Table of Content

Volume 3 Issue 2
26 June 1998

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Clinical pharmacokinetic study on levonorgestrel and possible accumulation after long-term treatment of themonthly combined oral contraceptive

ZHOU Xiao-Fei, SHAO Qing-Xiang, HAN Xue-Jun, WENG Li-Ju, JING Xiao-Ping, SANG Guo-Wei

1998, 3(2):  81-84. 

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Aim With comparison of pharmacokinetic profiles of levonor gestrel after single and mul tiple administration of thecombined oral contraceptive, this study would provide pharmacokinetic data for safety evaluation on proloned treatment of this monthly long-acting oral contraceptive.Methods Nine healthy fertile women received themonthly combined oral contraceptive (containing LNG 6 mg and quinestrol 3 mg) for up to 1 year.Blood samples werecollectedimmediately prior to drug intake and at consecutive timepoints after oral administration for determination of serum LNG by RIA.Intraindividual comparison was appliedin this long itudinal study.Results Serum LNG concentration-t imecurve showed an open two compartment model after single dose administration, with 2.86±1.60 hours for αT_1/2 and 1.52±0.35 days for βT_1/2.C_max of LNG was observed after 2.56±1.13 h in the1sttreatment cycle.Mean C_max was 141.36±70.20 nmol/L with signif icant interindividual variation.C m ax in 12 th treatment cyclereached to 314.83±128.55 nmol/L, which was much higher than that in the1st cycle. AUC_0~28 were 182.42±135.85 and 533.96±319.31 nmol/L·d^-1, respectively, also showingstatistically significant difference.There was no meaning ful di fference on T_max after sing le and mul tiple do sing.Themean value of βT_1/2 in the12th dosing was 1.67±0.48 days, which showed no ma rked changes, sugg esting that multiple do sing did no t influence thevelocity of drug metabolism.C_d21 declined below 100 pg/ml.Conclusion There was no obvious accumulation of LNG afterrepeated dosing of this monthly long-acting combined oral contreceptive.

Effects of estrogen on intimal thickening and impairment of vascular function after carotidinjury in rats

CHENG Xun-Min, ZHANG Ping, WANG Guo-Chao, HE Guo-Xiang

1998, 3(2):  85-88. 

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Aim Effects of estrogen on theproliferation of vascularsmooth muscle cells and theimpairment of endon thelium-d epentment vascularrela xation after vascular injury were studied.Methods Ovariectomized Wistar rats wererandomly dividedinto two subgroups treated with either 17βestradiol or vehicle and were subjected to balloon injury of theleft common carot id artery.Two weeks later, thedeg rees of myointimal thickening and proliferation of vascularsmooth muscle cells (VSMC)were evaluated by morphometric analysis and immunostained against proliferating cellular neuclear antigen (PCNA).Acety lcholine-induced endon thelium-depende ntrelax ation was measured.Results 17βestradiol signi ficantly inhibited theproliferation of VSMC (P<0.05)and attenuated neointimal area (P<0.05). Acety lcholine-induced endon thelium-dependentrelax ation was greatly reducedin injured arteries, with themax imal relax ation being 12 %±6 %.Estradiol ameliorated signif icantly theimpairment of vascularrelaxation, with themaximal relax ation being 48 %±9 %.Conclusion Estradiol can inhibitsmoo th muscle proliferation and ameliorate thedecrease in endon thelial-dependentrelax ation after balloon injury.

Appl ication oforthogonal t value methodin analyzing theprimary drugs in compound 961, a traditional Chinese medicine

LIU Hui-Bo, LI Lin, LI Bing, ZHANG, Li AN, Wen-Lin

1998, 3(2):  89-93. 

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Aim To analy ze theprima ry drugs of compound 961, which is composed of 10 t raditional Chinese drugs.Methods Theexperimental design was made by theortho gonal t value method put forw ard by Sun WM and Sun RY.Results and Conclusion A simplif ied and more Effectiverecipe compound 962, consisting of 6 drugs was formulated and preparedandits pharmacological eff icacywas verfied.Theuse oforthogonal t value method merits wider application in studying mult iing redientrecipes of t raditional Chinese medicine.Thecharacteristics of thedisease, thepharmacolog ical Effects of thet raditional Chinese drugs, theuse of mult iple animal models and mutiple parameters are factors thatrequireconsideration in research.

