Archive

• 01 November 2008 Volume 27 Issue 11

    

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  药物研究
  代谢性疾病用药专栏
  药物研究
  代谢性疾病用药专栏
  药物与临床
  药物制剂
  药品质量控制
  用药指南
  

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药物研究
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  药物研究

  Influence of CompatibilityDecoction Sequence on Medical Property of Zuojinwan and Fanzuojin by Microcalorimetry

  KONG Weijun;ZHAO Yanling;SHAN Limei;XIAO Xiaohe;GUO Weiying;LIU Jun

  2008, 27(11): 1287-1291.

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  ObjectiveTo investigate the influence of the sequence of "compatibilitydecoction" for rhizoma coptidis and fructus evodiae on medical property of zuojinwan and fanzuojin based on biophysics and biochemistry. MethodsMicrocalorimetry was used to analyze the thermogenic curves and parameters of Escherichia coli growth affected by zuojinwan and fanzuojin solution. In accordance with thermokinetic model, the relationships between k～c and I%～c of the drugs were fitted and IC50 were quantitated. The influence of the sequence of "compatibilitydecoction" on medical property of zuojinwan and fanzuojin was evaluated based on the literatures of ancient herbal. ResultsThe growth of Escherichia coli was improved by decoctions of fanzuojin, however inhibited by zuojinwan. IC50 of zuojinwan in "separated decoctioncompatibility" group (5.63 mg•mL1) was lower than that of "compatibilitycombined decoction" group (7.40 mg•mL1), which showed that the decoction of zuojinwan in "separated decoctioncompatibility" group was more effective. ConclusionMicrocalorimetry can be used to evaluate the influence of the sequence of "compatibilitydecoction" for rhizoma coptidis and fructus evodiae on the medical property of zuojinwan and fanzuojin.
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  药物研究

  The Effect of Integrin αvβ3 on Cell Proliferation and Invasive Ability of Osteosarcoma in vitro

  ZENG Heng;CHEN Anmin;LI Feng;YANG Caihong

  2008, 27(11): 1292-1293.

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  ObjectiveTo investigate the effect of integrin αvβ3 on cell proliferation and invasive ability of MG63 osteosarcoma cellline in vitro, so as to provide more experimental bases for treating osteosarcoma by antiαvβ3 integrin. Methods①The effect of various concentration of integrin αvβ3 monoclonal antibody on MG63 cells proliferation in vitro was detected by MTT method and SABC immunohistochemistry technique. ②The effect of various concentration of integrin αvβ3 monoclonal antibody on MG63 cells invasive ability in vitro was measured in the Boyden chamber invasive model. Results①The proliferation of MG63 osteosarcoma cells were markedly decreased by integrin αvβ3 monoclonal antibody in a dosedepended manner (P＜0.05). ②The invasive ability of MG63 cells was obviously inhibited by integrin αvβ3 monoclonal antibody in vitro in a dosedepended manner (P＜0.05), as well. Conclusion Integrin αvβ3 can positively regulate the cell proliferation and invasive ability of osteosarcoma, which provides more experimental bases for the glioma treatment by antiαvβ3 integrin.
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  药物研究

  Effect of Valerian Extract on Experimental Pulmonary Fibrosis in Rats

  CHEN Sumei;YANG Rongshi;ZENG Yulan;XUE Cunkuan

  2008, 27(11): 1295-1297.

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  ObjectiveTo evaluate the effects and mechanism of valerian extract on bleomycininduced pulmonary fibrosis in rats. MethodsWistar rats（irrespective of sex）were given a single intratracheal instillation of bleomycin at a dose of 5 mg•kg 1 to make a model of pulmonary fibrosis. 65 survival rats were randomly divided into four groups: highdose, lowdose（n=16, each）groups of Valerian, Colchicine group（n=16）and Model group (n=17). Each group was given the valeian extract at 100 mg •kg 1 and 20 mg •kg 1, 100 μg •kg 1 of colchicine and 10 mL• kg  1 of N.S. daily since the second day of model establishment. 6 rats were killed in each group on day 7, 10 rats were killed on day 28. Rats in control group (n=8) were instilled with saline intractracheally at a dose of 10 mL• kg  1and treated with N.S. 10 mL• kg 1. Rats in the control group were all killed on day 28. The right lower pulmonary lobes were harvested for HEstaining, and observed by Massonstaining. Expression of TGFβ1 was examined by immunohistochemistry and HYP was measured. Results3 rats（18.75%） were dead during experiment in the model group. Compared with the model, rats in valerian and colchicine groups showed attenuated alveolitis and lower expression of TGFβ1on 7 d （P＜0.05). The pulmonary fibrosis in valerian and colchicine groups was ameliorated on 28 d, and the contents of HYP was decreased as well, in comparison with those in the model group. ConclusionValerian extract could reduce the degree of alveolitis and fibrosis induced by bleomycin which may be due to suppression of TGFβ1.
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  药物研究

  Effect and Mechanism of Pentoxifylline on Peritoneal Function

  GONG Yanmei;ZENG Hongbing;LI Pengfei;LIU Xiaocheng;JIANG Yian

  2008, 27(11): 1298-1301.

