of aged rats.
  • 药物研究
    Effects of Bletilla Striata Polysaccharide on JAK/STAT Signaling Pathway in Oxidative Damaged Human Keratinocyte
    WANG Gang;CHANG Mingquan;YANG Guangyi;DU Shiming;YE Fang;ZHANG Xiuhua;YANG Jinxia
    2012, 31(6): 701-705. https://doi.org/10.3870/yydb.2012.06.004
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    ABSTRACTObjectiveTo investigate the protective effect and mechanism of Bletilla Striata polysaccharide on JAK/STAT signaling pathway in human keratinocytes (HKCs) with inflammation induced injury by CoCl2. MethodsAfter pretreated with Bletilla Striata polysaccharide, HKCs were interfered with certain dosages of CoCl2 to establish an inflammation induced injury cell model by oxidative stress from chemical oxidizing agent. The cell viability was detected by MTT method. The levels of cytokine TNFα, IL6 and IL8 were detected by ELISA, and expression of JAK2 was determined. ResultsBletilla Striata polysaccharide could boost the cell viability in a dosedependent manner. The contents of TNFα, IL6 and IL8 in the group of high or medium dosage of Bletilla Striata polysaccharide were significantly different from those in the control group (P＜0.05). ConclusionThe inflammation injury of HKC can be caused by oxidative stress from CoCl2. Bletilla Striata polysaccharide can inhibit release of TNFα, IL6 and IL8 through regulating expression of JAK2 in JAK/STAT signaling pathway, which might be one of the mechanisms of protection.
    • 药物与临床
  • 药物与临床
    Predictive Value of Excision Repair Cross-complementation Group 1 (ERCC1) Polymorphism on Chemotherapy Response and Survival of Advanced Nonsmall Cell Lung Cancer Patients Treated with Cisplatin
    WANG Lin;DAI Xiaofang;WU Gang;REN Jinghua;CHEN Weihong;LIU Zhao
    2012, 31(6): 720-724. https://doi.org/10.3870/yydb.2012.06.013
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    ABSTRACTObjectiveTo evaluate the predictive value of excision repair crosscomplementation group 1 (ERCC1) codon 118 polymorphism on chemotherapy response and survival of advanced nonsmall cell lung cancer (NSCLC) patients treated with cisplatin. MethodsIn 101 advanced NSCLC patients treated with platinumbased chemotherapy, polymerase chain reactionbased restriction fragment length polymorphism (PCRRFLP) assay was used to detect ERCC1 codon 118 C>T polymorphism. ResultsWe found codon 118 polymorphism was not correlated with sex, age, family history of malignant cancer, smoking, pathology type and stage, and chemotherapy response. Median survival time and oneyear survival rate of C/C genotype carriers were higher than those of C/T and T/T genotype carriers (13.7 m vs. 10.6 m; 67% vs. 35%, both P＜0.01). Multivariate analysis of Cox proportional hazard model showed that sex (Hazard ratio=1.907, P=0.022), pathology type (Hazard ratio=1.980, P=0.032) and ERCC1 codon 118 polymorphism (Hazard ratio=2.536, P＜0.01) were independently associated with reduced survival. ConclusionThe ERCC1 codon 118 (C>T) C allele can be a prediction factor for better survival of advanced NSCLC patients treated with cisplatin.
