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    药物研究
  • 药物研究
    Inhibitory Effect of Rhein on Cytochrome P450 Activity of Rat Liver Microsomes
    LI Dan;HAN Yonglong;MENG Xiangle;SUN Xipeng;YU Qi;GUO Cheng;
    2010, 29(3): 282-285.
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    (1. ABSTRACTObjectiveTo evaluate the effects of rhein on the activity of cytochrome P450 3A(CYP3A) enzyme of rat liver microsomes. MethodsRat liver microsomes were incubated with various concentrations of rhein and testosterone in vitro. The inhibition of CYP3A activity by rhein was evaluated by the amount of 6βhydroxytestosterone which was determined by HPLC. ResultsRhein suppressed the CYP3A activity in rat liver microsomes, with IC50 =36.74 μmol•L1 and Ki=20.73 μmol•L1, respectively. ConclusionRhein could decrease the enzyme activity of rat liver CYP3A in vitro.
  • 药物研究
    Determine the Serum Concentration of Carbamazepine in Patients with Epilepsia by HPCE and FPIA
    XIE Hua;WANG Rong;JIA Zhengping;XU Liting;ZHU Fangli;WANG Juan
    2010, 29(3): 286-288.
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    （1. ABSTRACTObjectiveTo set up a method to determinate the serum concentration of carbamazepine in patients with epilepsia by highperformance capillary electrophoresis (HPCE) and compare the two ways of carbamazepine determination in sera by HPCE and fluorescence polarization immunization（FPIA）. MethodsThe uncoated fusedsilica capillary (27 cm×75 μm) was used in HPCE. The electrophoresis condition included the 30 mmol•L1 Na2HPO4(pH=8.0) containing 75 mmol•L1 SDS as buffer, running voltage 18 kV, temperature at 30 ℃, UV detection at 280 nm and pressure for injection as 10 s. The sample was extracted by ethyl acetate, and the upper extract was evaporated to dryness with nitrogen. The residue was resolved by running buffer, sample was injected by pressure for 10 s. The standard TDx operation was used in FPIA. ResultsThe good linear relation with peak area in carbamazepine determination by HPCE was obtained within 2.188－100.000 μg•mL1 (r=0.998 9). Intraday RSD and interday RSD were less than 5%. ConclusionHPCE is simple, rapid and sensitive, with no significant difference from FPIA, and it is more suitable for routine blood drug monitoring at low cost.
  • 药物研究
    Effect of Intraarticular Injection of Recombinant Human Acidic Fibroblast Growth Factors on Expression of Matrix Metalloproteinases1 in Cartilage and Synovium of Early Traumatic Arthritis Model in Rats
    WANG Ning;BAI Xiangjun;YI Chengla;LIAO Yiliu;HU Duan;CHEN Jige
    2010, 29(3): 289-292. https://doi.org/10.3870/yydb.2010.03.005
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    ABSTRACTObjectiveTo explore effect of intraarticular injection of recombinant human acidic fibroblast growth factors on the expression of matrix metalloproteinases1 in cartilage and synovium of early traumatic arthritis(TA) model in male SD rats. Methods24 male SD rats were randomly divided into blank group (n= 8), experimental group (n= 8) and drug interventional group (n= 8). The animal models of TA were developed through transection of the medial collateral ligament plus partial medial meniscectomy in male SD rats. 1 μg rhaFGF was injected into articular cavity during or one week after operation. Two weeks after the operation, rats were sacrificed, HE staining was applied to observe the changes of the structure of cartilage and synovium, and immunohistochemical staining was applied to detect MMP1 expression in cartilage and synovium. ResultsThe expression of MMP1 in cartilage and synovium in the experimental group increased significantly as compared with the blank group,while the expression of which in articular cartilage and synovial membrane was abated. ConclusionIntraarticular injection of rhaFGF can reduce the expression of MMP1 in articular cartilage and synovial tissue of early traumatic arthritis rats, and inhibit the degeneration of articular cartilage and inflammation of the synovial tissues.
