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    药物研究
  • 药物研究
    FENG Binghong;ZHANG Xiaoling;ZHAO Yuhong;HUANG Yashen;YUAN Zhihui;LAO Ren;HUANG Huiqing
    2005, 24(10): 0-0.
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    ObjectiveTo survey the vasodilative effect of the extract of huoxuezhuyu recipe and to probe into its underlying mechanisms. MethodsThe vasodilative effect of the drug was studied with the guinea pig mesenteric microvasculature and isolated rat aortic rings. The content of nitric oxide(NO )in the blood plasma and aortic tissue, the activities of nitric oxide synthase (NOS) , constitutive nitric oxide synthase (cNOS) and inducible nitric oxide synthase (iNOS) in the aortic tissue were determined with the method of nitroreductase chromatometry. ResultsThe extract of huoxuezhuyu recipe was shown to counteract the vasocontrictive effect of norepinephrine on the mesenteric microvasculative of the guinea pig. It could also relax the isolated rat aortic rings constricted by phenylephrine. The vasorelaxing effect of the extract persisted despite pretreatment of the aortic rings with glibenclamide or propranolol. However, the extract of huoxuezhuyu exerted vasoconstrictive effect on the aortic rings if the endothelium had been denuded. The extract in high dose was shown to very significantly increase the content of NO in the blood plasma and the content of NO as well as the activities of NOS and cNOS in the aortic tissue. In contrast, the extract in low dose could significantly increase the activity of cNOS in the aortic tissue. ConclusionThe extract of huoxuezhuyu recipe was shown to have a vasodilative effect and its underlying mechanisms may be related to the activation of the vascular NOS and cNOS as well as the promotion of the release of NO from the endothelium of the blood vessel.

  • 药物研究
    FENG Binghong;ZHANG Xiaoling;ZHAO Yuhong;HUANG Yashen;YUAN Zhihui;LAO Ren;HUANG Huiqing
    2005, 24(10): 0-0.
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    ObjectiveTo survey the vasodilative effect of the extract of huoxuezhuyu recipe and to probe into its underlying mechanisms. MethodsThe vasodilative effect of the drug was studied with the guinea pig mesenteric microvasculature and isolated rat aortic rings. The content of nitric oxide(NO )in the blood plasma and aortic tissue, the activities of nitric oxide synthase (NOS) , constitutive nitric oxide synthase (cNOS) and inducible nitric oxide synthase (iNOS) in the aortic tissue were determined with the method of nitroreductase chromatometry. ResultsThe extract of huoxuezhuyu recipe was shown to counteract the vasocontrictive effect of norepinephrine on the mesenteric microvasculative of the guinea pig. It could also relax the isolated rat aortic rings constricted by phenylephrine. The vasorelaxing effect of the extract persisted despite pretreatment of the aortic rings with glibenclamide or propranolol. However, the extract of huoxuezhuyu exerted vasoconstrictive effect on the aortic rings if the endothelium had been denuded. The extract in high dose was shown to very significantly increase the content of NO in the blood plasma and the content of NO as well as the activities of NOS and cNOS in the aortic tissue. In contrast, the extract in low dose could significantly increase the activity of cNOS in the aortic tissue. ConclusionThe extract of huoxuezhuyu recipe was shown to have a vasodilative effect and its underlying mechanisms may be related to the activation of the vascular NOS and cNOS as well as the promotion of the release of NO from the endothelium of the blood vessel.
  • 药物研究
    CHEN Yueming;WANG Gang;ZHANG Shunquan;XIE Jian;GAO Lishu
    2005, 24(10): 0-0.