  • 药物与临床
    Effect of Rosuvastatin on 58 Patients with Type 2 Diabetic Mellitus Combined with Heart Failure
    LIU Haizhen;LIN Li;ZONG Wenxia
    2012, 31(6): 724-727. https://doi.org/10.3870/yydb.2012.06.014
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    ABSTRACTObjectiveTo observe the effects of rosuvastatin on left ventricular function, brain natriuretic peptide (BNP) and high sensitive Creactive protein (hsCRP) in type 2 diabetic patients with heart failure (HF). MethodsAll 120 type 2 diabetic patients with HF were randomly and evenly divided into two groups: control group and treatment group. All patients received basic treatment of type 2 diabetic mellitus and heart failure. Not only that, the patients in the treatment group were treated with rosuvastatin (10 mg•d－1). After 24 weeks, the changes of cardiac function, the levels of BNP, lipids, and hsCRP were detected and compared. ResultsIn both groups, the levels of BNP and hsCRP were positively correlated with heart function ［according to the New York Heart Association (NYHA) Functional Classification］ (r＝0.821, P＜0.01), and negatively correlated with left ventricular ejection fraction (LVEF) (r＝－0.730, P＜0.01). The levels of BNP and hsCRP were significantly different between the patients with different classification of heart function (P＜0.05). After treatment of type 2 diabetic mellitus and heart failure for 24 weeks, there was significant difference in the total effective rate between the treatment group and the control group (93.1% vs. 78.3%, P＜0.05), and the levels of BNP and hsCRP in both groups were significantly decreased (P＜0.05), LVEF was significantly increased (P＜0.05). The treatment group had more significant changes in the levels of BNP, hsCRP and LVEF than the control group. ConclusionThe increasing levels of BNP and hsCRP reflect clinical severity of type 2 diabetes patients with HF. Rosuvastatin can decrease the levels of BNP and hsCRP, and improve heart function, and it is effective in treating type 2 diabetes patients with HF.
  • 药物与临床
    Efficacy of Trazodone in Treatment of Schizophrenia with Anxious Symptoms
    FENG Shaohui
    2012, 31(6): 728-730. https://doi.org/10.3870/yydb.2012.06.015
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    ABSTRACTObjectiveTo study the therapeutic effect of trazodone on anxious symptoms, disease condition and social function of schizophrenic patients. MethodsSixtyone schizophrenic patients with anxiety symptoms were selected and randomly divided into two groups: treated group (n＝31) and control group (n＝30). Both groups were treated with the same antipsychotic drugs, while the treated group was added with trazodone. Severity of anxious symptoms of each patient was assessed with Hamilton Anxiety Scale (HAMA), schizophrenic severity with Brief Psychiatric Rating Scale (BPRS) and social functions with Personal and Social Performance scale (PSP) before the treatment and at the ends of the 4th and 8th weeks after the treatment. ResultsAt the end of the 8th week after the treatment, HAMA total scores of treated group and control group were (15.32±4.13) and (17.97±3.54); somaticanxiety factor scores were (7.32±2.86) and (9.10±2.55) (P＜0.05); BPRS total scores were (32.45±3.33) and (34.77±4.63) (P＜0.05); anxietydepression factor scores were (8.48±0.81) and (10.90±2.03) (P＜0.01); PSP scores were (70.55±5.21) and (66.17±6.07) (P＜0.01). ConclusionTrazodone can alleviate anxious symptoms and disease condition, and improve social function of schizophrenic patients with anxiety symptoms.
  • 药物与临床
    Efficacy and Safety of Paliperidone ExtendedRelease Tablets in Treatment of Male Patients with Acute Schizophrenia
    SU Wei;NA Wanqiu;LI Jianhua;YANG Jianhong;CHEN Haizhi;ZHOU Hujiang
    2012, 31(6): 731-734. https://doi.org/10.3870/yydb.2012.06.016
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    ABSTRACTObjectiveTo explore the efficacy of paliperidone extendedrelease tablets in the treatment of male patients with acute schizophrenia.MethodsIn a 12week openlabel study, 65 schizophrenics were randomly divided into study group ［treated with paliperidone extendedrelease tablets (n＝33, 6 mg per morning)］ and control group ［risperidone tablets (n＝32, starting dose: 1 mg•d－1; in a week the dose was increased to 2 mg, twice a day, in the afternoon and evening)］. They were assessed and analyzed by Positive and Negative Symptoms Scales (PANSS), Personal and Social Performance Scale (PSP), and Treatment Emergent Symptom Scale (TESS) before the treatment, in the 2nd, 4th, 8th and 12th weekends of the treatment. The level of serum prolactin was detected before the treatment, at the 4th, 8th and 12th weekends of the treatment. ResultsAt the end of the study, two groups had similar response rates (66.7% vs. 62.5%, P＞0.05). After the treatment, the factors and total scores of PANSS in the two groups were all significantly lower than those before treatment (P＜0.05). In the 2nd and 12th weekends of the treatment, the factors and total scores of PANSS in the study group were all significantly lower than those in the control group (P＜0.05). After the treatment, the total scores of PSP of both groups were significantly higher than those at baseline (P＜0.05). In the study group, the total scores of PSP in the 2nd and 12th weekends of the treatment were significantly higher than those in the control group (P＜0.05). The serum prolactin levels were increased after the treatment (P＜0.05). The serum prolatin level was lower in the study group than in the control group at the end (P＜0.05), and no hyperprolaetinemia adverse reaction was found in the study group. No severe adverse effects were found in both groups, and the incidence of treatmentemergent adverse events were lower in the study group (P＜0.05). ConclusionPaliperidone extendedrelease tablets are as effective as risperidone to improve social function of male patients with acute schizophrenia, and their safety are superior.