  • 药物研究
    Antioxidant Activity of Flavonoids from Stenoloma chusanum（L）. Ching in vitro
    WU Xiaoning;YU Chenhuan;XU Jinghong
    2010, 29(3): 292-294. https://doi.org/10.3870/yydb.2010.03.006
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    (1. ABSTRACTObjectiveTo investigate the antioxidant activity of flavonoids from Stenoloma chusanum (L.) Ching in vitro.MethodsThe radical scavenging, total antioxidant and reducing capacity of hydroxy radicals and lipid peroxides by the total flavonoids from Stenoloma chusanum(L.)Ching were detected and analyzed by using spectrophotometry and multiple linear regression analysis. The correlation between contents of total flavonoids and their antioxidant activity in vitro was surveyed. ResultsThe extracts showed strong antioxidant activities, free radical clearance and some reduction ability, by efficiently inhibiting lipid peroxidation in a dose dependent manner. ConclusionThe total flavonoids may be the main active component of Stenoloma chusanum (L.) Ching which exerting an antioxidative activity.
    • 抗结核病药物专栏
  • 抗结核病药物专栏
    Features of Death from Human Immunodeficiency Virus Infection Complicated with Tuberculosis
    HUANG Shaoping;LU Shuihua;LU Hongzhou
    2010, 29(3): 295-297. https://doi.org/10.3870/yydb.2010.03.007
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    ABSTRACTObjectiveTo compare clinical features of patients coinfected with human immunodeficiency virus (HIV) and mycobacterium tuberculosis（TB）who died during hospitalization. Methods43 patients admitted with HIV/TB who died during hospitalization and 67 patients died of TB but no HIV simultaneously, from Shanghai Public Health Clinical Center Affiliated to Fudan University from January 2005 to June 2009 were collected. Both groups were compared by the casecontrol study method. ResultsExtrapulmonary tuberculosis, combined with fungal infection and CD+4 cell declined (≤200 cell•μL1) in HIV/TB infection group were more obvious than those in the control group(P＜0.05); on the other hand, low positive rate of sputum bacteria smear and culture, high rate of multidrug resistance and cavity in lung were significantly lower that those in the control（P＜0.05）. ConclusionExtrapulmonary tuberculosis, fungal infections and CD+4 cell declining (≤200 cell•μL1) are common to be found in HIV/TB dual infected cases who finally died. While the cavity in lungs and the positive rate of bacteria in sputum is rare to be seen. The multidrug resistance is not the key feature to cause the death of TB/HIV dual infected patients.
    • 药物与临床
  • 药物与临床
    A Contrast Research of Concurrent Chemoradiotherapy by Capecitabine and 5Fluorouracil for Gastric Cancer
    QIU Hong;DING Fangyong;XIONG Huihua;LI Ruichao
    2010, 29(3): 306-309. https://doi.org/10.3870/yydb.2010.03.012
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    (1. ABSTRACTObjectiveTo investigate the shortterm adverse reactions and influence on the quality of life (QOL) of concurrent chemoradiotherapy of capecitabine and 5fluorouracil on gastric cancer. Methods67 patients who were eligible for concurrent chemoradiotherapy for gastric cancer were enrolled into study. The radiation dose was 45 Gy. 37 patients received capecitabine ［1 650 mg•（m2）-1•d-1］ as radiosensitizer, and 30 patients received 5fluorouracil ［400 mg•（m2）-1•d-1］, during the initial 4 days and 3 days before the completion of radiotherapy. The Chinese EORTC QLQ30 was used to evaluate the QOL of patients before and after radiotherapy. ResultsThe common adverse reactions appeared in both groups were myelosuppression, nausea and anorexia. Handfoot syndrome occurred in 12 patients of capecitabine group. In capecitabine group, scores of psychological dimension, family and social dimension, and selfevaluation of QOL were superior to 5fluorouracil group. ConclusionsAs a radiosensitizer for the postoperative concurrent chemoradiotheraphy of gastric cancer, capecitabine was superior to 5fluorouracil regarding to influence on QOL. Capetabine is worthy to be generalized as a standard treatment for the concurrent chemoradiotheraphy for gastric cancer.
