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    特约稿
  • 特约稿
    CAO Lili;ZHENG Xiuyan;DU Guanhua
    2004, 23(4): 207-0209.
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    Sivelestat is a newly developed elastase inhibitor which has been shown to have good protective effect on the lung tissue during acute experimental pulmonary injury. The underlying mechanisms of its effect are different from those of steroid drugs now available. It seems possible that sivelestat may be capable of selectively inhibiting elastase and depressing infiltration of inflammatory cells in the alveoli, and thereby exerting protective effects on vascular endothelium and pulmonary tissues injured by elastase.
  • 药物研究
  • 药物研究
    XIANG Min;WANG Guanglian;DING Longqi
    2004, 23(4): 213-0214.
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    To study the protective effect of qingganying (QGY) decoction on the murine liver injured by pacetaminophen (AAP). Methods:A murine model of liver injury induced by AAP served as the subject of the study. Changes in activities of alanine amiontransferase(ALT) and aspartate aminotransferanse(AST) as well as levels of total bilirubin in sera of the mice were kept under observation. Hepatic histopathology was also studied. Results:All three doses of QGY were shown to inhibit the activity of AST, medium dose (crude drug 28 g·kg1) and large dose (crude drug 56 g·kg1) of QGY were found to decrease the activity of ALT and lower the level of total bilirubin. Pathological sections revealed zonular necrosis and diffuse anomalies of hepatic cells in the liver of the AAP murine model untreated with QGY. In the liver of mice treated with large doses of QGY, the structure of the lobule of liver was intact and clear. Punctate necrosis of only a few hepatocytes and infiltration of a small number of lymphocytes were demonstrated. The degree of injury was relatively mild, as compared with that of the untreated model group. Conclusion:QGY decoction was shown to exert a certain protective effect on the liver injured by AAP in mice.
  • 药物研究
    CHEN Daiyong;ZHAO Miao;ZANG Zhihe;SUN Xizheng;ZHU Weidong
    2004, 23(4): 215-0216.
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    To study the factors influencing the release mechanism of rutin from sustainedrelease matrix tablets. Methods:The sustainedrelease matrix tablets of rutin were prepared by using hydroxypropylmethyl cellulose (HPMC) as the matrix material. The effects of the amounts of HPMC, microcrystalline cellulose (MCC) and pregelatinized starch on the in vitro drugrelease of rutin from the sustainedrelease matrix tablets were appraised with the release index n value of the Peppas empirical formula. Results:The rate of drug release was slowed down along with the increase of the content of HPMC. Addition of both MCC and pregelatinized starch speeded up the rate of rutin release from the tablets. Conclusion:The contents of HPMC, MCC and pregelatinized starch were shown to influence the release mechanism of rutin. Among these, the content of HPMC appeared to have the most pronounced effect.
  • 药物研究
    FANG Shungan
    2004, 23(4): 217-0218.
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    To probe into the best technology for the inclusion of Pacetaminophen(AAP) with betacyclodextrin(βCD). Methods:The 3 major factors influencing the inclusion ofAAP with βCD, namely inclusion ratio, time of stirring and inclusion temperature were subjected to analysis of variance and range analysis with the use of an orthogonal test in order to optimize the best condition for inclusion technology. Results:Data of the range analysis were RA>RB>RC; factor A: K3>K2>K1; factor B: K1>K2>K3; factor C: K3>K1>K2. The ratio of AAP to βCD was shown to exert a striking effect on the inclusion content(P<0.05). Changes in time of stirring and temperature showed little influence on the inclusion content(P>0.05).Conclusion:The best conditions for the inclusion technology were shown to be: the ratio of AAP to βCD, 1∶3; the time of stirring, 6 h and the inclusion temperature, 40℃.
  • 药物研究
    MA Pingbo;HUANG Zhongwei
    2004, 23(4): 220-0221.
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    To study the effect of different penetration enhancers on the percutaneous permeability of compound ketoconazole cream in vitro. Methods:Isolated rat skin was taken as the permeable barrier by using a modified simple cell device. The content of ketoconazole was dertermined with HPLC. The accumulative total percentage of percutaneous permeability was calculated. Results:All of the five penetration enhancers were shown to increase the penetration of ketoconazole in the cream. Conclusion:3% dipentane(DP)+1.5% azone was found to have the best penetration enhancing effect, followed successively by 3% DP, 3% menthol(M), 1.5% DP+1.5% M and 2% azone.