  • 药物与临床
    Clinical Observation of Type 2 Diabetic Patients with Insulin Pump Usage during Perioperative Period of Coronary Artery Bypass Grafting
    HUANG Yuanqin;RAO Dan;LONG Yanli
    2012, 31(6): 735-737. https://doi.org/10.3870/yydb.2012.06.017
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    ABSTRACTObjectiveTo observe operation, clinical efficacy and safety of insulin pump in patients with type 2 diabetes mellitus (T2DM) during perioperative period of coronary artery bypass grafting. MethodsThe patients were assigned into two groups: CSII group (n＝23), treated with continuously hypodermic injection by insulin pump; MSII group (n＝21), treated with multiple injection of insulin. Blood glucose and lipid levels before and after the surgery, infection rate of incision and total hospitalized days were observed. ResultsBlood glucose time in CSII group and MSII group was (3.22±1.31) and (7.00±4.07) days, respectively. One case in CSII group and 3 cases in MSII group developed hypoglycemia, with statistically significant difference (P＜0.05). The doses of insulin in CSII group and MSII group were (40.82±16.79) and (40.00±15.23) U•d－1. Total hospitalized days for CSII group and MSII group were (22.86±12.76) and (29.18±20.94) days, respectively. There was one case of incision infection in each group. ConclusionBy using CSII method, blood glucose can be controlled faster and better.
    • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    Preparation and Properties of Glaucocalyxin A-loaded Selfassemble Nanomicelles
    YANG Linjie;ZHANG Jian;SHI Jiawen;WANG Xiangtao
    2012, 31(6): 775-778. https://doi.org/10.3870/yydb.2012.06.024
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    ABSTRACTObjectiveGlaucocalyxin A shows a significant antitumor effect, but the poor water solubility greatly limits its further application. To solve this problem, micelles were intended to be prepared for the administration of Glaucocalyxin A. MethodsGlaucocalyxin A micelles were made by using solvent evaporation method with triblock polymer PLGAPEGPLGA being the carrier. The preparation was optimized by means of orthogonal experimental design. The critical micelle concentration (CMC) of the polymer was determined with pyrene fluorescent probe method. Dialysis was employed to measure the entrapment efficiency and drugloading rate. Particle size and zeta potential were studied using Zetasizer nano ZS instrument and the morphology was observed under transmission electron microscope. The drug release in vitro was studied. ResultsThe CMC of the polymer was 2.5×10－3 mg•mL－1. The mean diameter of the particle was (62.49±0.60) nm with the zeta potential being (－25.4±0.4) mV; the average entrapment efficiency was (84.85±2.00)% and the average drugloading rate was (5.36±1.00)%. The drug release profile in vitro exhibited 12hour sustained release effects and fit Higuchi linear equation. ConclusionGlaucocalyxin Aloaded nanomicelles, gained with the use of polymer PLGAPEGPLGA, could solve the poor solubility of the drug. Meanwhile, because of the sustained release and enhanced permeability and retention effect, due to the nanoparticle size, it is expected that they may have a good potential application prospect in antitumor therapy.