  • 药物与临床
    Treatment of 80 Cases of Chronic Pulmonary Heart Disease Following Rapid Ventricular Tachycardia by Diltiazem
    SHEN Sanying;CAI Yifang ;PENG Dingfeng
    2010, 29(3): 309-311. https://doi.org/10.3870/yydb.2010.03.013
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    (1. ABSTRACTObjectiveTo investigate the effect of diltiazem in the treatment of acute outbreak of chronic pulmonary heart disease following rapid ventricular tachycardia. Methods158 patients with acute outbreak of chronic pulmonary heart disease following rapid ventricular tachycardia were selected and randomly divided into the treatment group and control group. 80 cases in treatment group were injected intravenously with 0.25 mg•kg1 diltiazem first, then infused at 5－15 mg•h-1 or administered with diltiazem orally to control ventricular velocity. 78 cases in the control group were injected intravenously 0.2－0.4 mg•d1 with cedilanid, given digoxin 0.125－0.250 mg•d1 orally, and treated later in the same way as the treatment group. ResultsThe ventricular velocity was well controlled and cardiac function, clinical symptom and signs were significantly improved in the treatment group compared with the control (P＜0.05). ConclusionDiltiazem is efficient in treatment of chronic pulmonary heart disease following rapid ventricular tachycardia, with favorable safety and tolerability.
  • 药物与临床
    Comparative Study of Propofol Combined with Remifentanil or Fentanyl during Painless Abortion
    JIA Ruifang;FU Yanfang;MENG Xiaoyan;ZUO Mingzhang
    2010, 29(3): 313-316. https://doi.org/10.3870/yydb.2010.03.015
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    ABSTRACTObjectiveTo compare the therapeutic effects of using propofol combined with fentanyl or remifentanil in painless abortion. Methods90 pregnant women who selected painless abortion were randomly divided into three groups, 30 in each group. Group L was given with 2% lidocaine 40 mg first, then injected intravenously with propofol 2 mg•kg1 30 s later. Group F and group R were separately given with fentanyl 1 μg•kg1 and remifentanil 1 μg•kg1, then injected intravenously with propofol 1.5 mg•kg1 after 2 minutes or 30 s, respectively. Propofol was added in accordance with the dynamic response. The recovery time, wakeup time, infusion pain, body movement, dose of propofol, numbers of patient who needed additional propofol, the analgesia effects, HR and MAP at different time during the whole operation were investigated. ResultsThe doses of propofol in group F and group R were less than those in group L（P＜0.01）, there were fewer cases received additional propofol in group R than group F and group L（P＜0.05）, the wakeup time was shorter in group R and group F compared with group L（P＜0.01）, the scale of infusion pain in group R was much better than that in group F and group L（P＜0.01）.ConclusionThe effect of propofol combined with remifentanil was better than the other two methods in painless abortion.
    • 药物制剂
  • 药物制剂
    Optimization of Preparation of Indomethacinβcyclodextrin Inclusion Complexes
    LI Fei;HAO Jifu;WANG Jianzhu;GUO Fengguang;HAO Liyong
    2010, 29(3): 350-352. https://doi.org/10.3870/yydb.2010.03.029
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    ABSTRACTObjectiveTo optimize the preparation of indomethacinβcyclodextrin inclusion complexes using coprecipitation method. MethodsEffects of molar ratio of indomethacin (IDM) to βcyclodextrin(βCD), inclusion temperature and polarity of the medium on complex formation were evaluated by orthogonal test. The complexation of indomethacin in the inclusion complexes was identified by differential scanning calorimetry (DSC) and the optimized conditions of preparation were determined. Results It was revealed that the complexes were formed and the dissolution rate of the drug was increased significantly. The optimal conditions were as follows: inclusion temperature was 60℃, IDM: βCD was in a 1：1.5 molar ratio, acetone/water was 1：4. Under this condition, the inclusion efficiency could reach 98.5%. ConclusionInclusion temperature is the most significant factor influencing formation of the complexes among the three factors as inclusion temperature, molar ratio of IDM: βCD and proportion of organic solvent to water.
  • 药物制剂
    A Comparative Study of Preparation for Gucha Jiangzhi Capsule by Using the Wet （highefficient） Mixing Granulation and Pendular Granulation
    CAO Yan;FAN Yanbo;ZENG Qingfeng;HONG Yi;FANG Nianbai;YU Shanggong
    2010, 29(3): 353-355. https://doi.org/10.3870/yydb.2010.03.030
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    ABSTRACTObjectiveTo optimize the granulation process for preparing Gucha Jiangzhi capsule by different methods of wet（highefficient）mixing granulation and pendular granulation. MethodsGucha Jiangzhi capsule was produced by wet（highefficient）mixing granulation and pendular granulation, respectively, and the nature of particles, filling capacity and load were compared. ResultsParticles which obtained by highefficient mixing granulation were in uniform dense, highvolume filling, and conforming to the load difference of formulation. ConclusionHighefficient mixing granulation is a feasible and efficient method, and it could provide the guidance for granulation of gucha jiangzhi capsule.
