Showing papers in "Chinese New Drugs Journal in 2001"

The anti-virus and hepatoprotective effect of bicyclol and its mechanism of action

Abstract: Bicyclol is a synthetic novel anti hepatitis drugIt has remarkable hepatoprotective and certain anti hepatitis virus actionsOral administration of 50,100,200 mg·kg -1 bicyclol protected livers of mice from damage induced by CCl 4,D galactosamine,acetoaminophen and BCGplus lipopolysacharides (LPS) expressed in decreases of ALT and AST as well as morphological damage of liver tissuesAddition of bicyclol to the cultivated 2215 cell line inhibited secretion of HBeAg and HBsAg as well as HBV DNA levelThe results of mechanistic study on bicyclol indicated that bicyclol is not an inhibitor of transaminase,but a cell membrane protector through elinmination of free radicalsMoreover,bicyclol can protect hepatocyte nuclear DNA from damage and reduce the apoptosis induced by immuno stimulating compound Con A [

Safety of Tripterygium Wilfordii

Abstract: Tripterygium Wilfordii ,a traditional Chinese herb,was reported to have immunoregulatory effects.It has been used in clinic for treatment of rheumatoid arthritis,systemic lupus erythematosus and kidney disease.But it is toxic,with an incidence of ADRs significantly higher than other drugs.The organal systems affected by ADRs of Tripterygium Wilfordii were gastrointestinal,urogenital,cardiovascular,blood circulatory systems as well as bone marrow.Therefore,development of new preparations to reduce its toxicity is in need to satisfy clinical uses. [

Study on the efficacy of phencynonate hydrochloride tablets in prevention of motion sickness

Abstract: Objective:To observe the efficacy of phencynonate hydrochloride tablets in prevention of motion sickness.Methods:The randomized,double blind,controlled crossover study was conducted in tank crews.They were divided to receive phencynonate hydrochloride tablets 2mg,or dimenhydrinate 50mg,or placebo 100mg.Results:The total effective rate and significant effective rate for phencynonate hydrochloride tablets group were 77.42% and 48.38% respectively.There was significant difference in efficacy between active and placebo groups (P0.01) but no significant difference in comparison with control group.The sedative effect of phencynonate hydrochloride tablets was less pronounced in comparison with dimenhydrinate.Conclusion:Phencynonate hydrochloride tablets is a safe and effective agent for prevention of motion sickness.

Progress in research of the active chemical components of Cornus officinalis

Abstract: The clinical application of Cornus officinalis,a Chinese traditional medicine,in combination regimen and the pharmacodynamics of its active components were reviewed in this paper.

The effect of polysaccharides from seaweed(SPS) on regulating the immune function in mice

Abstract: Objective:To observe the immune regulating effect of SPS in normal mice and mice with immunosuppression.Methods:Phagocytic function of peritoneal macrophage,carbongranular clearance ability,hemolysin production level,DTH induced by DNFB and T,B lymphocyte proliferation in normal mice were determined.The hemogram,thymus index,type distribution of T lymphocyte and proliferation of lymphocyte T and B in mice with immunodepression were determined.Results:In normal mice,SPS can induce the phagocytic function of peritoneal macrophages,promote the carbongranular clearance at high dose,increase hemolysin production at high and medium dose,accelerate the proliferation of T and B lymphocytes and enhance the specific and nonspecific immune function.In mice with immunodepression,SPS can relieve dysimmunity and increase the thymus index,T lymphocytes,CD + 8 cells and stimulate the proliferation of T and B lymphocytes by regulating hemogram.Conclusion:As an immunoregulator and anti viral agent,SPS may be developed into a new kind of anti HIV agent.