  • 药物制剂与药品质量控制
    Study on Preparation of Epirubicin Hydrochloride Loaded Poly (LLacticcoGlycolic Acid) Nanoparticles and the Effects in Vitro
    SONG Jingjing;LI Hui;FU Hongxing;JI Jiansong
    2012, 31(6): 779-782. https://doi.org/10.3870/yydb.2012.06.035
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    ABSTRACTObjectiveTo prepare epirubicin hydrochlorideloaded poly Llacticcoglycolic acid (PLGA) nanoparticles and investigate the characteristics. MethodsThe epirubicin hydrochlorideloaded PLGA nanoparticles were prepared by double emulsionsolvent evaporation method. The main effective factors such as the amount of PLGA, Tween80 in external water phase, and the ratio of poloxamer 188 to Tween80 were orthogonally designed. Drug entrapment efficiency, drug loading rate and drug utilization were determined. ResultsBy using the optimal formulation, the drug encapsulation efficiency of the nanoparticles was (32.6±1.2)%; the drug loading was (7.2±0.5)%; the drug utilization was (51.6±3.4)%; the mean size of the nanoparticles was 166.6 nm; the drug release continued 160 hours.ConclusionEpirubicin hydrochlorideloaded PLGA nanoparticles are prepared successfully and simply without use of polyviol and display sustained drug release properties.
  • 药物制剂与药品质量控制
    Preparation of Sparfloxacin pHSensitive in-situ Ophthalmic Gel and Its Corneal Penetration in Vitro
    DENG Xiang;HE Wen
    2012, 31(6): 783-785. https://doi.org/10.3870/yydb.2012.06.036
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    ABSTRACTObjectiveTo prepare sparfloxacin (SF) pHsensitive insitu ophthalmic gel (ISG) and study the corneal penetration in vitro. Methods0.3% carbopol and 14% poloxamer was applied as gel base to prepare the SFISG. The viscosity of the gel was determined. SF eyedrops at the same concentration served as control. Retention capability and corneal penetration of SFISG were studied in vitro.ResultsThe SFISG had the property of pseudoplastic fluid and the viscosity increased significantly with the increase of pH value. Compared with the SF eyedrops, the gel could significantly enhance the retention capability and corneal penetration in vitro (P＜0.05). ConclusionThe SFISG with promising pHsensitivity, retention capability and corneal penetration in vitro is valuable to be studied further.
  • 药物制剂与药品质量控制
    Measurement of Dynamic Viscosity of Methacrylic Acid Copolymer Ⅱ
    LU Ming;WANG Linbo;HAN Peng;CHEN Zhukang;YANG Meicheng;CHEN Guiliang
    2012, 31(6): 786-788. https://doi.org/10.3870/yydb.2012.06.037
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    ABSTRACTObjectiveTo study the rheology behavior of methacrylic acid copolymer Ⅱ and establish a method to measure its dynamic viscosity. MethodsDynamic viscosity was determined by malvern kinexus ultra concentric cylinder rheometer at a shear rate of 10 s－1 and 20 ℃. ResultsMethacrylic acid copolymer Ⅱ was newtonian fluid, whose dynamic viscosity was 5.06 mPa•s (RSD=0.25%, n=30). ConclusionThe method is convenient, accurate and of good repeatability to determine dynamic viscosity of methacrylic acid copolymer Ⅱ.
  • 药物制剂与药品质量控制
    Investigation on Influential Factors of Formulation of Capsule Shell of Compound Shenqi Soft Capsule
    WANG Chunyan;YANG Jianchun;CAO Dongmei;ZHENG Lina;LI Yunxia
    2012, 31(6): 788-790. https://doi.org/10.3870/yydb.2012.06.038
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    ABSTRACTObjectiveTo select an optimal capsule shell of compound shenqi soft gelatin capsule and study the effect of the formulation factor on the dissolution rate of gelatin shell. MethodsUV method was set up to determine the release of lemon yellow from the gelatin shell. The effect of some additions on the dissolution rate of gelatin shell was studied. ResultsThe results showed that the dissolution rate changed irregularly with the increase of the ratio of the gelatin to glycerine. The optimal formulation of capsule shell was gelatinglycerinwater, with a ratio of 1.0：0.4：1.0, containing 1.2% (volume) of citric acid, 0.4% (volume) of glycine, 0.2% (volume) of titanium and 0.2% (volume) of chocolate. ConclusionThe formula of the capsule shell of the compound shenqi soft gelatin is feasible and applicable for production.