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    ObjectiveTo approach the relationship between the metabolism of clozapine in patients with schizophrenia and polymorphism of loci –2964 and 734 in P450 1A2(CYP-1A2) with the aim of providing theoretical basis for the rational use of clozapine. Methods122 patients with schizophrenia meeting the CCMD3H and DSM-Ⅳ diagnostic criteria for the disease were included in the study. Of these, 56 people were smokers and 66 were nonsmokers. All the patients were given each 50 mg·d-1 of clozapine PO as an initial dose. The dose was increased to 300 mg·d-1 PO as a fixed dosage within 2 weeks. The course of treatment with the fixed dosage lasted 8 weeks. According to the results of Brief Psychiatric Rating Scale (BPRS) assessment, the drug was judged as effective if the subtraction mark rate was greater than 30 and ineffective if it was equal to or smaller than 30. The steady state concentrations of clozapine and desmethylclozapine in sera of the patients were determined with high press liquid chromatography( HPLC). CYP-1A2 genotypes of the patients were detected with restriction fragment length polymorphism (RFLPs). The relationship between genotypes and phenotypes were analysed with statistical methods.ResultsThe overall effective rate of clozapine in the treatment of the disease was 85.2%. The plasma clozapine concentration of the smokers was lower, while the ratio of desmethylclozapine to clozapine was higher as compared with those of nonsmokers, respectively (P<0.05 and, P<0.01). According to the polymorphisms of CYP 1A2 5' flanking 2964 and locus 734 of intron 1, 6 genotypes were detected with RFLPs: G/G-2964A/A734,G/A-2964A/A734,A/A-2964A/A734,G/G-2964C/A734,G/A-2964C/A734 and G/G-2964C/C734 ,while genotypes A/A-2964C/A734,G/A-2964C/C734,A/A-2964C/C734 were not demonstrated. The frequency of allele G at locus –2964 was 0.75, while that of allele C at locus 734 was 0.31. The ratio of desmethylclozapine to clozapine in patients with G/G-2964A/A734 genotype was significantly higher than that in patients with non G/G-2964A/A734 genotypes both in smokers and nonsmokers(P<0.05, P<0.05). ConclusionPatients with G/G-2964A/A734 genotype were shown to have high inductivity and enzyme activity of CYP 1A2, suggesting that G-2964 and A734 may be related to individualized treatment of schizophrenics with clozapine.
  • 药物研究
    WANG Yan
    2005, 24(10): 0-0.
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    ObjectiveTo study the pharmacokinetics and relative bioavailability of sparfloxacin dispersible tablets in humans. MethodsA single oral dose of 400 mg of the 2 sparfloxacin preparations——dispersible tablets and common tablets were separately given to each of the 18 healthy male volunteers in an open randomized autologous crossover test. The interval between the administrations of the 2 preparations was 2 weeks. Venous blood samples were taken from each of the subjects 0.5, 2.0, 3.0, 4.0, 4.5, 5.0, 5.5, 6.0, 8.0, 12.0, 24.0, 48.0, 72.0 and 96.0 h after the medication, respectively. Serum concentrations of sparfloxacin were determined with RPHPLC.ResultsThe pharmacyokinetics parameters AUC0→∞,Cmax,tmax of sparfloxacin dispersible tablets and common tablets were (48.11±4.04)h·μg·mL-1,(1.51±0.16)μg·mL-1,(1.86±0.15) h and (47.12±5.23)h·μg·mL-1,(1.49±0.21) μg·mL-1 ,(4.51±0.21) h, respectively. The bioavailability of dispersible tablets relative to that of common tablets was (102.10±12.01)%. ConclusionIt was shown by statistical analysis that the difference between the Cmax of the two preparations was significant while the differences between the AUC0→∞ and Cmax were not, suggesting that the bioavailability of the 2 preparations were similar. However, dispersible tablets were absorbed more rapidly
  • 药物研究
    LI Cairong;YANG Xiao;ZHU Zhonghua;CAI Fei
    2005, 24(10): 0-0.
