Table of Content

Volume 4 Issue 2
26 June 1999

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Change of the blood apparent viscosity following tranumatic brain injury and the effects of iloprost on it

LIU Hai-Peng, ZHANG Ke-Cheng, CAI Wen-Qin, XU Shi-Rong

1999, 4(2):  81-84. 

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Aim The change of the blood apparent viscosity following traumatic brain injury and the effect of iloprost on it were observed.Methods The mode rate brain trauma of rabbits was produced with the PBI-Ⅱ type injury device.The brain trauma was treated with iloprost (30 μg·kg^-1, iv).The blood samples at 1、6 and 24 h following brain trauma were collected.The apparent viscosity was measured with The Low Shear 30, and the hematocrit was measured meanwhile.The coefficient of the power function and the calculative apparent viscosity at the time when the hematocrit was 0.40, were compared.Results The blood viscosity was significantly increased at 1 h after brain trauma, and was increased continually at 6 h, but at 24 h it was distincly decresed as compared with that at 6 h.It was more increased after brain trauma at low shear than that in the control group.The blood viscosity both in the trauma and control groups was markedly decreased by the effects of iloprost. Conclusion The changes of the blood viscosity after brain trauma may play a role in the occurrence of the secondary brain damage.iloprost may be an effective drug for treating traumatic brain injury.

Caffeic acid, ferulic acid:a new kind of non-peptide endothel in antagonist¹

WANG Feng, LIU Min, YANG Lian-Chun, WANG Jing-Yuan, CAI Qing, LU Min, LI Fei

1999, 4(2):  85-92. 

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Aim The antagonist effects of cinnamic acid compounds of caffeic acid and ferulic acid on endo thelin-1 biological responses and their antagonist mechanism to endothelin-1 were studied.Methods Caffeic acid and ferulic acid, in different dosage were separately given int raperitoneally to mice and intravenously torats.The protective effect on acute death of mouse and the vasodilatative effect on constriction of isolated rings induced by ET-1 and the change of blood pressure of normotensive rats were observed.The drugs were also administered orally to DOCA-salt hypertensive rats, and the body weight, cardio vasculartissues wet weight, gene expression of ET-1, c-fos and HSP70 mRNA, plasma levels of ET-1 in DOCA-salt hypertensive rats were measured.By binding experiment of ¹²⁵I-ET-1 with 3T3 cells.The antagonism of Caffeic acid and ferulic acid on ET-1 was determined.Results Both Caffeic acid and ferulic acid could dose-dependently delay the acute death induced by ET-1, blunt the elevation of blood pressure on normotensive rats markedly, dilate the vasoconstriction of isolated aorticrings, blunt the elevation of systolic blood pressure and development of cardiov ascular hypertrophy in DOCA-salt hypertensive rats, inhibit gene expression of ET-1, c-fos, HSP70 mRNA and decrease the plasma levels of ET-1.both of them bind compet itively with ¹²⁵I-ET-1 on 3T3 cells. Conclusion Caffeic acid and ferulic acid are a new kind non-peptide ET antagonists.

Effect of vanadate given by gavage on OGTT and glucoregulatory hormones in STZ-diabetic rats

JIN Wen-Sheng, ZHANG Zhong-Hui, ZHANG Ping

1999, 4(2):  93-97. 

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Aim The antihy perglycemia effect of vandate in a certain do sage and the concurrent change of relevant hormones were observed.Methods Gavage method was employed to introduce sodium or thovanadate (20 mg·kg^-1·d^-1, 2 wks)into Wistar rats with or without diabetes, and oralglucose tolerance test (OGTT), glucose-induced insulin secretion curve (GIISC), body weight and serum levels of glucagon and corticosterone were detected.Results This dosage of vanadate did not exert significantly inf luence on OGTT and serum levels of glucagon and corticosterone, but inhibited maximal insulin secretion and body weight gain in normal rats.In diabetic rats, by contrast, OGTT was improved significantly and the elevated glucagon and corticosterone were reduced markedly or normalized by vanadate, but body weight and GIISC did not change significantly. Conclusion Vandate in such dosage lowers glycemia effectively, ameliorates the disorder of glucose homeostasis and glucotropic hormones, but has obvious side-effect on body weight.

Influence of bupivacaine combined with dexamethesone on epidural blockade

ZHANG Yuan-Xin, AN Feng-Mei, HOU Shu-Jian, SHUN Hui-Zen, ZHANG Hai-Ling, GAO Zhong-Yu

1999, 4(2):  98-100. 