Effect of Gui Qi San andits separated prescription on immunoregulative effect in mice

ZHU Xiao-Xin, WANG Meng, WU Dun-Xu, ZHANG Yu-Zheng, GONG Bin, FANG Zhao-Qin, XU Pin-Chu, WANG Ren, XI Pei-Li, LIAO Han

1998, 3(2):  94-97. 

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Aim Theimmunoregula tive Effect of Gui Qi San andits separated prescription on immune functions of mice was to be studied.Methods Theeffect of Gui Qi San and its separated prescription only mphocytes was observed after theimmune function of mice was damaged by cyclophosphamide.Results They could evidently counteract mice spleen degeneration caused by cyclophosphamide or improve their life quality, promote immunosuppressied mice T.Blymphocytes proliferation, act ivate NK cells, increase CD⁴⁺/CD⁸⁺cells ratroby increasing CD⁴⁺ cell, and lowerecAMP level in spleen cell.Thecompo site prescription had bettereffectthan its separated prescription and PSP.It had no Effect on immune function of normal mice.Conclusion Gui Qi S an andits separated prescription hadimmunoregulative Effect on immunosuppressied mice.

Effects of scopolamine on intravenous morphine self-administration and reinstatement of responding in rhesus monkeys

ZHA NG Fu-Qing, ZHOU Wen-Hua, WANG Zhao-Lin, YANG Guo-Dong

1998, 3(2):  99-102. 

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Aim To study theEffects of scoplamine, a marscarinicreceptor antagonist on intravenous morphine self-administration and reinstatement of responding in rhesus monkeys (fixed ratio 1, FR1).Methods Rhesus monkeys were trained to press response lever for intravenous morphine self-administration under a fixed ratio 1 schedule in a daily 4 h session.Response pattern, total responserate, total mophine intake and spontaneous activity wererecorded duringsessions.Effects of acute pre treatment with different doses of scopolamine on self-administration were studied, and alson theEffects of acute and chronic treatment with scopolamine on reinstatement of responding by priming dose of morphine were observed afterext inction of self-administration were observed.Results Theresul ts showed that acute treatment of scopolamine (0.025 ~ 0.75 mg/kg)could not only attenuate intravenous morphine self-administration under a F R1 schedule, which was represented by decreased total morphine intake and responserate persession, but also delay theinitiation of morphine self-administration.Theresponse pattern was affected under this treatment.Chronic Effect of scoplamine was also evaluated afterext inction during which a daily dose of scopolamine(0.25 mg/kg)was administered, andin thetesting day, only a priming dose of morphine (0.25 mg/k g)was administered.Chronic scopolamine treatment caused 45 % decrease of responserate by morphine priming.Conclusion Chronic scopolamine treatment might inhibitthereinstatement of responding afterextinction.

Effect of China-produced enalapril on long-term life quality of patients with dilated cardimyopathy and severecardiac dysfunction

PENG Ying-Xin, HUANG Xi-Zheng, WANG Zhen-Qi, ZHANG De-Lan, YANG Su-Jie

1998, 3(2):  103-104. 

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Aim and Metheds Theinfluence oforal enalapril on long-term quality of life was obser vedin 41 patients with dila ted cardiomyopathy and severecardiac dy sfunction (N YHA class Ⅲ-Ⅳ, left ventricularejective f raction<30 %), Theoral enalapril(10 ~ 40 mg/d ay)was give n for 24 months in addition to digitalis, diure tic drog and vasodilators (nitraes mainly).Results Follow-up rate was 95.1 %.Themaximal six-minute-walking distance was increased by 43.0 % (P<0.01)and exercisetolerance and t imewere increased by 73.1% and 61.4%, respectively (both P<0.001)and left ventriclesystolic parameters were improvedinvarying deg rees.Conclusion Thelife quality of patients with cardiomyopathy and severecardiac dysfunction could be greatly improved by administration of enalapril.