The efficacy and safety of mesalazine in the treatment of inflammatory bowel disease——A nationwide multicenter clinical trial

Abstract: Objective:To observe the efficacy and safety of Etiasa,a control released tablet of mesalazine,in treatment of inflammatory bowel disease(IBD) in comparison with salicylazosulfapyridine (SASP).Methods:The randomized,multicenter,and controlled study was conducted in 89 patients with endoscopy confirmed mild or moderate ulcerative colitis (UC) or Crohn's disease (CD) of initial onset.They were randomly allocated to Etiasa ( n =52) or SASP( n =37)both in a dose of 1.0g qid for 6 weeks.After that they were examined by endoscopy.The efficacy and side effects were evaluated at week 4 and week 6.Results:There were 3 patients in SASP withdrawn from the study because of allergic reaction or leukopenia at the end of the 4th week.52 patients in Etiasa group and 34 patients in SASP group completed the study.The obvious improvement rate in Etiasa group at the end of the 4th and the 6th week is 52.0% and 71.2% respectively,by evaluation of patients vs 20.6% and 50.0% in SASP group ( P 0.05).Disappearance rate of GI symptoms at the end of the 6th week is 57.7% in Etiasa group vs 50.0% in SASP group( P 0.05).Cure rate confirmed by endoscopy at the end of the 6th week is 26.9% in Etiasa group vs 2.9% in SASP group ( P 0.05).The incidence of side effects is 1.9%(1/52) in Etiasa group vs 10.8%.(4/37) in SASP group( P 0.05)。Conclusion:Etiasa is an effective agent for treatment of IBD. [

Recent research progress in lamivudine,a new anti HBV agent

Abstract: Lamivudine is a new kind of anti hepatitis B agent from nucleosides.It inhibits the DNA synthesis of HBV via decreasing the bio activity of DNA polymerase that depended on RNA.It may be useful in treatment of all kinds of hepatitis B.Its chemical properites,pharmacokinetic feature,mechanism of action,clinical uses,adverse drug reactions,and drug resistance are reviewed.

The progress and evaluation of agents for gastrointestinal motility

Abstract: The classfication of gastrointestinal motility diseases is defined on the basis of symptom patterns,for which there is no well-defined pathophysiology and pathogenesis.Therefore,the treatment is aimed at symptoms improvement.In this paper,the pharmacological mechanism of currently available agents and the new generation of agent under development were reviewed.The new agents under development include dopamine receptor antagonist,benzamide and non-benzamide 5-HT 4 receptor agonist and antagonist,motilin receptor agonist,nitric oxide synthase inhibitor,opioid receptor antagonist,GABA B-receptor agonist,CCK A receptor agonist and somatostatin analogues.

Effects of liuweidihuang decoction on immune function of autoimmune mice induced by Campylobacter jejuni (CJ)

Abstract: Objective:To study the therapeutic effects and the possible mechanism of Liuweidihuang decoction(LW) in treatment of immune diseases.Methods:To observe the immunomodulatory effects of LW in autoimmune mice induced by CJ using techniques of enzyme linked immunosorbent assay(ELISA),JH3,D,Z TdR incorporation and plaque forming cell (PFC) assay.Results:Chronic inflammation occurred in liver of autoimmune mice and the serum titers of autoantibodies including anti dsDNA and antinuclear antibodies were significantly elevated.LW in dose of 5 or 10 g·kg -1 ·d -1 for 15d can significantly alleviated the chronic inflammatory response in liver,lowered the anti dsDNA antibody level and antinuclear antibody level,and inhibited the enhanced antibody production response and splenocyte proliferation in mice.Conclusion:LW possesses the effect to improve autoimmune pathological changes,and to reduce the autoimmune inflammatory damage,the mechanism of which are closely related to restoration of the unbalanced immune function in mice model.