  • 药物制剂与药品质量控制
    Content Determination of Asperosaponin VI in Qufengzhitong Capsules
    LI Daqing;WANG Manning;LIANG Xiaoli;WANG Xiaohong
    2012, 31(6): 791-792. https://doi.org/10.3870/yydb.2012.06.039
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    ABSTRACTObjectiveTo establish a method to determine the content of asperosaponin VI in qufengzhitong capsules by high performance liquid chromatograph (HPLC). MethodsDiamonsil C18 (2) chromatographic column (4.6 mm×250 mm, 5 μm) was used. Mobile phase consisted of acetonitrilewater (28：72). The flow rate was 1.0 mL•min－1. Detection wavelength was set at 212 nm. ResultsThe linear range of Asperosaponin VI was from 0.29 to 3.62 μg (r＝0.999 6). The regression equation was A＝172.46C－5.860 5. The average recovery was 98.4% (RSD＝0.58%). ConclusionThe method is simple, rapid and accurate, and can be used for the quality control of qufengzhitong capsules.
  • 药物制剂与药品质量控制
    Determination of Active Components in Concentrated Breast Pills by HPLC
    ZHAO Can;DUAN Hongzhang;ZHANG Qi;ZHANG Yanliu;SHAN Shiguang;QU Fujun;WANG Wei
    2012, 31(6): 793-798. https://doi.org/10.3870/yydb.2012.06.040
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    ABSTRACTObjectiveTo establish a method about highperformance liquid chromatography (HPLC) to determine concentration of germacrone, peoniflorin, saikoside (d), and ferulic acid in concentrated breast pills. MethodsConcentrated breast pills were prepared by ethanol and water extraction. DiamonsilC18 column (4.6 mm×200 mm, 5 μm) was used. Mobile phases of the four active components were as follows: germacrone, methyl cyanides: phosphoric acid solution (50：50, pH 3.23); peoniflorin, methanol: water (25：75); saikoside (d), methanol: methyl cyanides: water (20：35：45); ferulic acid, methanol: water: glacial acetic acid (32：68：0.5). Flow rate was 1.0 mL•min－1. Wavelength was 210, 230, 201 and 323 nm, respectively. Injection volume was 20 μL. Column temperature was 35, 25, 25 and 25 ℃, respectively. ResultsThe peak area of each of the active component showed a good linear relationship with the concentration in the corresponding linear range, r values were: 0.999 9, 0.999 85, 0.999 5, 0.999 5. The average extraction recoveries were: 75.91%, 82.38%, 75.04%, 67.67%. ConclusionThis method is simple and reliable; it can be used for the determination of active components in the concentrated breast pills.
    • 用药指南
  • 用药指南
    Study on Compatible Stability of Cefalotin Sodium for Injection in Three Kinds of Infusions
    WANG Ru;TONG Binliang;DUAN Liguang;YANG Shumin;YANG Jizhang
    2012, 31(6): 800-802. https://doi.org/10.3870/yydb.2012.06.042
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    ABSTRACTObjectiveTo study the compatibility stability of cefalotin sodium after mixing with fructose injection, invert sugar electrolyte injection and xylital injection.MethodsThe pH value and appearance were observed after cefalotin sodium mixing with 3 kinds of injections for 6 hours at (20±1) ℃, and the content of cefalotin sodium was determined by high performance liquid chromatography (HPLC). ResultsAppearance and the content of cefalotin sodium in xylital injection had no significant change within 6 hours, but the pH value decreased 0.5; appearance, the pH value and the content of cefalotin sodium in invert sugar electrolyte injection had no significant change within 6 hours; appearance and the pH value of cefalotin sodium in fructose injection had no significant change within 6 hours, but the content decreased. ConclusionCefalotin sodium mixed with the three kinds of injections at (20±1)℃ is stable. Cefalotin sodium mixed with fructose injection should be used within 2 hours.
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