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    ObjectiveTo survey the therapeutic effect of epigallocatechin3gallate (EGCG) on the kidney lesion and its influence on renal oxidative stress and content of plasma homocysteine (Hcy) in rats with experimental diabetes. Methods47 inbred adult SD rats served as the subjects of the study. The rat model of experimental diabetes was set up in 37 rats by a single intraperitoneal injection of 65 mg·kg-1 of streptozotocin for each animal. 30 diabetic rats were randomly divided into 3 groups: model group, treatment group Ⅰ and treatment group Ⅱ.10 normal rats served as normal controls. Four weeks after the induction of experimental diabetes, rats of the treatment groupsⅠ and Ⅱ were given each an intraperitoneal injection of 2.5 mg·kg-1·d-1 and 5 mg·kg-1·d-1 of EGCG, respectively. Rats of the model group and normal controls were given each an intraperitoneal injection of 0.1 mol·L-1 citric acid buffer solution in equivalent amount q.d.. The course of treatment lasted 12 weeks. During the 12th week of treatment, 24 h urine and blood from the caudal vein from each rat of the 4 groups were collected and all of the animals were then sacrificed. The content of malonyldialdehyde(MDA), the activity of superoxide dismutase(SOD) and GSHPx in the kidney tissue as well as the plasma concentration of Hcy were determined. ResultsA striking increase in the ratio of the kidney weight(mg) to body weight(g), a prominent weakening of the renal antioxidation capability associated with enhanced oxidative stress and a significant increase in the plasma content of homocysteine were demonstrated in rats of the model group as compared with those of rats in the control group(P<0.01).The amount of 24 h urine protein, the contents of blood glucose, blood lipids and serum creatinine were notably greater in rats of the model group than those in rats of the control group (P<0.01). In rats of the treatment group Ⅰ and group Ⅱ , the ratio of kidney weight to body weight was smaller than that in rats of the model group(P<0.05 or P<0.01). The amount of 24 h urine protein, the contents of blood lipid, serum creatinine in EGCG treated rats were also lower than those in rats of the model group(P<0.05 or P<0.01). In contrast, the activities of SOD and GSHPx in the kidney tissue of EGCG treated rats were significantly higher than those in rats of the model group(P<0.05). Meanwhile, the content of MDA in the kidney tissue and that of homocysteine in the blood plasma of EGCG treated rats were remarkably lower than those in rats of the model group(P<0.05).ConclusionEGCG was shown to exert a protective effect on the kidney of diabetic rats by increasing the antioxidation capability and decreasing the oxidative stress of the kidney as well as lowering the plasma homocysteine.
  • 药物研究
    SHU Chengren;QIU Jun;WANG Gaosheng
    2005, 24(10): 0-0.
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    ObjectiveTo probe into the protective effect of the ethanol extract of the seed of Fagopyrum tartaricum(FTGE)on the liver acutely injured by chemicals in mice. Methods120 mice of the Kunming strain served as the subjects of the experiment. For the study of the effect of FTGE on the liver injured by CCl4 , 60 mice were randomly divided into 6 equal groups. Mice of the low dose, medium dose and high dose groups were given each by gastragavage 20,40 and 60 g·kg-1·d-1 of FTGE for 7 consecutive days, respectively. Mice of the normal control group and CCl4 model group were given each equivalent amount of purified water by the same route for 7 days. Mice of the positive control group were given each 200 mg·kg-1·d-1 of bifendate by gastrogavage as well for 7 days. Except for the mice of the normal control group, animals of all the other 5 groups were given each 7 days later an intraperitoncal injection of 10 mg·kg-1 of 0.1% CCl4 peanut oil solution. After a 16 h. fasting, blood samples were collected for the determination of serum alanine aminotransferase(ALT) and aspartate aminotransferase(AST)while liver tissue was taken for pathological examination. For the study of the effect of FIGE on the liver injured by galactosamine(D-Galn), 60 mice were divided into 6 equal groups. Mice of the low, medium and high dose groups were given each by gastrogavage 20,40 and 60 g·kg-1·d-1of FIGE for 12 consecutive days. Mice of the normal control group and DGaln groups were given each 20 mL·kg-1·d-1 of 0.9% sodium chloride solution by the same route for 12 days. Mice of the positive control group were given each 15 mg·kg-1·d-1of bifendate by gastrogavage as well for 12 days. Except for mice of the normal control group, rodents of all the other 5 groups were given each 1 h. after the last gastrogavage an intraperitoneal injection of 800 mg·kg-1of 10% D-Galn. After a 16 h fast, the mice of all 6 groups were sacrificed and blood samples were collected for the determination of serum ALT and AST while liver tissue was taken for pathological examination. ResultsFTGE was shown to lower the activities of serum ALT and AST very strikingly in a dose dependent manner in mice with acute liver injury induced by chemical hepatotoxins CCl4 and D-Galn(P<0.01). A dramatic alleviation of the histopathological changes of the liver was also demonstrated in mice pretreated with FTGE before the induction of liver injury as compared with those of mice of the CCl4 and D-Galn model groups without FTGE pretreatment(P<0.01). ConclusionFTGE was shown to exert a remarkable protective effect on the murine liver acutely injured by CCl4 and DGaln.