Study on the effect of boanmycin against human-hepatoma BEL-7402 cells and its mechanism in molecular level

Abstract: Objectvie:The effects of boanmycin(BAM) against hu ma n hepatoma,BEL 7402 cells,and its mechanism in molecular level were studied in vitro .Methdos:The cellular clonogenic assay and NAG method were used for exa mining the effect of anti tumor.The big molecular synthesis,the expression onco gene and antioncogene,and the DNA damage were investigated with incorporation of some objects labeled with [JH3,D,Z],with dot blot and with neutral gel electrophoresis,respectively.Results: IC 50 of BAM with clonogenic assay and with NAG metho d was 8.6×10 -9 mol·L -1 and 6.2×10 -6 mol·L -1 ,respectiv ely.It showed high anticancer activities and obvious dose effect relationship.T he experiment indicated that BAM strongly inhibited cellular DNA,RNA and protein synthesis,but the effects of inhibiting cellular DNA and protein synthesis were more strongly than RNA synthesis.By dot blot of total RNA isolated from BEL 74 02 cell treated with BAM at 10 μmol·L -1 ,the expressions of c myc,N ras and p53 gene were strongly inhibited.Double strand cleavage DNA in repairing w as analyzed by neutral gel electrophoresis.This result indicated that DNA damage in BEL 7402 cells,which was incubated with BAM for 1 hour,was unable to repair itself.Conclusion:The results suggested that BAM was extensive antitumor anti biotic with high potency and was worthy to be further studied.

The multi-center clinical study of the efficacy of ornidazole against acute anaerobic infections and vaginalis trichomoniasis

Abstract: Objective:To evaluate the efficacy and safety of o rn idazole tablet in the treatment of acute anaerobic infection and vaginalis trich omoniasis.Methods:In this random double-blind double-dummy control clinical tr ial,121 patients with acute anaerobic infections and 80 patients with vaginalis trichomoniasis were treated with ornidazole tablet or tinidazole tablet for 3～1 0 days,with the dose of 500 mg twice daily by mouth,the stomatological patients were received the dose of 500 mg·d~(-1),qd and double dosis at the first tim e.Results:In the treatment of acute anaerobic infections,the total effec tive rate,bacterial clearance rate and adverse reaction rate of ornidazole and tinidazole were 98.4%,(96.2%,)11.5% and 85%,90.7%,28.3% resp ecti vely,the adverse reactions were generally mild and well tolerated.The significan t differences of total effective rate and adverse reaction rate between two grou ps were observed.In the treatment of vaginalis trichomoniasis,the total effectiv e rates of two groups were 100%.Conclusion:Ornidazole is an effective and safe drug for treating acute anaerobic infections and vaginalis trichomoniasis,the adverse reaction rate is less compared with tinidazole.

Isolation,purification and composition of polysaccharide X-C-3-II obtained from Angelica sinensis (Oliv)Diels

Abstract: Objective:To study the composition of polysaccharide,X-C-3-Ⅱ,from Angelica sinensis(Oliv)Diels.Methods:The X-C-3-Ⅱ was isolated by extraction with hot water and precipated with alcohol;purified by column chromatography using DEAE-Sephadex A-25 as absorbent.Its composition was determined by gas chromatography.Results:A polysaccharide,X-C-3-Ⅱ,with a molecular weight of 1.0×105 was obtained.It consisted of glucose,galactose,arabinose,rhamnose and galacturonic acid in molar proportion of 56.0∶22.1∶18.9∶1.9∶1.1.Conclusion:X-C-3-Ⅱ is isolated first time from the plant.

Cholinergic therapeutics for Alzheimer's disease

Abstract: Alzheimer's disease (AD) is a progressive neurodegenerative disorder with severe cognitive, behavioral,and functional impairment.Although its etiology is still unknown,it is generally accepted as related to the cholinergic deficit in the brain. In this paper,the cholinergic therapeutics for AD including the precursors of acetylcholine, the acetylcholinesterase inhibitor, the postsynaptic muscarinic M 1 receptor agonists,and agents facilitating acetylcholine release were reviewed.

New clinical applications of docetaxol

Abstract: Docetaxol is a newly taxoid anticancer,which has been used in the treatment of many carcinomas,including mammary cancer,NSCLC,pancreatic cancer,soft tissue sarcoma,head and neck cancer,stomach cancer,ovary cancer,prostate cancer,etc.Its antitumor activity is remarkable either in monotherapy or in combination therapy.Its clinical applications were reviewed in this paper.