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  ObjectiveTo investigate the effect and possible mechanism of Pentoxifylline in treating peritoneal function of SD rats. MethodsRats were randomly divided into three groups: the control（group A, given N.S. 20 mL daily）, model (group B) and pentoxifylline treated (group C), the two groups latter were i.p. 4.25%high glucose peritoneal dialysis fluid 20 mL, added in LPS at 8 d，10 d，12 d.Besides. rats in group C were treated with 6 mg•kg1 pentoxifylline daily. Five weeks later, the function of peritoneum was evaluated by a 2hour peritoneum equilibrium test (PET) and vascular endothelial growth factor (VEGF) in blood and dialysate was detected by ELISA method. Meanwhile, the expression of VEGF mRNA in mesenterium was detected by RTPCR method. ResultsGlucose reabsorption(D2/D0) and net ultrafiltration(UF) volume in group B and C were significantly lower than those in group A, especially for group B; Dialysatetoplasma urea ratio(D/Purea) in group B and C was significantly higher than that in group A, group B was more obvious. In group C, the concentration of VEGF in blood and dialysate was decreased obviously and VEGF mRNA in mesentery was down regulated, compared with those in group B. There were significant correlations between the concentration of VEGF in blood and dialysate and D/Purea, D2/D0, respectively. ConclusionPentoxifylline is beneficial to peritoneal function，the mechanism of which may be associated with decreased expression of VEGF.
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  药物研究

  A Pharmacokinetic Study of Omeprazole in Plasma by Liquid Chromatography Spectrometry

  LI Hongmei;ZHENG Heng;LI Feie;YANG Binbin

  2008, 27(11): 1301-0.

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  ObjectiveA sensitive and specific high performance liquid chromatography (HPLC) assay was developed to study the relative bioequivalence and bioavailability of omeprazole in plasma. MethodsTwenty volunteers were orally given with omeprazole capsules and enteric capsules as a standard, respectively, in a randomized crossover test. The concentration of omeprazole in plasma was determined by RPHPLC and pharmacokinetic parameters were calculated by DAS2.0 Software. ResultsThe pharmacokinetic parameters of the test and reference formulations were as follows: Cmax were (1 176.26±622.48) and (1 278.19±733.30) ng•mL1,AUC0→t were（3 514.80±3 353.86）and (3 800.49±3 566.14) ng•mL1•h，AUC0→∞ were (3 696.12±3 667.41) and（4 017.86±3 925.34) ng•mL1•h ,tmax were (2.65±0.93 )and (2.45±0.94) h. No significant difference for parameters of the two formulations was found. ConclusionThe two formulations are bioequivalent.
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  药物研究

  Effect of Estrogen Replacement on Expression of Vagina Hormone Receptor in Oophorectomized Rats

  WANG Hong;ZHANG Yuanzhen;LIU Wenhui

  2008, 27(11): 1304-1306.

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  ObjectiveTo investigate the effect of estrogen replacement on expression of vagina hormone receptor in oophorectomized rats and the molecular mechanism. Methods 40 SD Rats (12weekold) were randomly divided into four groups: contrast rats, sham operated rats, ovariectomized (OVX) rats, and ovariectomized rats with ERT (OVX+EV), 10 in each. The contrasts were normal rats, the sham operated rats were only cleared away fat tissues beside ovary with the same size of it. Meanwhile, both OVX and OVX+EV ones were ovariectomized. 3 weeks after ovariectomy, rats were treated with estradiol valerate 800 μg•kg1•d1 for 8 weeks. The expression of estrogen receptor α and β in vagina tissues was detected by immunohistochemistry. ResultsThe oophorectomized rats showed less ERα、ERβ expression than contrast ones in the vagina epithelial cell（P＜0.01), however, estrogen replacement therapy increased the expression（P＜0.01）. Conclusion Estrogen replacement therapy enhances expression of estrogen receptor, which strengthening the response of receptors.
代谢性疾病用药专栏
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  代谢性疾病用药专栏

  Effects of Jolethin on Calcitonin GeneRelated Peptide and Vascular Endothelial Growth Factor in Rats with Diabetic Nephropathy

  YAO Chunhong;WU Hanni

  2008, 27(11): 1314-1317.

