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Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Table of Content

    Volume 3 Issue 4
    26 December 1998
    Nerve growth factor prevents nitric oxide release and nitric oxide synthase gene expression induced by glutamate in primary cortical cultures of fetal rats
    WU Jun-Fang, WANG Ping, ZHANG Jun-Tian
    1998, 3(4):  241-244. 
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    Aim To study the effects of nerve growth factor (NGF) on nitric oxide (NO ) release and constitutive nitricoxide synthase (cNOS) geneexpression induced by glutam ate(Glu) in cortical neuronal cuItures.Methods Neuron viability was measured to assay NGF effect.NO content and the expression of cNOS mRNA w ere determined by fluo-rometric method and Northe rn blotting respectively.Results Glu (0.5~2.0 mmolL)induced a marked increase of neuronal death and NO content in cultured cerebral cortical neurons.L-NAME (100μmol/L) and NGF (100μg/L) signifi cantly inereased neuronal surviving and decreased NO release.Hemolglobin (Hb),which binds NO,completely prevented Gluinduced cell death and NO release at 500 pμmoY L.NGF (50,100μg/L)sigmificantly inhibited cNOS m RNA expression induced by Glu (0.5 mmoYL).Conclusion NO mediates Gluneurotoxicity in cortical neuronal cultures and NGF protects the neurons against Gluneurotoxicity viainhibiting the activity of cNOS and the release of NO.
    Application of simvastatin in hyperlipidemic patients after renal transplantation1
    XU Feng, FAN Li-Pei, WU Zhao-Hui, ZOU Heng-Qing, ZHANG Zhong-Yi
    1998, 3(4):  246-249. 
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    Aim To study the effect and safety of simvastatin in hyperlipidemic patients after renalt ransplantation.Methods Seventeen hyperlipidemic patients after renalt ransplantation(with to talcholesterol level higher than 6.2 mmol/L)were given simvastatin 10 mg/day for 1 month.The venous blood was collected from an antecubital vein.Plasma lipid and cyclosporine concentration in w hole blood w ere determined before and 1 month after simvastatin administration.Cholesterol (TC)and triglyceride (TG)in plasma w ere determined by standard enzymatical procedures on a Biochem autoanalyzer (Beckman,USA).The blood cyclosporine concentration was determined by specific FPIA method.Results Plasma TC levels w ere decreased markedly from 8.74 ±2.18 mmol/L to 7.59 ±3.28 mmol/L (P<0.05),TG levels were kept unchanged,and the whole blood cyclosporine concentrations w ere increased significantly from 185.31 ±39.02 ng/ml to 257.33 ±57.78 ng /ml (P<0.01)after 1 month of simvastatin administration in 17 recipients.No severe adverse drug reactions were observed.Conclusion Low dose simvastatin can be safely used to treat hyperlipidemic patients after renal transplantation.
    Relationship between bladder cancer and slow N-acetylators phenotyped with caffeine as a probe drug in Chinese population
    GUO Rui-Chen, CUI Xi, XU Zhi-Shun, WANG Ben-Jie, LI Chao-Wu
    1998, 3(4):  250-255. 
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    Aim Acetylator status of 203 healthy controls and 67 patients with bladder cancer was observed.Methods All the subject s w ere N-acetylate-phenotyped with caffeine asametabolic probe drug.Urine samples were collected 2 hours after a cuPof 140mg-caffeine-spiked coffee was taken under fasting condition in the morning.The caffeine metabolites,5-acetylamino-6-formylamino-1-me thyluracil(AFMU) and 1-methy lxanthine (1X)were analysed by High Performance Liquid Chromatog raphy(HPLC).The frequence histogram and probit plot were constructed to select the antimode which was used to assess slow and fast acetylator statusboth in healthy controls and patients with bladder cancer.Results The peak hight ratios (PHR)of AFMU/1X were from 0.06 to 6.5 for healthy voluteers and 0.1 to 6.31 for patients with bladder cancer.Of the 203 healthy controls involved in this study 73.7%(149/203)had the AFMU/1X>1.10,and were classified as fast acetylators,and 26.3%(54/203)as slow acetylators,while 53.7%(36/67)were fast acetylators and 46.3%(31/67)were slow acetylators in patients with bladder cancer.The oddsratio was 2.376,and the genefreqency for healthy controls and for patients with urinary bladder cancer was 0.51 and 0.68 respectively.Conclusion The acetylator status of Chinese population is polymorphic and completely in concordance with that determined by dapsone,isoniazid or sulfamethazine methords as previously reported.Slow acetylators might be susceptible to urinary bladder cancer.