The pharmacokinetics of atofluding in cancer patients

Abstract: Objective:To explore the pharmacokinetic characteristics of atofluding in cancer patients.Methods:18 cancer patients were randomly and equally divided to receive orally atofluding 800,1 000 and 1 200mg respectively,after administration of atofluding,the serum level of its metabolites,5 FU and TFU,at different time was determined by HPLC.Data obtained were treated and its pharmacokinetic parameters were calculated.Results:In human body,atofluding was metabolized mainly to 3 ortho methylbenzoyl 5 fluorouricil,the latter's pharmacokinetics was fitted to one compartment model.Very great individual difference in atofluding metabolism was observed among patients.Pharmacokinetic parameters of atofluding didn't differ significantly with doses.Conclusion:Very great individual difference was observed among patients in metabolism of atofluding,and therapeutic drug monitoring or individualization of dose may be necessary. [

Observation of the efficacy of cetirizine in treatment of chronic and acute urticaria

Abstract: Objective:To evaluate the safety and efficacy of cetirizine in treatment of acute and chronic urticariaMethods:Patients with urticaria were randomly divided to receive once daily oral 10 mg cetirizine or once daily oral 10mg Zyrtec(imported cetirizine) for 7 days (for acute urticaria) and 14 days (for chronic urticaria)Results:In cetirizine group,the effective rate was 667% for acute urticaria cases ( n =24) and 740% for chronic urticaria cases ( n =26)In the control group,the effective rate was 885% for acute urticaria cases( n =26) and 640% for chronic urticaria cases( n =25)The adverse event rate was 231% for active group and 196% for control groupThere were no significant differences between groups in both the effective rate and the adverse event rateConclusion:Cetirizine is a safe and effective H 1 receptor antagonist for treatment of acute and chronic urticaria

Efficacy and safety of injectable azithromycin in treatment of pneumonia in children

Abstract: Objective:To evaluate the efficacy and safety of injectable azithromycin in treatment of pneumonia in children.Methods:110 children with acute pneumonia were recruited into the multicenter open study.They were treated with injectable azithromycin in once daily dose of 10 mg·kg -1 for 5～7 days.Results:A total effective rate of 90% was obtained with a mild adverse reaction incidence of 7.2%.Conclusion:The results suggested that injectable azithromycin is effective in treatment of pneumonia in children with mild adverse reaction.

Recent progress in proton pump inhibitors

Abstract: The mechanism of action and clinical characteristics of proton pump inhibitors(PPIs),a class of antiacids widely used in clinic including omeprazole, lansoprazole,pantoprazole,rabeprazole,leminoprazole and perprazole,are reviewed in this paper. [

Advancement and prospect in research of fresh herbal medicines in China

Abstract: The clinical application of fresh herbal medicines in recent 10 years in China,the traditional and modern methods for keeping herbal medicines fresh,the difference in efficacy of dry and fresh herbal medicines,the development in preparations of fresh herbal medicines and new trend in research of this aspect were reviewed in this paper.

Extraction,separation,and examination of the effective hypoglycemic component of cushaw polysaccharide

Abstract: Objective:To refine the crude product of cushaw polysa ccharide.Methods:The crude cushaw polysaccharide was refined by ion exchange co lumn,Sepherose column,and Sephadex _ 200 column,after lyophilization,a white po wder of polysaccharide was obtained.The quality of this polysaccharide was anal yzed by paper chromatography and glass fiber paper electrophoresis.Results:No more than 3 spots are allowed to present in the chromatogra m.Conclusion:The polysaccharide thus obtained appears to be composed of a single component.