  • 药物制剂
    Optimization of Extraction for Total Flavone in Congbai
    WANG Wei;ZHANG Changgong
    2010, 29(3): 357-359. https://doi.org/10.3870/yydb.2010.03.035
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    (1. ABSTRACTObjectiveTo optimize the extraction process for total flavone in congbai. MethodsThe optimum extracting technics for total flavone from congbai was screened out by adopting single factor and orthogonal design experiment to evaluate the extraction efficiency of total flavone. ResultsThe optimal extraction process was as follows: refluxed the powdered herbs with diameter less than 0.175 mm by using 10 times more 80% ethanol at 80 ℃ for three times, 2 hours each time. ConclusionThe optimal extraction process is stable and suitable for isolating the total flavone from congbai.
  • 药物制剂
    Optimization of Extracting Technics for Isolating Total Alkaloids and Dehydrocavidin from Corydalis saxicola Bunting
    WANG Jing;LU Tulin;MAO Chunqin;HU Fang;HUANG Wei
    2010, 29(3): 360-363. https://doi.org/10.3870/yydb.2010.03.032
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    ABSTRACTObjectiveTo optimize the extracting technics for isolating total alkaloids and dehydrocavidin from Corydalis saxicola Bunting by orthogonal design. MethodsCorydalis saxicola Bunting was extracted with ethanol or acid by reflux and percolation, respectively. Then the four factors caused the quantity and concentration of solvents, extracting time and frequency were optimized. ResultsThe ethanol refluxing process was better than other processes for isolating total alkaloids and dehydrocavidin from Corydalis saxicola Bunting. The optimal condition was as follows: extracted the crude drug with 10 times more 75% ethanol for 3 times (120 min/time). ConclusionThis optimized extraction process is simple, stable and feasible.
    • 药品质量控制
  • 药品质量控制
    Determination of Atractylenolide Ш Contents in Xiangsha Yangwei Tablets by HPLC
    CHEN Qinhua;LI Peng;YI Yong
    2010, 29(3): 365-367. https://doi.org/10.3870/yydb.2010.03.034
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    ABSTRACTObjectiveTo establish a method for determination of atractylenolide Ш contents in xiangsha yangwei tablets by HPLC. MethodsUsing the highperformance liquid chromatography (HPLC) determination method: a column was Kromssil C18 column (4.6 mm × 250 mm, 5 μm), the mobile phase was methanolwater (60：40), the flow rate was 0.8 mL•min1and the detection wave length at 220 nm. ResultsThere was good linearity between the peak area and the content of atractylenolide Ш in the rang of 1－50 μg•mL1; the average recovery of sample was 99.61% (RSD：1.67%). ConclusionThis method is simple, sensitive, accurate and reliable for the content determination of atractylenolide Ш in xiangsha yangwei tablets.
  • 药品质量控制
    Content Determination of Nuciferine in Folium Nelumbinis Oral Liquid by RPHPLC
    FANG Jianguo;LI Yanyan;WAN Jin;WANG Wenqing;WANG Qiulan
    2010, 29(3): 367-369. https://doi.org/10.3870/yydb.2010.03.036
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    ABSTRACTObjectiveTo establish a RPHPLC method for content determination of nuciferine in Folium nelumbinis oral liquid. MethodsReversephase high performance liquid chromatography (RPHPLC) was carried out with a HypersilBDS C18 column (4.6 mm×150 mm,5 μm) at 40 ℃. Mixture of methanolwatertriethylamideacetic acid (50：48：1.4：0.7) was used as mobile phase at a flow rate of 0.7 mL•min1 with detection at 270 nm. ResultsNuciferine showeded a good linear at the range of 1.282－25.640 μg•mL1(r=0.999 1). The average recovery was 99.7%（RSD=1.25%），101.0%(RSD=0.95%) and 99.5%(RSD=1.14%), respectively. ConclusionThe method is accurate, sensitive and can be used for the quality control of Folium nelumbinis oral liquid.
