Table of Content

Volume 9 Issue 11
26 November 2004

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Current researches of angiotensin receptor blockers in treatment of patients with chronic progressive renal disease

WU Ji-Ning, LIU Bi-Cheng

2004, 9(11):  1201-1204. 

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The renin-angiotensin system plays an important role in the progression of chronic renal disases. At present, the main lapproach for treating the chronie prognessive renal disease is to block the role of renin-an-giotensin system. Recently,angiotensin receptor blockers have being realized in width with its few side fect and good safety. A number of experimental and clinical resuls in recent 10 years have indicated that ARB can prevent or even reverse the progression of chronic renal diseases in many ways effectively and provided great evidences for current therapy of CPRD.

Current researches on pharmacokinetic/pharmacodynamic (PK/PD) modelling

HUANG Xiao-Hui, LI Jun

2004, 9(11):  1205-1208. 

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Pharmacokinetic/pharmacodynamic (PK/PD) modelling plays more and more important role in the study of pharmacology. This paper recommends some new research progress including PK models, PD models, four basic attributes of PK/PD model,population PK/PD mod-el, physiological PK/PD model, and some questions about utilization of Sheiner effect compartment model.

Pharmacokinetics and pharmacodynamics research on salviol B in healthy volunteers

GAO Rui, ZHANG Yi, WANG Shuo-Chen, XU ling, ZHENG Qing-Shan

2004, 9(11):  1209-1212. 

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AIM: To study the pharmacokinetics and pharmacodynamics of salviol B in healthy volunteers and explore the relationship between the blood concentration of salviol B and the platelet aggregation and adhesiveness. METHODS: Nine male volunteers were administered 200, 300 and 400 mg salviol B (ivgtt) by cross-over design. The blood samples of different time points in these subjects were sampled and the drug concentrations of salviol B were analyzed by HPLC. The rates of platelet aggregation and adhesiveness were determined by efficacy indices. RESULTS: Salviol B was a two-compartment model with fast elimination (t_1/2, 1 h) and a large apparent volume of distribution. The C_maxwas 14 mg·L^-1. The rates of platelet aggregation and adhesiveness decreased after administration, and it was related to the change of drug concentration. The effect hysteresis rings were found from the curves of efficacy-concentration. CONCLUS-SION: Salviol B can decrease the rates of platelet ag-gregation and adhesiveness with efficacy hysteresis. It is an agent with fast elimination.

Effects of 7-nitro indazole on anesthetic depths in rabbits induced by propofol

ZHAO Da-Zhong, CHEN Jian-Yan, HUANG Shao-Nong, ZHENG Yong-Hui, ZHANG Yun

2004, 9(11):  1213-1216. 

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AIM: To investigate the regulative effects of 7-NI on anesthetic depths in rabbits induced by propo-fol. METHODS: Twenty Japanese large auris rabbits of both sexes were randomly divided into 2 groups (n=10 in each): control group was given 2 milliliter peanut oil, ip and trial group was given 50 mg·kg^-17-NI, ip. After twenty minutes of administration, propofol were target-controlled infused by Graseby 3 500 injection pump that connected with jugular vein. The loss of chewing was in-dicated the light anesthesia. The blood concentration of propofol and the bispectml index (BIS), and heart rate variability index(HRVI) were determined as the light an-esthetic depth reached. In order to observe the changes of BIS and HRVI, the control group was given 50 mg·kg^-17-NI, ip in the light anesthetic depth. RESULTS: 50 mg·kg^-17-NI significantly decreased the target blood concentrations in the light anesthetic depth. Administra-tion of 50 mg·kg^-1 7-NI increased the anesthetic depth after the light anesthetic depth reached (P>0.05). CONCLUSION: 7-NI can increase the anesthetic action of propofol by selectively inhibition of the activity of cen-tral nNOS, indicated that central NO/cGMP signal trans-duction pathway play an important role in the general an-esthesia machanism of propofol. Propofol may influence NO/cGMP signal transduction pathway by selectively inhi-bition of the activity of central nNOS.

Characteristics of antinociceptive effects of choline in central nervous system in mice

SU Dong-Mei, LIU Yue, WANG Yue, WANG Ru-Huan, WANG Hai

2004, 9(11):  1217-1220. 