    Quantitative analysis of analgesic effect and acute toxicity of acetaminophen , butabital and caffeine in combination in mice
    ZHENG Qing -Shan, GUI Chang-Qing, SUN Rui-Yuan
    1998, 3(4):  256-260. 
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    Aim To analyzed and evaluate the analgesic effect of acetaminophen (Ace),butabital(But)and caffeine (Caf)in combination.Methods According to the formula uniform design method,7 different doses at 7 different pro portions were administered (ig)to observe the analgesic effect in mice by the swirling tail method.The optimum doses and proportion in combination were obtained according to the experimental data,ma thematical analysis and the special field demand,which was demonstrated by another experiments (the swirling tail method and the light -electric vibrating box method).Acute toxicity of the combination was quantitatively analyzed by the parameter method.Results The combination of Ace 40.7,But 6.4 and Caf 5 mg/kg (proportion as 8.1∶1.25∶1)was appropriate and the acute toxicity didn't increased.Conclusion The formula uniform design method can be effectively applied to analyze the multidrug effects,but its result must take a special field demand into account,and the estimated optimum dose and proportion for combination be demonstrated by another further experiment.
    Inhibitory effects of Losartan on c-fos expression and intracellular free calcium elevation induced by Angiotensio Ⅱ in cardiomyocytes of neonatal rats
    SUN Qi, FENG Hui, WU Jun-Fang, NIU Feng-Zhen
    1998, 3(4):  261-267. 
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    Aim To study effects of Losartan on c-fos mRNA expression and free int racellular Ca2+([ Ca2+] i)level induced by AngiotensionⅡ(AngⅡ)in cardiomyocytes of neo natalrats.Methods Effect of Losartan on c-fos mRNA ex pression induced by AngⅡin cardiomyocytes was studied with dot blotting assay.Ca2+was measured with Ca2+sensitive fluorescent indicator (Fura-2/AM) using AR-C M-M IE cation measurement system.Results AngⅡtemporally induced c-fos gene expression and significantly increased the [Ca2+] ielevation in cardiomyocytes of neonatal rat s.However,the dynamic changes of c-fosgene expression and [Ca2+] i could be inhibited by Losartan 20μmol/L,but not by PD123319.Lo sartan 1~100μmol/L significantly inhibited AngⅡinduced [Ca2+] ielevation in adose-dependent manner.Conclusion The results suggest that c-fos expression and[Ca2+] ielevation induced by AngⅡare mediated by AT1 subtype acceptor.Losartan maybe an effective drug in treating cardiac hypertrophy.
    Distribution of penicillin G,cefazolin , tobramycin and clindamycin in nucleus of intervertebral discs in rabbit
    YUA N Cheng, SUN Gang, HUANG De-Qing, ZENG Lin
    1998, 3(4):  269-271. 
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    Aim The distribution of four antibiotics:penicillin G,cefazolin,tobramycin and clindamycin in the nucleus of intervertebral discs in New Zealand rabbit was studied.Methods At 0.5 and 1 hour after ear intravenous injection,the concentration of four antibiotics in serum and in nucleus in infected intervertebral discs of rabbits were determined by high performance liquid chromatography methods.The antibiotic concent rations of serum and nucleus w ere compared.Results The ratios of nucleus to serum antibiotic concentration were ranged from low to high in asequence of penicilin G,cefazolin,tobramycin and clindamycin.The ratioes for the antibiotics,except for penicillin G,were increased in infected rabbit,with the ratios for tobramycin and clindamycin increased markedly (P<0.05).The rate of removing on the antibiotics from nucleus was lower than from serum.Conclusion There is no interrelation of cerum and nucleus in antibiotic concentrations.Clindamycin and tobramycin are the antibiotics of shoice in treating infected intervertebraldiscs.