Effect of bupivacaine combined with procaine or lidocaine on thebrachial plexus blockade

ZHANG Yuan-Xin, HU Shuang-Gui, GAO Zhong-Yu, DONG Xi-Gui, ZHANG Hai-Ling

1998, 3(2):  106-108. 

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Aim Theonset of complete blockade of brachial plexus andits sustained t imecaused by bupivacaine alone or by thedrug in combination with procaine and lidocaine werecompared.Methods 8086 patients received forearm and hand operations wererandomly dividedinto three groups, namely bupivacaine, bupivacaine plus procaine and bupivacaine plus lidocaine groups.Results Theonsett imeof complete block was shorter andits sustained period was long er in bupivacaine plus lidocaine group than theon ther groups (P<0.05 or P<0.01).When used with adrenlline, bupivacaine in any dosage w ould bring along er sustained period time(P<0.01). With theanesthetic dose decreased, there was a drop in theonsettimeof complete blo ck and thesustained period.Conclusion All theanesthetic methods could be usedin upperlimb's operations in patients who have different pathogenies, phy siques and operative times.

Protective Effect of dexamethasone on human fetal heart cells in culture infected by coxsackie B-2 virus

WANG Jian-Xin, YU Bu-Yun

1998, 3(2):  109-111. 

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Aim Theeffects of Dexamethasone(Dex) on human fetal heart cells intected by Coxsackie B-2 virus were studiedinvitra.Methods Thelevels of LDH were de termined, thecytopathic effect (CPE), thebeat ing of heart cells and electromicroscopic findings were observedin cultured heart cells infected by coxsackie B-2 virus.Results LDH levels were much low er in theDex-treatedinfected group than those in theinfected group.Less CPE could be foundin theDex-treatedinfected group, while theCPE appeared rapidly in theinfected group atthesameintervals.Atthefi rst day, themyocytes showed nearly normalul trastructure in theDex-treatedinfected group, how ever, themi tochondrial cristae were unclear in theinfected group.Conclusion Dexamethasone exerted someprotective Effects on cultured human fetal heart cells infected by Coxsackie B-2 vi rus.

Clinical comparison of ant ibacterial action of sparfloxacin with lomefloxacin

WANG Rui, WANG Ya-Qin, FA NG Yi, LIU Qing-Feng, JI Shu-Guo, WANG Yue-Song

1998, 3(2):  112-114. 

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Aim This study aimed at clinical comparative trial of sparf loxacin (SPLX)with lomef loxacin (LMLX).Methods Tw enty four patients with bacterial infections in respiratory tract or urinary tract wererandomly seperated to two groups of SPLX and LMLX.Af ter administration of 200 ~ 300 mg of SPLX once daily or 200 ~ 400 mg of LMLX twice daily, theclinical Effects were observed and defined as cure, obvious efficiency, effcativeness and no Effect.Results Isolation rate of bacteria from patients was 91.7 %.Total intake amount of SPLX was signi ficantly less than that of LM LX, but curerate and effectiverate in group SPLX were signi ficantly higher than in group LM LX.There were no adverse drugractions in both groups.Conclusions SPLXis a safe and effective drug among fluoroquinolones in treatment of bacterial infections.Theratio of Effect over dose of sparf loxacin is higher than that of lomefloxacin.

Effects of Dafang Tea on blood-lipid and weightreduction in obeserats

YANG Jun, LIU Xing-Shun, Koinosuke Hayashi

1998, 3(2):  115-118. 

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Aim TheEffects of Dafang Tea on blood-lipid and weightreduction was investig ated.Methods Newly born baby rats wereadministered subcutaneously with monosodium glutamate(MSG)for five consecutive days.With biochemistry and morphology methods, theeffects of Dafang Tea on obeserat models andits mechanism were studied.Results Dafang Tea possessed obvious Effects of lowering theserum level of tricyleride, inhibiting fat absorption in intestinal tract and promoting fa t metabolism.Dafang Tea (4.05 g/kg)had remarked Effect on weightreduction, in comparion with that in other groups.Conclusion Hig her concentration of Dafang Tea can serve as one kind of keep-fi t agent.