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Aim The efficacy of bupivacaine administered alone or in combination with dexamethesone in epidural blockade was observed.Methods 120 cases of microsurgical operation in lower extremities were randomly divided intofour groups in double blind form,.The bupivacaine (0.75%, 1.4 mg/kg) was administered alone in the control group(A) and in combination with different doses of dexamethesone(0.075、0.15、0.3 mg/kg)in the test groups (B,C and D)respectively.The anesthetic time, postoperative analgesic time and the effect of neuromuscular blockade in each group were compared.Results The onset time in the test groups was shorter than that in the control group, and the anesthetic time and postoperative analgesic time in the test groups were longer than those in the control group. Conclusion The efficacy of bupivaceine combined with dexamethesone was superior to that of it alone in epidural blockade.

Microcalorimetric study of ant iviral effect of antiviral antibiotic 17997

LU Jian-Hua, TAN An-Min, TAO Pei-Zhen

1999, 4(2):  101-103. 

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Aim and Methods The thermog enesis curves of Vero cells infected by HSV-Ⅰ and the effect of 17997, a newly-found antiviral antibiotic, on the duplication of HSV-Ⅰ were determined by the LKB 2277 themal activity monitor.Results We found that HSV-Ⅰ interfered a with the metabolism of the Vero cells that had been infected and there was an increase in the heat production.When the Vero cells were treated with 17997 at the concent ration of 1×10^-6mol·ml^-1, the thermo genesis curves can decline to that of normal metabolism of Vero cells. Conclusion The antibiot ic 17997 can inhibit the duplication of HSV-Ⅰ and has no effect on the metabolism of Vero cells.

Cardiotoxicity of sodium γ-hydroxybutyrate and ketamine in neonatal primary myocardial cell cultures

ZHANG Tie-Zheng, WANG Feng-Xue, LUO Jun, CHEN Wei

1999, 4(2):  104-107. 

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Aim The cardio to xicity profile of sodium γ-hydroxy butyrate and ketamine was investigated.Methods 4 day-old cultured neonatal primary my ocardial cells obtained from 2to3-day-old Wistar rats were divided into 5 groups, with group C serving as control and groups HL, HH, KL and KH treated with sodium γ-hydroxy butyrate (3×10^-3 mol·L^-1 and 3×10^-2 mol·L^-1) and ketamine (1×10^-5 mol·L^-1 and 1×10^-4 mo l·L^-1)for 8 h. The contractility、morphology and cytoplasmic enzyme (LDH,AST, CK and ALP)release of my ocardial cell and the concentration of elect rolytes (K⁺, Na⁺, Cl-and Ca²⁺)in the medium were measured 8 h following the intrav enous anesthetics administ ration.Results In group KL, the beatingrate of neonatal my ocardial cell was increased (P<0.05), while in group KH decreased significantly (P<0.05).The release of LDH and AST in the cell cultures of group KH was increased and ALP decreased (P<0.05)associated with an adve rse effect on morphology.The results show that group HL, HH and KL had little or no effect on all indices of toxicity evaluated electrolytes were not significantly different between groups. Conclusion The high concent rations of ketamine has significant direct myocardial depressant action, while sodium γ-hydroxy butyrate and low concent rations of ketamine have little or no effect on cardio to xity, in fact, the low concent rations of ketamine has positive chronot ropic and inot ropic action.

Pharmacokinetics of sparfloxacin in the patients with abnormal kidney function

LIANG Zhu, ZHANG Ying-Wei, PAN Han-Qing, ZHANG Ai-Ping, YUAN Cheng

1999, 4(2):  108-111. 

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Aim To observe pharmaco kinetics of sparfloxacin in the patients with abnormal kidney function.Methods Sparfloxacin concent ration in serum and urine of ten patients were measured by a reversed phase high performance liquid chromatography method after having a single dose and multiple dose of 200 mg sparfloxacin tablet.The Pharmacokinetics parameters were computed with program PKBP-N₁.Results The main pharmacokinetics parameters at single dose of sparfloxacin were T_1/2(ka) =(1.02±0.22)h, T_1/2(β)=(15.73±3.20)h, T_peak =(3.88±0.75)h, C_max =(0.59±0.17)mg·L^-1 and AUC_0-∞=(11.25±2.13)mg·h·L^-1, while at multiple dose were T_1/2(ka)=(1.25±0.27)h, T_1/2(β)=(16.90±4.13)h, T_peak =(4.18±0.78)h, C_max =(0.79±0.21)mg·L^-1 and AUC_0-∞=(13.34±2.25)mg·h·L^-1.The discharge rate in 24h of original sparfloxacin in urine were (10.58±1.47)% and (11.08±1.94)% separately.C_max and AUC in multiple dose were marked higher than in single dose(P<0.05).The retainfactor was 1.19. Conclusion The pharmacokinetics parameters of sparfloxacin are not signi ficantly changed in patients with middle-abnormal kidney function had not change.