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  ObjectiveTo investigate the protective effects of Jolethin on rats with experimental diabetic nephropathy and the possible mechanism underlying. MethodsThirty male Wistar rats were randomly divided into three groups: the normal control（NC），rats with diabetic nephropathy（DN）and diabetic rats treated with Jolethin（D＋J）. The rat model of diabetes mellitus was produced by injection of streptozocin（STZ）3 days after, rats in D＋J group were treated with Jolethin 0.9 mg•kg1•d1. After 8 weeks of the treatment，plasma levels of CGRP was measured by radioimmunoassay; the expression of VEGF in glomeruli were detected by immunohistochemical technique; UAER，Ccr，kidney weight∕body weight（KMI），body weight and blood glucose for 24 h were measured as well. ResultsCompared with those in the NC group，the plasma CGRP，Ccr and body weight were significant decreased （P＜0.01），nevertheless, the UAER，KMI，renal expression of VEGF and blood glucose for 24 h were obviously increased（P＜0.01）in the DN group. Compared with those in the DN group，rats in D＋J had significant higher Ccr（P＜0.05）and significant lower renal expression of VEGF（P＜0.01），except for CGRP.ConclusionJolethin has no significant effect on secretion of CGRP，but suppresses the overproduction of VEGF, which leading to prevention against diabetic nephropathy.
药物研究
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  药物研究

  Study on the Mutagenesis of Bellidifolin as a Hypoglycemic Component

  WEN Li;CHEN Jiachun

  2008, 27(11): 1317-1319.

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  ObjectiveTo investigate the genotoxicity of the active hypoglycemic component, Bellidifolin．MethodsBellidifolin was detected by Ames test, the micronucleus test in polychromatic erythocytes from bone marrow in vivo; and in TA97,TA98,TA100 and TA102 strains of salmonella typhimurium with or without the addition of liver microsomal enzyme activation system(+/S9) in vitro. ResultsNo obvious difference was found between groups of Bellidifolin and the negative control in the micronucleus test. It was showed that the number of rafutidine induced revertant colonies from different groups didn’t exceed over two times of those spontaneously formed under the condition with S9 or without S9 in Ames test. ConclusionNo mutagenicity was found in Bellidifolin in the test.

代谢性疾病用药专栏
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  代谢性疾病用药专栏

  The Effect of Hydrocortisone and Simvastatin on Contents of NFκB and ICAM1 in Aorta of Hypercholesterolemic Rats

  LIU Yougen;LU Fengming;ZHANG Song

  2008, 27(11): 1320-1323.

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  ObjectiveTo investigate the effect of hydrocortisone, simvastatin on contents of NFκΒ and ICAM1 in the aorta of hypercholesterolemic rats and its mechanism of preventing and treating atherosclerosis. MethodsSD rats were divided into the blank group，highfat diet group，hydrocortisone group，and simvastatin group. Rats in the blank group were fed with normal diet. Rats in other groups were fed with lipidrich diet and drugs. 16 weeks later, contents of TG, TC, LDL in serum were detected by the radioimmunity method. The internal membrane, muscular layer and ratio of positive cells with NFκΒ p65 and ICAM1 were observed by immunohistochemistry technique. ResultsThe aortic tunica intima and muscular layer in hydrocortisone group and simvastatin group were thicker than those in the highfat dietfed group, but thinner than those in the blank group. The ratio of the positive cell of NFκΒ p65 and ICAM1 in hydrocortisone group and simvastatin group were less than in highfat diet group, and larger than those in the blank. ConclusionBoth hydrocortisone and simvastatin have antiatherosclerosis effects, which could be attributed to inhibited activation of NFκΒ and secretion of ICAM1.
药物与临床
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  药物与临床

  30 Cases of Upper Respiratory Tract Symptom Caused by Common Cold Treated with Oral Solution of Pseudoephedrine Hydrochloride,Triprolidine Hydrochloride and Dextromethorphan Hydrobromide

  ZUO Peng;XIONG Shengdao;XIONG Weining;XU Yongjian;LIU Jin;ZHAO Jianping;XU Shuyun;LAN Fen

  2008, 27(11): 1334-1337.