  • 药物研究
    ZHANG Dunlan;JIN Zhichun;TAN Gongping;LI Hui;SHAO Dongshan;XIONG Fuliang
    2004, 23(4): 222-0224.
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    To probe into the basis of the pharmacodynamics of penqiangshu capsules in the treatment of chronic pelvic inflammation by observing the effect of the drug on the immune function and microcirculation in experimental animals. Methods:To appraise the influence of penqiangshu capsules on the immune function, their effects on the phagocytic function of peritoneal macrophage of the mouse, clearance of autologous blood clot in the abdominal cavity of the rabbit etc. were assayed. For the assessment of the influence of penqiangshu capsules on the microcirculation, their effects on the number of crossings in the capillary network of the mesenteric microcrculation, flow rate of blood in arteries in the mouse etc. were examined. Results:Penqiangshu capsules were shown to strikingly enhance the phagocytic function of macrophages from the abdominal cavity of the mouse, the effect being better than that of fukeqianjin tablets and close to that of levamisole. The drug was also shown to promote the absorption and clearance of autologous blood clot in the abdominal cavity of the rabbit, the effect being better than that of fukeqianjin tablets. These findings suggested that penqiangshu capsules had a fairly good effect of enhancing immune function. The effect of penqiangshu capsules in ameliorating microcirculation was shown to be better than that of fukeqianjin tablets and close to that of anisodamine.Conclusion:Penqiangshu capsules were shown to exert a series of pharmacological effects including enhancement of immunity, amelioration of microcirculation, activating blood flow and removing blood stasis.
  • 感染性疾病用药专栏
  • 感染性疾病用药专栏
    WANG Lihua;ZHANG Jingliang
    2004, 23(4): 225-0226.
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    To probe into the clinical therapeutic effectiveness and adverse reactions of cerebroprotein hydrolysate as an adjunct to the routine measures for the treatment of epidemic encephalitis B. Methods:70 patients with epidemic encephalitis B were randomly divided into 2 groups, the treatment group(n=36)and control group(n=34). On the basis of routine combined treatment including oxygen inhalation, antifebrile measures, sedation, control of convulsion, dehydration with mannitol, rational use of respiratory stimulants and energy mixtures to combat respiratory failure supported by sputum aspirator and respirator, patients of the treatment group were given each 10~20 mL of cerebroprotein hydrolysate added to 250 mL of 5% glucose solution administered by IV instillation, q.d.. The patients were subjected to 2 courses of treatment, with each course lasting 14 days. Patients of the control group were submitted only to the routine combined treatment. The course of treatment was the same as that of the treatment group. Results:By the termination of the course of treatment, the overall effective rates were 91.7%and 61.8% for the treatment group and control group, respectively. The therapeutic effectiveness in patients of the treatment group was superior to that of the control group (P<0.05). No distinct adverse reactions were encountered. Conclusion:Cerebroprotein hydrolysate was shown to have definite therapeutic effectiveness in the treatment of epidemic encephalitis B and is therefore worth spreading its clinical application.
  • 感染性疾病用药专栏
    SUN Weihua
    2004, 23(4): 227-0228.