  • 精神科用药专栏
  • 精神科用药专栏
    ZHU Peijun;WANG Yuanhua;ZHU Peilin;ZHANG Jing
    2005, 24(10): 0-0.
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    ObjectiveTo assess the therapeutic effectiveness and safety rate of lithium carbonate combined with fluoxetine in the treatment of patients with bipolar affective disorder.Methods68 patients with bipolar affective disorder were randomly divided into two equal groups, the treatment group and the control group. Patients of the treatment group were given each 1.0 g of lithium carbonate, q.d. combined with 20 mg(initial dose) to 40 mg (maximum dose) of fluoxetine, q.d.. Patients of the control group were given each 1.0 g of lithium carbonate, q.d. combined with amitriptyline beginning with an initial dose of 25 mg q.d., increasing to 150 mg q.d. 1 week later and reaching finally to a maximal dose of 250 mg q.d. if necessary, according to the patients' condition. All of the 4 medicaments were administered orally, and the course of treatment in both group lasted 8 weeks. The clinical therapeutic effectiveness was assessed with the Hamilton Depressive Scale (HAMD) and Clinical Global Impression (CGI) ,while adverse reactions were appraised with the Treatment Emergent Symptom Scale(TESS). ResultsThe overall effective rates in patients of the treatment group and control group were 90.9% and 80.8%, respectively(P>0.05), and the rates of excellent therapeutic effect in patients of the treatment group and control group were 81.8% and 73.1%,respectively(P>0.05). However, in patients of the treatment group, adverse reactions were less common and there was a better drug compliance and lower rate of switching from depression to mania. ConclusionLithium carbonate combined with fluoxetine was shown to be effective and safe in the treatment of patients with bipolar affective disorder .
  • 精神科用药专栏
    ZHANG Junqing;WANG Qiuling;ZHANG Zeng
    2005, 24(10): 0-0.
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    ObjectiveTo compare the therapeutic effectiveness and safety rate of mianserin and amitriptyline in the treatment of postschizophrenic depression.Methods86 patients with postschizophrenic depression were randomly divided into two equal groups , the treatment group and the control group. Patients of the treatment group were given each 30-90 mg·d-1 of mianserin PO, while patients of the control group were given each 75-225 mg·d-1 of amitriptyline PO. The course of treatment in both groups lasted 6 weeks. The clinical therapeutic effectiveness was assessed with the Hamilton Depressive Scale(HAMD) and Positive and Negative Symptom Scale(PANSS) ,while adverse reactions were appraised with the Treatment Emergent Symptom Scale(TESS). ResultsThe rates of excellent therapeutic effect of mianserin and amitriptyline were 62.8% and 65.1%, respectively (P>0.05).The differences between the HAMD and PANSS scores before and after the treatment in patients of both groups were highly significant (P<0.01), showing striking improvement of the patients condition. However, mianserin started to act quickly , and its adverse reactions were less common and more trifling than those of amitriptyline. ConclusionMianserin was shown to have definite therapeutic effect in the treatment of post schizophrenic depression. It was also safe during medication and well tolerated by the patients.
  • 精神科用药专栏
    ZHANG Chuanzhi;WANG Qiuling;SHI Zhongli
    2005, 24(10): 0-0.