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  ObjectiveTo evaluate the efficacy and safety of pseudoephedrine hydrochloride, triprolidine hydrochloride and dextromethorphan hydrobromide oral solution for treating upper respiratory tract symptom caused by common cold (rhinocleisis,nasal discharge,pharyngodynia,cough,expectoration). Methods60 patients with common cold were divided into the test group and control group and studied in a randomized, doubleblind and parallelism control way. The patients in the test group were administered with pseudoephedrine hydrochloride,triprolidine hydrochloride and dextromethorphan hydrobromide 10 mL q 8 h, and the patients in control were given with compound pseudoephedrine hydrochloride 10 mL q 8 h,for 3～5 days. The clinical efficacy and safety of the two groups were observed. ResultsThe total obvious effective rate of both groups was 93.33% and 89.66%, respectively, and the total effective rate were 96.67% and 96.55%, respectively. Moreover, the adverse events of drugs in the test group and control group were 2 cases (6.67%) and 3 cases (10.00%), respectively. There were no significant differences between two groups（P＞0.05）. The rate of improvement for expectoration in the test and control group were 97.69% and 88.10%, respectively, which showed that drugs in the test group was superior to those in the control. ConclusionThe oral solution of pseudoephedrine hydrochloride,triprolidine hydrochloride and dextromethorphan hydrobromide is effective and safe for the treatment of upper respiratory tract symptom caused by common cold ( rhinocleisis,nasal discharge,pharyngodynia,cough,expectoration).
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  药物与临床

  102 Cases of Acute Upper Respiratory Infection Treated with Lianhuaqingwen Capsule

  HU Ke;JIANG Yan;SHI Meijun;HU Chunhua;LIU Zhenlian;WAN Zhihui

  2008, 27(11): 1337-1340.

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  ObjectiveTo evaluate the efficacy and safety of lianhuaqingwen capsule for treating acute upper respiratory tract infection. MethodsThe clinical randomizedcontrolledtrails were conducted. VitC yinqiao tablets was used as control. A total of 206 subjects with acute upper respiratory tract infection were enrolled in our study, in which 102 patients randomly assigned in the treatment group were orally given lianhuaqingwen capsule (4 capsules, tid) for 3 d, and the other 104 patients were orally administered with VitC yinqiao tablets (2 pills,tid) for 3 d. ResultsThe clinical efficacy rates were 91.2% and 73.1% in lianhuaqingwen capsule group, and VitC yinqiao tablets group, respectively. Compared with control group, lianhuaqingwen capsule was more effective for improving main symptoms including fever, chill, headache and myalgia, with the therapeutic rates for whjch were 90.2%,85.4%,89.5%,91.0%, respectively. No significant difference on incidence of side effects in both groups was found (P＞0.05). ConclusionThe results suggest that lianhuaqingwen capsule is an effective and safe agent for treating acute upper respiratory tract infection, and is superior to VitC yinqiao tablets.
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  药物与临床

  Combine the Conservative Therapy with Naloxone for Sever Alcohol Withdrawal Syndrome

  FU Shouzhi;WU Hongyong;DU Xiaojuan;Wang Jialiang;LIU Yong

  2008, 27(11): 1340-1342.

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  ObjectiveTo evaluate the effectiveness and safety of naloxone combined with conservative therapy in the treatment of severe alcohol withdrawal syndrome. Methods50 patients with alcohol withdrawal syndrome were randomly assigned to naloxone group and control group. Each group has 25 patients. The control group received comprehensive conservative therapy. Naloxone group was given with a combination of naloxone with conservative therapy. The alleviation of symptoms and side effects were monitored. ResultsThe duration of symptoms was shorter in naloxone group versus the control group with a statistical significance（P＜0.01），and combination with naloxone reduced the dosage required for benzodiazepines and haloperidol（P＜0.01）. The combined therapy with naloxone decreased the need of sedatives, which may lead to hypersecretion of respiratory mucous. Moreover, there were no noticeable side effects. The prognosis was improved obviously, as well. ConclusionThe combination of conservative therapy with naloxone is an effective and safety treatment for alcohol withdrawal syndrome.
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  药物与临床

  21 Cases of Secondary Pulmonary Infection of Acute Leukemia Cotreated with Thymic Peptide α1

  WANG Jiru

  2008, 27(11): 1343-1345.