Relative bioavailability and bioequivalence evaluation of gliclazide tablets

XU Rong-Qing, DENG Shi-Shan, XIA Zhi-Lin, GUO Shun-Min

1999, 4(2):  112-114. 

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Aim To compare relative bioavailability and bioequivalence of gliclazide tablets. Methods Ten healthy male volunteers in two groups were given orally gliclazide tested and reference tablets (160 mg)in randomized crossover study.The serum concentration of gliclazide was assayed by HPLC and the bioequivelence of two formulations was evaluated by analysis of two onesided tests.Results Serum concentration-time curves of gliclazide fitted to an one-compartment open model.T_max were (4.272±0.631)h and (4.031±0.574)h, C_max were (7.497±0.935)μg·ml^-1 and (7.408±1.171)μg·ml^-1 and AUC were (104.986±27.523)μg·h·ml^-1 and (108.232±22.437) μg·h·ml^-1 for tested and reference tablets, respectively.The relative bioavailability of gliclazide tested tablet was 96.679%. Conclusion The tested and reference tablets of gliclazide are of bioequivalence.

Preventive effect of Naoluotang, a compound of Chinese medicine on experimental atherosclerosis in quails

ZANG Dong-Lian, XU Qing-Rong, HU Bing

1999, 4(2):  115-118. 

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Aim The effects of Naoluotong, a cempeund of Chinese medicine on atherosclerosis were studied.Methods One hundred and twenty male quails were divided at random into 6 groups.The quaits in 5 groups, including the control group,Naoluotong (3, 6, 12 g·kg^-1·d^-1)groups, and Yuejiancao oil (6 g·kg^-1·d^-1)group, received hyper-f at forage, and in the six th group were fed on stock diet.Half of the quails in each group were kill 4 wk after.The levels of TC, TG, LDL-C,V LDL-C and HDL-C in serum were measured in Biochemilal method.The remainder quails were fed on above forege continuously for another 4 wk and then were killed.The levels of TC, TG, LDL-C,V LDL-C and HDL-C in serum and the contents of TC and TG in myocardium and aorta were tested, and the change of endo-aorta was determined.Results The levels of TC, TG, LDL-C and V LDL-C were decreased, the level of HDL-C and the v atio of HLD-C/TC were increased by Naoluotong (6, 12 g·kg^-1·d^-1)in the quails fed on hyper fat forage for 4wk (P<0.05, P<0.01).In the remainder quails which were raised for 8wk, the above items were similar to the quails fed for 4wk, the effelts of Naoluotong was dose-d ependent in adjusting blood lipid, and the contents of TC and TG in aorta and myo cardium were decreased (P<0.05)and the lesion of endo-aorta was also improved by Naoluotong (6, 12 g·kg^-1·d^-1). Conclusion Naoluotong has the action to adjust blood lipid-adjusting and to antag ouise atherosclerosis.

Inhibitory effect of Bezoar Qianjinsan on central nervous system

XU Qing-Rong, LI Na, XU Yong, LIU Wei-Dong, TIAN Chun-Lin, WANG Xin-Jun

1999, 4(2):  119-121. 

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Aim To explore the inhibitory effect of Bezoar Qianjisan on central nervous system.Methods Bezoar Qianjinsan was applied to mice via stomach to observe its effect on the convulsion induced Caffeine sodium benzoate, or elect rostimulation and the spontancous activity of mice.Bezoar Qianjinsan was also applied together with pentobarbital sodium or codeine to observe the hypnotic effect by test ing the disappearance of ref lex 15 min after drug application, or the analgesic effect by observing mice's writhing motion.Result Bezoar Qianjinsan could antagonize drug or ellevtrost imulation induced convulsions obviously, enhance the hypnotic action of pentobarbital sodium, potentiate the analgesic effect of codeine, and to some extent reduce the spantaneous activity of mice.The da ta were statistically very significant as compared with those in the control group(P<0.01). Conclusion Bezoar Qianjinsan could inhibit central nervo us activity of mice.

Effects of lidocaine and propofol on the activities of myocardial sarcolemmal Na⁺-K⁺-ATP ase and sarcoplasic reticulum Ca²⁺-ATPase following ischemia-reperfusion

LIU Hong-Liang, DAiti-Jun, WANG Jun, ZEN Yin-Ming

1999, 4(2):  140-143. 