Observation of antagonism of aescuven forte tofree oxygen radical injuries in superf icial venons vericosis of legs

WANG Chun-Xi, JIA Run-Ying, ZHAO Weng-Guang, ZANG Guang-Sheng, YAO Di

1998, 3(2):  120-121. 

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Aim Theantagonism oforal Aescuven forte tofree oxyg neradical injuries in superf icial venons vericosis of legs was to be observed.Methods Theserum levels of SOD, GSH, LPO in 60 patients with superf icial venous vericosis in legs were determined by radioimuno assay, DTNB method and TBA method.Results All patients had high level of serum LPO and low levels of serum SOD and GSH.All levels above could re turn tonormal aftereffective treat-ment with Ascuven Forte.Conclusion This study sug gested that thedeter mination of SOD, GSH, LPO is helpful to investig ate themechanism of illness and treatment, and to providereliable laboratory indexes for oral medicine use.

Protective Effect of Pulastiua chinensis on hepatic toxic injury induced by combining rifampin with isoniazidin mice

LU Xi-Ming, WANG Jian-Gang, WANG Xue-Ting, WU Ying-Ping, WANG Shu-Ying, LI Yan

1998, 3(2):  122-123. 

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Aim Theprotective Effect of pulastiua chinensis (PC)on hepatic toxic injury induced by combinig rifampin with isoniazid was to be observedin mice.Methods Theliver index, level of SGPT, content of MDA of liver homogenate, and degree of liver cell injury were invest igatedin mice.Results PC could decreasethelevel of SGPT, theconte nt of MDA and thedeg ree of liver injury (P<0.01).Conclusions PChas theprotective Effect on hepatic toxic injury induced by combining rifampin with isoniazidin mice.

Pharmacokinetics and bioavailabil ity of astemizole tablets

LIU Jun-Bao, CAO Qi, YANG Guang-De, YANG Yin-Jing

1998, 3(2):  124-126. 

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Aim and Methods Thepharmacokinetics and bioavailability of thedomestic and theimported astemizole tablets were studiedin 6 Chinese healthy volunteers by radioimmunoassay in a clinical trial of cross-over design.Results Themain pharmacokinetic parameters calculated by thepractical pharmacokinetics program 87 wereas follow s:For thedomestic product, Vd=5.34±1.85 L;αT_1/2=0.74±0.37 h;βT_1/2=286.10±220.11 h;CL=0.052±0.031 ng/ml;T_max=1.56±1.32 h;C_max=1.04±0.10 ng/ml;AUC=262.69±162.18 ng/ml·h^-1.For theimported product, V d=8.24±2.56 L;αT_1/2=1.16±0.98 h;βT_1/2=260.38±260.37 h;CL=0.089±0.079 ng/ml;T_max=1.37±0.82 h;C_max=0.93±0.14 ng/ml;AUC=250.66±148.05 ng/ml·h^-1.Therelative bioavailability of thedomestic tablets was 127.8 %.Conclusion No signif icant pharmacokine tic difference has been found be tw een thedomestic andimpor ted astemizole tablets.

Effect of benazepril on hypertensive left ventricular hypertrophy and ventricular arrhythmias

WANG An-Cai, JI Qin-Jiong, ZHU Xiang-Ming

1998, 3(2):  127-128. 

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Aim To invest igate theEffect of benazepril on hypertensive left ventricular hypertrophy(LVH)and ventricular a rrhy thmias (VAs).Methods Thecardiac shape and arrhy thmic prevalencc were detected by 24h ambulatory electrocardiographic monitoring and Colour Dopplerechocardiog rphy beforeand 6 months after taking benazepril in 56 cases of hypertensive patients.Results Theincidences of VAs and Lown's grade ≥3 ve ntricular arrhy thmias were 77.7 % and 48.1 % in 27 cases with LVH, significantly higher than 34.4 % and 10.3 % in 29 cases without LVH (P<0.01).Remarkableregression of IVS, LVPW and LVMI was found after half yeartreatment of benazepril (P<0.05 or 0.01), so did LA (P<0.01).Meanwhile, theincidence of VAs, particularly complexventricular ar rhy thmias was significantly decreased.Conclusion Benazepril has a favorable Effect on hypertnsive left ventricular hypertrophy and ventricular a rrhy thmias.