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    ObjectiveTo survey the quality of life in patients with schizophrenia treated with quetiapine. Methods62 patients meeting the CCMD3 diagostic criteria for schizophrenia were assigned to 2 groups, the treatment group (n=30) and the control group(n=32). Patients of the treatment group were given each 300-600 mg·d-1of quetiapine ,b.i.d., PO. Patients of the control group were given each 300-500 mg·d-1 of clozapine,b.i.d. or t.i.d., PO. The course of treatment in both groups lasted 6 months. The Positive and Negative Symptom Scale( PANSS) was used to assess the therapeutic effectiveness, and changes in the quality of life in all of the patients were kept under observation. ResultsThe differences were not significant between the 2 groups of schizophrenics with respect to the changes in the positive and negative symptoms as well as the total scores of PANSS (P>0.05). After the 6 month treatment, a striking improvement was demonstrated almost in every aspect of the quality of life in patients treated with quetiapine except for the spirit domain. In contrast, only partial improvement in the quality of life was shown in patients treated with clozapine, which had no help to the schizophrenics in the domains of physiology, psychology and independent character.ConclusionIt was shown that quetiapine was superior to clozapine in improving the schizophrenics' quality of life.
  • 精神科用药专栏
    YE Cuiwei;ZHOU Feiqin
    2005, 24(10): 0-0.
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    ObjectiveTo assess the therapeutic effectiveness and safety rate of mirtazapine in the treatment of patients with depression associated with anxiety.Methods60 patients with depression associated with anxiety were divided into two groups, the treatment group and the control group. 29 patients of the treatment group were given each 15-45 mg of mirtazapine, PO, q.n.,31 patients of the control group were given each 100-200 mg·d-1 of amitriptyline, PO, t.i.d.. The course of treatment in both groups lasted 6 weeks. The therapeutic effectiveness was assessed with the Hamilton Depressive Scale(HAMD) and the Hamilton Anxiety Scale(HAMA) while adverse reactions were appraised with the Treatment Emergent Symptom Scale(TESS). ResultsThe rates of excellent therapeutic effect in patients of the treatment group and control group in the management of the depression symptoms were 72.4% and 71.0%, respectively(P>0.05), while those in patients of the treatment group and control group in coping with the anxiety symptoms were 79.3% and 51.6% ,respectively(P<0.01). Mirtazapine started to act early in the 1st week of treatment in patients of the treatment group. while amitriptyline began to act one week later in patients of the control group. Adverse reactions in patients of the treatment group were less common and more trifling than those in patients of the control group. The main adverse reactions in patients of the treatment group included xerostomia, somnolence, increased body weight, gastrointestinal discomfort etc..ConclusionMirtazapine was shown to have good therapeutic effect in the treatment of depression associated with anxiety. It started to act quickly and was superior to amitriptyline in the management of anxiety symptoms.
  • 药物与临床
  • 药物与临床
    LAO Guoqin;WU Yong;WANG Jialiang
    2005, 24(10): 0-0.