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Aim To investigate the effects of lidocaine and propofol on the activities of myocardial sarcolemmal Na⁺-K⁺-ATPase and SR Ca²⁺-ATPase following ischemia-reperfusion. Methods forty-eight rats were randomly divided into six groups:Sham group(the coronary was not sutured), NS group (saline 5 ml·kg^-1), L5 group (lidocaine 5 mg·kg^-1), L₁₀ group (lidocain 10 mg·kg^-1), P300 group (propofol 300 μg·kg^-1·min^-1)and P1000 group (propofol 1000 μg·kg^-1·min^-1).Five minutes before ischemia, Saline or lidocaine was injected intrav eneously within 30 seconds and propofol was infused intraveneously till the onset of ischemia.The left coronary artery was occluded with a silk suture for fifteen minutes, then loosened to achieve reperfusion for ten minutes.The activities of sarcolemmal Na⁺-K⁺-AT Pase and SR Ca²⁺-A TPase were measured with pho to colorme-t re.Results Compared with that in NS group the activ ities of S R Ca²⁺-A TPase in the lido caine groups were increased significantly (P<0.05), while the activites of sarco lemmal Na⁺-K⁺-A TPase in propofol groups were increased significantly(P<0.05, P<0.01 respectively).Propofol of 1000 μg·kg^-1·min^-1 could increase the activity of SR Ca²⁺-ATPase (P<0.05).Lidocaine of 10 ml·kg^-1 could increase the activity of sa rco lemmal Na⁺-K⁺-ATP ase significantly (P<0.05). Conclusion Lido caine, propofol could attenuate my ocardial ischemia-reperfusion injury by increasing the activities of sarcolemmal Na⁺-K⁺-ATPase and SR Ca²⁺-AT Pase during reperfusion.

Inhibitory effects of DDPH on contraction of isolated ileum of guinea pigs induced by some mediators

HU Guo-Sheng, HUANG Xian-Ju

1999, 4(2):  143-146. 

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Aim To investigate the effects of 1-(2, 6-dimethy lphenoxy)-2-(3, 4-dime thox ypheny-lethy lamino)pro pane hydrochloride (DDPH)on cont raction of isolated ileum of guinea pigs induced by some mediators.Methods The routine methods for experiment on contraction-effect of the isolated ileum were emplayed.Results Histamine, acetyl choline and CaCl₂ separetely caused a significant cumulative concentration-related effect on ileum constraction with the pD₂ values being 7.7、9.8 and 5.3 respectively.after being incubated with DDPH of different dosage for 15 min, the responses elicited by Hist.ACh and CaCl₂ were depressed and the pD₂'values were 4.0, 3.8 and 3.9 respectively.Cumulative concent ration of DDPH and verapamil Resulted in a concentration dependent relaxing effect on contraction of ileum induced by K⁺ 60 mmol·L^-1 with the IC₅₀ values being 2.7 μmol·L^-1 and 0.7 μmol·L^-1. Conclusion DDPH has significant relaxing effect and a calcium antagonistic effect on ileum.

Study on the postantibiotic effects of twenty ant imicrobial agents against S.aureus

WANG Rui, FANG Yi, CHEN Qian, LIU Gui-Yang, LIU Qing-Feng, LIU You-Ning

1999, 4(2):  146-149. 

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Aim The postantibiotic effects (PAE)of 20 ant imicrobial agents against S.aureus collected from patients with nosocomial infections were studied.Methods PAE was determined by the spectrophotometric method and calculated by the difference of time in regrow th phase of bacte ria between tested and controlled groups.Results The PAE of β-lactams against S.aureus was short, but PAEs of macrolides, fluroquinolones and amino glycosides and fosfomycin were marked, especially PAEs of macrolides were up to 2 h in sub-MIC.PAEs of penicillins and carbenpenem were longer than that of cephalospories, PAEs of macrolides, aminoglycosides and fluroquino lones were obviously longer than PAEs of β-lactams in four times of MIC of the drugs. Conclusion PAEs of the antimicrobial agent s, which inhibite synthesis or proteins of DNA, and fosfomycin are significant longer than that of β-lactams(it may be associated with different action mechanisms).

Effect of pseudoephedrine hydrochloride mixture on the histamine-induced contraction of isolated bronchial smooth muscle in guinea pig ＆ the prescription analysis for the mixture

CAO Fang, LIU Shu-Qing, FENG Wei-Yi, KANG Ai-Qun, YANG Bing-Xing

1999, 4(2):  150-152. 

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Aim ＆ Methods The effect of pseudoephedrine hydrochloride mixture, a compound consisting of pseudoephedring hydrochloride, dextromethorphan hydrobromide and chlorpheniramine, on the histamine-induced cont raction of guinea pig bronchial smooth muscle was studied in vitro by the method of receptor kinetics.Results ＆ Discussion The result showed that H1 receptor of histamine in isolated bronchial smooth muscle was competitively blocked by chlorpheniramine and noncompetitively blocked by pseudoephedring hydrochloride. Though the significant antagonism on the H₁ receptor was not observed with dextrome hydrobromide alone, synergetic asthma-relieving effects were shown as the medicine was simultaneously administ rated with pseudoephedring hydrochloride or chlorpheniramine.furthermore, when these three drugs were simultaneously administ rated, the most obvious synergetic could be observed.