  • 药品质量控制
    Determination of Residual Ｓolvents in Roxithromycin by CGC
    WANG Jian;LIU Yongmei;LI Yinghong
    2010, 29(3): 369-371. https://doi.org/10.3870/yydb.2010.03.037
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    ABSTRACTObjectiveTo establish a headspace capillary gas chromatography(CGC) method for the determination of residual solvents in roxithromycin. MethodsResolved the sample in dimethyl sulfoxide. Methanol and acetone in roxithromycin were separated by DB624 capillary column（30.0 m×0.53 mm, 3.0 μm）through headspace injection. The column temperature was maintained at 40 ℃ for 5 min, then rose to 200 ℃ at the rate of 30 ℃•min1 and maintained at 200 ℃ for 3 min. Acetic acid and dimethylformamide in roxithromycin were separated by DB624 capillary column（30.0 m×0.53 mm,3.0 μm）through direct injection. The column temperature was maintained at 100 ℃ for 6 min, then raised to 200 ℃ at the rate of 30 ℃•min1 and maintained at 200 ℃ for 5 min. ResultsThe residual solvents was separated completely. The calibration curve of each solvent showed a good linear relationship with fine precision and accuracy. ConclusionsThis method is accurate and reliable. It can be used for the determination of residual solvents in roxithromycin.
  • 药品质量控制
    Content Determination of Hesperidin in Qufeng Mixture by HPLC
    JIANG Zhengli;HE Ren;JIANG Xiao
    2010, 29(3): 372-374. https://doi.org/10.3870/yydb.2010.03.038
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    ABSTRACTObjectiveTo establish a method for content determination of Hesperidin in qufeng mixture by HPLC. MethodsA Hypersil ODS2 (250 mm×4.6 mm，5 μm) column was used at normal temperature. A mixture of methyl alcohol and water (45：55) was used as mobile phase delivered at a flow rate of 1.0 mL•min1 with detection at 283 nm. ResultsHesperidin was shown a good liner relationship at the range of 4.63～23.16 μg•mL1（r＝0.999 5) with a average recovery at 99.0% and RSD at 1.80%. ConclusionThis method is reliable, simple, accurate and can be applied for the quality control of qufeng mixture.
  • 药品质量控制
    Content Determination of Gluconate Zinc, Ferrum and Calcium in a Compound Oral Solution by Atomic Absorption Spectrometry
    MA Yonggui;WAN Jin;WANG Wenqing;FANG Jianguo
    2010, 29(3): 374-376. https://doi.org/10.3870/yydb.2010.03.039
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    ABSTRACTObjectiveTo establish a atomic absorption spectrometry(AAS) method for content determination of zinc, ferrum and calcium in compound zinc gluconate，ferrous gluconate and calcium gluconate oral solution. MethodsThe sample was digested with nitric acid and the content of zinc, ferrum and calcium was determined by FAAS method.ResultsGood linearity, precision and accuracy of zinc, ferrum and calcium were observed in this method. The average recovery of zinc, ferrum and calcium were 99.7%(RSD1.72%), 99.5%(RSD0.72%) and 100.2%(RSD1.17%) (n=9), respectivelly. ConclusionThis method is simple，accurate and rapid. It can be used for quality control of zinc, ferrum and calcium in compound zinc gluconate，ferrous gluconate and calcium gluconate oral solution.
    • 用药指南
  • 用药指南
    Compatible Stability of Cefoselis Mixed with Five Hemostatics
    LUO Songmei;TIAN Weiqiang;HUA Junyan;WU Jiajia
    2010, 29(3): 383-387. https://doi.org/10.3870/yydb.2010.03.043
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    (1. ABSTRACTObjectiveTo study the compatible stability of cefoselis with five hemostatics, which are PAMBA, etamsylate, carbazochrome sodium sulfonate, vitamin K1 and tranexamic acid. MethodsThe appearance, pH value and content of cefoselis mixed with five hemostatics for eight hours were studied by Kratio UV and dualwavelength analysis at different time points. ResultsNo significant changes in the appearance, pH value and content of cefoselis were observed after mixing with five hemostatics for eight hours. ConclusionSulfate cefoselis is stable eight hours after mixed with five hemostatics in 0.9% sodium chloride injection.
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