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    To probe into the clinical therapeutic effectiveness of artesunate in the treatment of cerebral malaria. Methods:64 patients with cerebral malaria diagnosed by demonstration of plasmodium falciparum in thick drop blood smears were randomly divided into 2 equal groups. Patients of the treatment group (n=32) were given each an initial dose of 2.4 mg·kg1 of artesunate dissolved in 1 mL of 5% sodium bicarbonate solution and added to 10 mL of 5% glucose solution administered by slow IV injection. 12 h later, a second dose of 1.2 mg·kg1 of artesunate was given in the same way. For the succeeding 6 days, a daily dose of 1.2 mg·kg1 of artesunate was given in the same manner to each of the patients of the treatment group. Patients of the control group (n=32) were given each an initial dose of 20 mg of quinine dissolved in 500 mL of 5% glucose solution administered by IV instillation, which was completed within 4 h. 8 h later, a second dose of 10 mg·kg1 of quinine was given in the same way. Thereafter, 10 mg·kg1 of quinine was given q.8.h. in the same manner until the patients could take medicines by mouth. Quinine tablets in a dose of 10 mg·kg1 were then given q.8.h. PO to each patient of the control group until a course of treatment of 7 days was completed. Results:Artesunate started to act quickly, being rapid to control the symptoms of malaria. The cure rates on the 7th day of the treatment were 90.6% and 87.5% in the artesunate group and quinine group,respeclively, the difference being insignificant(P>0.05). The times of abatement of fever were 24 h and 48 h, and those of blood plasmodium elimination were 30 h and 60 h in patients of the artesunate group and quinine group,respectively,the differences being highly significant(P<0.01). Conclusion:Both artesunate and quinine were shown to be effective in the treatment of cerebral malaria. However, artesunate was found to act more quickly in the treatment of pernicious cerebral malaria, with only mild side effects. It is also effective in the treatment of malaria caused by quinineresistant strains of malaria parasites. It should be the drug of first choice in the treatment of malaria that quinine fails to effect a cure.
  • 感染性疾病用药专栏
    LI Zhiliang;WEI Jia;XIE Junqiang;CHONG Yutian
    2004, 23(4): 229-0231.
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    TO appraise the therapeutic effectiveness of traditional Chinese medicines in the treatment of severe chronic viral hepatitis B. Methods:148 patients with severe chronic viral hepatitis B served as the subject of the study. Among these, 65 patients suffered from severe chronic viral hepatitis B, 29 cases of which received only conventional therapy while the other 36 were subjected to treatment with traditional Chinese medicines on the basis of the conventional therapy. 32 patients suffered from severe viral hepatitis B associated with hepatic failure. Of these, 18 patients had received decoction treatment longer than one week before admission, while the other 14 had not been treated with traditional Chinese medicines prior to admission. All these 32 patients were subjected to treatment with traditional Chinese medicines. The remaining 51 patients in the restoration stage of severe hepatitis associated with hepatic failure were discharged from our hospital from March 2000 to June 2002. Of these, 27 patients were treated with traditional Chinese medicines while the other 24 were not. For the treatment of chronic viral hepatitis B, the major traditional Chinese medicine was Oriental Wormwood Decoction modified by adding Capejasmine, rhubarb, elephantopus scaber, bupleurum root, Japanese St. Johns wort etc.. Traditional Chinese medicines prescribed for the treatment of severe viral hepatitis B in the localities were shown to have the same basis as ours, modified by adding scutellaria root, phellodendron bark, giant knotweed rhizome, oldenlandia, subprostrate sophorca root, Chinese angelica root, pilose asiabell root etc., totalling more than 15 traditional Chinese medicines. For patients in the convalescent stage of severe hepatitis with serum total bilirubin and aminotransferases completely restored to normal levels, 3 g of honeyed pills containing freshwater turtle shell, pangolin scales, zedoary, notoginseng, dragon's blood, Chinese angelica root, pilose asiabell root, chicken's gizzardmembane, subprostrate sophora root etc., were given to each of them PO, b.i.d. for 2 consecutive weeks followed by a break of one week. The course of treatment lasted 2 months. Levels of serum total bilirubin, plasma thromboplastin antecedent, hyaluronic acid, laminin, type Ⅲ collagen and type Ⅳcollagen were monitored and compared with those assayed before the treatment. Results:Apparently better therapeutic effectiveness was demonstrated in patients treated with traditional Chinese medicines than in those who were not (P<0.05). Conclusion:Traditional Chinese medicines were shown to lower the levels of serum total bilirubin in patients with severe chronic viral hepatitis B. Striking amelioration of serum indices of liver fibrosis was also noted in patients in the restoration stage of severe hepatitis associated with hepatic failure as a result of the treatment with traditional Chinese medicines. However, components of traditional Chinese medicines may aggravate injuries of liver cells in the treatment of acute liver failure.
  • 药物与临床
  • 药物与临床
    SHEN Lingxun;LIU Qiaohong;HUANG Anbin;YU Likai
    2004, 23(4): 234-0235.