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    ObjectiveTo study the effect of compound fetal bovine liver extract tablets in combination with lamivudine on hepatic fibrosis in patients with chronic hepatitis B. Methods174 patients with chronic hepatitis B were randomly divided into 3 groups: the control group(n=56),positive control group(n=58) and treatment group (n=60).Patients of the control group were submitted to a 6 month treatment course with oral medication of 2 Fructus silybi tablets and drugs for symptomatic treatment . On the basis of the treatment for patients of the control group, patients of the positive control group were given each additionally 100 mg of lamivudine q.d. PO for at least one year. Based on the treatment for patients of the positive control group, patients of the treatment group were given each 2 tablets of compound fetal bovine liver extract PO t.i.d. for 6 months. Serum levels of hyaluronidase (HA), type Ⅲ procollagen (PCⅢ), laminin(LN), type Ⅳ collagen (Ⅳ-C) were determined with radioimmunoassay (RIA)in patients of all 3 groups before and 3 as well as 6 months after the beginning of the treatment. The internal diameter of the trunk of the portal vein, the average speed and volume of blood flow in the portal vein and the thickness of the spleen were examined with color Doppler. Light microscopic examination of the liver pathohistology was carried out in 60 patients before and 6 months after the beginning of treatment. ResultsAfter 6 months of treatment, levels of serum PCⅢ,HA,LN and Ⅳ-C in patients of the positive control group and treatment group were notably lower than those in patients of the control group(P<0.01), and these hepatic fibrosis indexes were also significantly lower in patients of the treatment group than those in patients of the positive control group(P<0.01). Situations of the internal diameter of the trunk of the portal vein, the speed and volume of the blood flow in the portal vein and the thickness of the spleen were strikingly improved in patients of the positive control group and treatment group as compared with those of the control group(P<0.01 or P<0.05).Among these, the extent of improvement in the internal diameter of the trunk of the portal vein and the thickness of the spleen was greater in patients of the treatment group than that in patients of the control group(P<0.05 or P<0.01). Striking improvement in the scoring of the activity of the liver inflammation and the extent of hepatic fibrosis was demonstrated in patients of the positive control and treatment group as compared with that in patients of the control group(P<0.01). The improvement in these parameters, however, was more significant in patients of treatment group than in patients of the positive control group(P<0.01). ConclusionIt was shown that compound fetal bovine liver extract tablets in combination with lamivudine exerted a definite therapeutic effect in the treatment of chronic hepatitis B with hepatic fibrosis.
  • 药物制剂
  • 药物制剂
    HE Guofang;QI Xiaohong;LIN Fang;MIN Min
    2005, 24(10): 0-0.
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    ObjectiveTo optimize the preparation technology for the inclusion compound of clarithromycin-β-cyclodextrin and to improve its solubility and bioavailability.MethodsThe inclusion compound was prepared with the solution method, and an orthogonal test was used to optimize the conditions for the technology of preparation.ResultsThe optimal condition for the inclusion compound of the drug were: clarithromycin∶β-cyclodextrin=1∶1;time for inclusion :5 h;inclusion temperature:60℃.ConclusionThis inclusion technology may improve the solubility and bioavailability of clarithromycin in the inclusion compound.
  • 药品质量控制
  • 药品质量控制
    GUO Dan;YANG Xixiao;HOU Lianbing
    2005, 24(10): 0-0.
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    ObjectiveTo set up a method for the determination of the content of lead (plumbum, Pb) in the traditional Chinese medicine changtong oral liquid. MethodsInductively coupled plasmamass spectrometry (ICPMS) was used for the determination of lead under the following conditions: forward power , 1.35 kW;reflection power,<5 W;sample depth , 6.8 mm;cold argon gas flow, 12.0 L·min-1;auxiliary argon gas flow, 1.0 L·min-1,and nebulous argon gas flow, 1.0 L·min-1. ResultsThe calibration curve was linear when the concentrations of the heavy metal Pb were in the range of 1-8 μg·mL-1(r=0.999 2).The average rate of recovery of Pb was 99.12%,RSD=2.86%(n=5). ConclusionThe method was shown to be simple, rapid and sensitive and could be used for the quality control of the changtong oral liquid with respect to its content of Pb. The Pb content in the changtong oral liquid accorded with the national stipulations.
  • 药品质量控制
    JIANG Ping;CHEN Hongying;WANG Wenqing
    2005, 24(10): 0-0.
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    ObjectiveTo set up a reversephase high performance liquid chromatography( RP-HPLC) method for the determination of the content of paeoniflorin in rupineixiao oral liquid. MethodsThe chromatographic column was a YMC-Pack ODS (4.6 mm×250 mm,5μm). The mobile phase was consisted of methanolwater glacial acetic acid ( 25∶75∶0.2) ,and the detecting wavelength was 230 nm. The column was kept at room temperature.ResultsThe linear relationship was fairly good when the amount of paeoniflorin added was within the range of 0.201-3.348 μg (r=0.999 9) . The average rate of recovery was 98.60% ,RSD=1.70%(n=6). ConclusionThe method was shown to be suitable for the determination of the content of paeoniflorin in rupineixiao oral liquid