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  ObjectiveTo investigate the efficacy of thymic peptide α1 on secondary pulmonary infection of acute leukemia. MethodsThirtyeight patients with secondary pulmonary infection of acute leukemia were divided into two groups, the control group and thymic peptide α1 combined with antibiotic treatment group. Both groups were treated with antibiotics for two weeks, while the therapeutic group was s.c. treated with 1.6 mg thymic peptide α1 as well. The percentage of T lymphocyte subsets(CD+3 、CD+4 、CD+8) in peripheral blood was detected by direct immunofluorescence, and IL2,IL6 and INFα were analyzed by enzyme linked immunosorbent assay. The effect was carefully observed. ResultsIn the thymicpeptide α1treatment group, IL2,as well as the percentages of CD+3 、CD+4、and CD+8 increased significantly(P＜0.05and P＜0.01) and INFα was lowered (P＜0.01) after treatment. INFα of the control group was lowered(P＜0.05) while CD+4 significantly increased（P＜0.01）after treatment. Total effective rates were 90.4% and 70.5% for the treatment group and the control one, respectively（P＜0.05）. ConclusionThymic peptide promotes immune function of the infected patiens, by enhancing production of cytokines and improving the unbalance of cellular immunity.
药物制剂
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  药物制剂

  Modulation of Release Rates of Risperidone Loaded Microspheres by Mg （OH）2

  HU Zhenhua;YUAN Weien;WU Fei;WANG Bo;JIN Tuo

  2008, 27(11): 1374-1376.

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  ObjectiveThis paper focused on adjusting the release rates of risperidone from PLGA microspheres by coencapsulating Mg （OH）2. MethodsRisperidone loaded microspheres coencapsulated Mg （OH）2 were prepared by solidinoilinwater(S/O/W) emulsion solvent evaporation method. HPLC was used to determine risperidone loading capacity and evaluate the invitro release of microspheres. ResultsThe particles, about 50 μm, possessed well spherical shape. Mg （OH）2 accelerated the release rates of risperidone from PLGA microspheres. After 34 days, the percentage of released risperidone from microspheres with Mg （OH）2 was all more than 90%, but the control was not up to 70%. The in vitro release profiles of microspheres were various with different concentrations of Mg （OH）2 coencapsulated. ConclusionThe amount of Mg （OH）2 added into microspheres can improve the release behavior of risperidone from PLGA microspheres to achieve more perfect clinical effect.
药品质量控制
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  药品质量控制

  Study on the Stability of Ambroxol Nebulisation

  ZHAO Huanyu;WANG Xin;WANG Jing

  2008, 27(11): 1384-1385.

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  ObjectiveTo evaluate the compatible stability of main contents in the ambroxol nebulisation. MethodsAmbroxol nebulisation was prepared according to the prescription and stored at 2－8 ℃. The appearance of the solution was observed at 0,1,2,3,4 d. Ambroxol Hydrochloride and dexamethasone sodium phosphate were determined by RPHPLC. ResultsNo obvious change was noted in appearance within 5 days. The main contents consistently remained over 96%. ConclusionNebulisation could be stable at 2－8 ℃ and used within 5 days.KEY WORDSNebulisation；Stability；Ambroxol hydrochloride；Dexamethasone sodium phosphate
用药指南
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  用药指南

  Genotype and Drug Resistance of Klebsiella Pneumoniae from Hubei Expressing CTX-M Extended Spectrum Betalactamase

  MEI Siqing;LI Congrong;HUANG Jun;LV Xia;PENG Shaohua

  2008, 27(11): 1407-1410.

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  ObjectiveTo explore the transmission mechanisms of Klebsiella pneumoniae from Hubei expressing CTXM βlactamases, providing bases for rational use of antibiotics in clinic. MethodsA total of nonrepetitive 70 K.pneunoniae producing ESBLs were detected by phenotypic confirmatory test based on NCCLS criteria. PCRRFLP and DNA sequencing were carried out for blaCTXM typing; Susceptibility of the CTXM producing strains to 9 antibiotics was performed through a disk diffusion test; DNA homology of clonal strains was analyzed by plasmid transfer experiments and RAPD. ResultsThe incidence of CTXM expression was 46% in ESBLsproducing isolates, all of which was CTXM1 subtype, and CTXM3 was the most common type. The strains with CTXM were resistant to a lot of antibiotics, but 100% sensitive to imipenem. The resistance mediated with ESBLs in CTXM strains was horizonly transferred. The strains were from different clones by DNA homological analysis. ConclusionImipenem could be the drug of first choice for treating K.pneumoniae with CTXM βlactamasesproducing strains. The transmission of CTXM producing strains is mainly mediated by plasmids, which forces us to intensify the detection of ESBLs strains with CTXM type in Hubei province.