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    To compare the therapeutic effectiveness of prednisone combined with other drugs with that of prednisone alone in the treatment of polymyositis (PM) and dermatomyositis (DM). Methods:67 patients with PM and DM were divided into 2 groups. Patients of the control group (n=35) were given each 1 mg·kg1 of prednisoone alone, PO, q.d.. On the basis of the same prednisone therapy as that in the control group,patients of the treatment group (n=32) were given each additionally 7.5~10.0 mg of methotrexate, PO, per week, 3 tablets of colquhounia root ( traditional Chinese medicine), PO, t.i.d.. The course of treatment in both groups tasted 4 weeks. Myodynamia, skin rash,serum levels of ALT, AST, LDH and creatinine kinase (CK), as well as drug adverse reactions were kept under observation. Results:After the treatment, myodynamia in patients of both groups showed different degrees of improvement. 54.3% of the patients in the control group and 62.5% of those in the treatment group had a ≥2 grade improvement of myodynamia. The difference between the 2 groups was insignificant (P>0.05). Serum levels of ALT, AST, LDH and CK levels were strikingly lowered in patients of both groups as compared with those before the treatment (P<0.01). However, the extent of the lowering of ALT, AST, LDH and CK levels was evidently greater in patients of the treatment group than in those of the control group (P<0.05). Conclusion:Combined treatment was shown to result in a more rapid decline of serum muscle enzyme levels and to exert a better shortterm therapeutic effect in the treatment of PM/DM, as compared with treatment with prednisone alone.
  • 药品质量控制
  • 药品质量控制
    GE Hongliu;PAN Xin;BAO Jianquan
    2004, 23(4): 257-0258.
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    To determine the content of maminoglutethimide, the key impurity in aminoglutethimide with an HPLC method.Methods:Chromatography was performed on a Waters Spherlsorb column (4.6 mm×150 mm, 5 μm), with a mixture of pH 5.0 acetate buffer: methanol (75∶25) as the mobile phase. The detection wavelength was 240 nm. Results:The content of maminoglutethimide in aminoglutethimide was shown to be <1.0%. The calibration curve was linear in the range of 0.025~0.150 μg (n=5, r=0.999 8), and the average rate of recovery was 100.7% (n=5, RSD=1.33%). Conclusion:The method was shown to be accurate, sensitive, reliable and could be used as the limit test of maminoglutethimide in aminoglutethimide.
  • 药品质量控制
    ZHAO Zhongxiang;CAI Yaling;LI Xiaoli;RUAN Jinlan
    2004, 23(4): 259-0260.
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    To set up an HPLC method for the content determination of rutin in baihua extract. Methods:Chromatography was performed on an Agilent ZORBAX Eclipse XDBC8 column(4.6 mm×150 mm, 5 μm). The mobile phase was a mixture of methanolwaterglacial acetic acid (29∶68.3∶2.7) ,with a flow rate of 1.0 mL·min1. The column temperature was 20℃. and the detection wavelength, 360 nm. Results:The calibration curve was linear over the range of 5.54~66.48 μg·mL1, the average rate of recovery was 101.97%, RSD=0.79%(n=5).Conclusion:The method proved to be simple, rapid, reliable and well reproducible in the content determination of rutin in baihua extract.It may thus be used as a measure for quality control of the product.
  • 用药指南
  • 用药指南
    SHEN Jianxing;CHEN Junliang
    2004, 23(4): 264-0265.
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    To set up a simple and convenient RPHPLC method for an onestep simultaneous determination of the blood concentrations of phenobarbital (PB), phenytoin sodium (PT) and carbamazepine (CBZ).Methods:PB, PT and CBZ were extracted from the serum with dichloromethane and analysed on a C18 column. The mobile phase was methanol: deionized water(57∶43), the column temperature, 30℃, the detection wavelength, UV254 nm and the flow rate, 0.8 mL·min1. Results:The linear ranges were 2.540.0, 2.540.0 and 1.2520.0 μg·mL1 for PB, PT and CBZ, respectively. The average rate of recovery were 100.4%, 103.7% and 97.3%, respectively.and the RSD withinday and betweendays were less than 10.0%(n=5). Conclusion:The method was shown to be simple, convenient , reliable and suitable for monitoring the blood concentrations of PB, PT and CBZ.