    Effects of 17β-estradiol on isolated pig basilar arteries
    CHU-Min, SUN De-Fu, LI Xiang-Duan
    1998, 3(4):  272-274. 
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    Aim and Methods The relaxing and inhibitory effects of 17β-estradiol(E2)on KCland 5-HT induced contraction of isolated pig basilar arteries were observed.Results After incubation with E2(10-5,10-4.2mol/L),the phasic contract ion induced by KCl was inhibited in a concentration-dependent manner in artery rings(IC50was10-4.8mol/L),and the concentration effect curve generated by 5-HT was also inhibited (pD2'was4.57).Conclusion E2 has vasodilatory effect on isolated pig basilar arteries.
    Effect of Kangshuaiming mixture on ability of learning and memory of mice
    GAO Mei-Hua, LI Jing-Mei, YANG Jun, WA NG Jing
    1998, 3(4):  275-278. 
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    Aim The effect of Kang shuailing mixture on ability of learning and memory of mice was observed.Methods Mice were given different chemical substances to build special experimental models.With the methods of passive avoidance reaction (stePdown test,stePthrough test and labyrinth test)the action of Kang shuaining mixture was observed.Results The experiment show ed that Kang shuaining mixture could decrease the learning disorder caused by scopolamine,promote the ability of memory of mice with spaceorientation disorder caused by per tobarbital sodium,and antagonize disorder of memory consolidation induced by sodium nitrite and disorder of memory reappearance induced by ethanol.Conclusion Kang shuaining mixture possess obvious effects on learning and memo rypromotion at different levels.
    Evaluation of bioavailability and pharmacokinetics of film-coating special shaped tablet of acetaminophen in health volunteers
    TANG Chun-Ping, JIN Miao-Zhen, ZHEN Yi-Yue, FEN G Yi-Fan, OU Shao-Ying, MENG Qing
    1998, 3(4):  279-281. 
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    Aim The pharmaco kinetics and relative bioavailability of domestic film-coating special shaped tablet of acetaminophen were studied.Methods A single oral dose of 500 mg of the two formations (test and reference preparation)was given to 10 healthy male volunteers according to randomized 2-w ay cross-over design,blood sample was with drawn 10 hours after administ ration,and plasma concent rations of acetaminophen were assayed by a high performance liquid chromtography (HPLC)method.Results The concentration-time curves of the two preparations fitted to a one-compartment model with first order absorption and lag time.The main pharmacokinetic parameters of the tested preparation were as follows:Cmax=5.51±1.24 mg/L,Tpeak=1.03±0.43h,T1/2k a=0.27±0.16h,T1/2ke =2.60±0.51h,AUC0~t =23.69±4.08 mg·h·L-1,MRT=3.65±0.22 h.Conclusion The relative bioavailability of the test preparation is 102.5±13.3% to the reference preparation.The bioavailabity of the two kinds of acetaminophen is equal,showing that the two kinds of preparations are bioequivalent preparations.
    The preparation of corneal collagen shield and its clinical application
    ZHAO Shi-Hong, GUO Lian-Zheng, HOU Qin-Ying, WANG Kai-Hui
    1998, 3(4):  282-284. 
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    Aim The method of preparing corneal collagen shield and its the rapeutic effect teating Herpes Simplex Kera tit is (HSK)w ere studied.Methods Collagen was extracted from sclera of pig.Using centrifugal method to make corneal collagen shield.After soaked with Aciclovir (ACV),the corneal collagen shields w ere used for treating HSK.Results The results indicate that in the grouPof corneal collagen shield soaked with ACV the average recover time of cornea was 9.45 days,in the grouPof instillation of ACV eye drops the average recover time was 14.36 days.The curerate and effective rate of the two groups were 90.63%、65.63% and 96.88%、81.25%(P<0.05).Conclusions The corneal collagen shield immersed with ACV will play an important role in HSK treatment.
    Recent advances in pharmacologic prevention and treatment of osteoporosis
    XU Mei, XU Jing-Wen
    1998, 3(4):  288-298. 
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