Plasma drug level of risperidone and its clinical significance

Abstract: Objective:To observe the relationship among oral dose,plasma drug level,and the efficacy and side effects of risperidone.Methods:The controlled study was conducted in 38 patients with schizophrenia.They were randomly and equally divided to receive 2 or 4 mg risperidone for 8 weeks.The plasma drug level of risperidone and its active metabolite,9-hydroxyrisperidone,were measured by HPLC method at the end of week 2,4 and 8.The PANSS,CGI,TESS,and ESRS were evaluated at week 1,2,4,6 and 8.Results:Risperidone was effective in both positive and negative symptoms of schizophrenia,but the onset of action for positive symptom was quicker than that of the negative.There was a significant difference in plasma drug level of risperidone and its metabolite between 2 mg and 4 mg groups but no significant difference in efficacy.The effective dose range for risperidone and its active metabolite may be 30～45 ng·mL -1.Conclusion:The effective and safe method for medication of risperidone starts with small dose(2～4mg) and then increases in dose gradually.The efficacy and side effect of risperidone can be predicated and prevented by plasma drug concentration of risperidone and its active metabolite.

Effect of ranitidine bismuth citrate on experimental gastric ulcer

Abstract: Objective:To study the effect of ranitidine bismuth citrate (RBC) on four kinds of experimental gastric ulcer.Methods:The inhibitory effect of RBC on experimental ulcers:including aqueous extract excitability ulcer in mice,acetic acid induced ulcer in rats,pyloric ligational ulcer in rats,ethanol induced ulcer in rats were observed.Results:RBC showed significant protective effect on 4 experimental gastric ulcers.RBC significantly reduced the gastric ulcerogenesis,gastric acid secretion,and gastric pepsin activity(in pyloric ligation model) in animal models.Ranitidine HCl was also effective in treatment of gastric ulcer but less potent than RBC in these models.Conclusion:RBC is a suitable agent for treatment of gastric ulcer because it possesses the inhibitory effect of gastric acid secretion of ranitidine and mucosal protective and pepsin inhibitory effect of bismuth. [

Preliminary study on preparation of paclitaxel microsphere

Abstract: Objective:In order to reduce the toxic side effects,preparation of paclitaxel microsphere has been studied.Methods and Results:Paclitaxel microsphere was prepared by single coacervation method using gelatin as encapsulating agent in addition of an apropriate inhibitor.Conclusion:The paclitaxel microsphere thus prepared is stable.The process is reproducible with low cost. [

Side effect of atypical antipsychotics

Abstract: Atypical antipsychotics are a new kind of antipsyc ho tics with more potent antipsychotic efficacy and without extrapyramidal reaction in lower doses.However,they also have some side effects.In this paper,the side effects of some atypical antipsychotics,including clozapine,risperidone,olanzap ine,quetiapine,ziprasidone and sertindole were reviewed.

The trend in research of carbapenem antibiotics

Abstract: Carbapenem is a new group of β-lactam antibiotics with a broad antibacterial spectrum and a different structure from traditional β-l actam antibioticsCarbapenem is active against gram-positive,gram-negative,aer obic,and anaerobic bacteria and is stable to lactamasesIt can be divided into type 1 carbapenem:unstable to DHP-I;type 2 carbapenem:stable to DHP-I but cann ot be used alone;and type 3 carbapenem:stable to DHP-I and can be used alone

The liver-protective and immunomodulative effect of Shahepatide in mice with immune liver injury

Abstract: Objectives:To explore the effect of Shahepatide,an active polypeptide extracted from shark liver,on secretion of IFN γ and TNP β from human periperal blood mononuclear cells (PBMC)and to explore its liver protective effect in mice with immune liver injuryMethods:Shahepatide was added to PBMC and culturedThe content of IFN γ and TNF β in the culture supernatant were measuredMice model of immune liver injury was created by endotoxin attack and their blood AST and ALT level were determinedResults:Shahepatide can induce secretion of IFN γ from PBMC( P 001),inhibit production of TNF β from PBMC,can significantly reduce the abmomal elevation of serum ALT and AST in mice with immune liver injury and obviously reduce their pathological liver injuryConclusions:Shaheptide possesses an excellent prospect in treatment of hepatitis B,liver cirrhosis,and chronic hepatitis,as well as in modulation of immunologic functions