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AIM: To investigate the characteristics of the antinociceptive effects of choline in central nervous system (CNS) in mice. METHODS: Hot-plate test (icv) was used to study the antinociceptive effects of cho-line, the influences of many antagonists on the antinoci-ceptive effects of choline were observed, the potential mechanisms underlying the antinociceptive effects of cho-line were discussed. RESULTS: With the administration of choline 90-120 μg per mouse, antinociceptive effects showed in a dose-dependent manner. MLA(50 μg per mouse), a-BTX(2 μg per mouse) and atropine(0.1 μg per mouse) significantly blocked the effect of choline; mecamylamine(5 μg per mouse) and naloxone(2 μg per mouse) failed to block choline-induced antinociception. CONCLUTION: Choline-induced antinociception is me-diated by α₇-nAchR subtype, while mAchR seems to be related to choline-induced antinociception.

Studies on toxicokinetics of single or combination administration of bromo-tetrandrine and adriamycin in beagle dogs

XIAO Shu-Hua, WEI Guang-Li, LU Rong, LIU Chang-Xiao, WANG Feng-Peng

2004, 9(11):  1221-1225. 

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AIM: To study the toxicokinetics after single or combination administration of bromotetrandrine (W198) and adriamycin in beagle dogs. METHODS: The concentrations of W198 and adriamycin in biological samples were determined by HPLC with ultraviolet and fluorescence detection. RESULTS: After successive in-travenous administration of 15 mg·kg^-1 W198, the values of AUC_0-24h of W198 were 6.15±0.66, 26.55±9.43 and 33.63±2.31 mg·h^-1·L^-1 for 1st, 3rd and 72nd administration, respectively, After successive in-travenous administration of 15 mg·kg^-1 adriamycin, the values of AUC_0-24h of adriamycin were 0.70±0.21 and 1. 19±0.19 mg·h^-1·L^-1 for 1st and 3rd administration, respec-tively.After successive intravenous combination administration of W198 and adriamycin, the values of AUC_0-24h of W198 were 25.52±6.04 and 42.60±4.14 mg·h^-1·L^-1, and the AUC_0-24h of adriamycin were 0.39±0.05 and 0.77±0.19 mg·h^-1·L^-1 for 3rd administration of W198 combined with 1st administration of adriamycin and 39th administration of W198 combined with 3rd administration of adriamycin, respectively. CONCLUSION: Both bro-motetrandrine and adriamycin have significantly accumula-tion effects in beagle dogs after successive intravenous ad-ministration, and bromotetradrine can reduce the systemic exposure of adriamycin after co-administration of the two drugs.

HPLC assay for tolbutamide and its metabolites in biological sample by solid phase extraction and study of its pharmacokinetics in human

WANG Rui, CHEN Kun

2004, 9(11):  1226-1230. 

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AIM: To establish a HPLC method by solid-phase extraction which was used for determining tol-butamide and its metabolites in human plasma and urine, and to study its pharmacokinetics. METHODS; The concentrations of tolbutamide and its metabolites in human plasma and urine by solid-phase extraction were deter-mined by HPLC. Watere Spherisorb 5 μm Phenyl column (4.6 mm×250 mm) was used as the analytical column and the mobile phase was consisted by methanol-0.02 mmol·L^-1 pH 3.3 Na₂Ac buffer(28:72). The flow rate was 1 ml·min^-1 and UV detection wavelength was 230 nm. The concentrations of tolbutamide and its metabolites in plasma and urine in healthy volunteers were determined by HPLC and the pharmacokinetic parameters were ana-lyzed by 3p97. RESULTS: The linear range was 2-100 μmol·L^-1 (r=0.999) for tolbutamide in human plasma by solid phase extraction. The recovery was 105.1%-103.9%. The linear range was 2-50 μmol·L^-1 (r=0.999) for carboxytolbutamide in human urine. The recovery was 98.8%-100.1%. The linear range was 1-50 μmol·L^-1 (r=0.999) for 4-hydroxytolbutamide in human urine. The recovery was 95.4%-103.5%. The linear range was 1-50 μmol·L^-1 (r=0.999) for tolbu-tamide in human urine. The recovery was 97.7%-106.6%. The within-day and between-day derivations of all samples were less than 15%. A single oral dose of 500 mg tolbutamide was administrated to the volunteers, the main pharmacokinetic parameters AUC_0-∞, t_1/2, T_max, C_max, and MR_0-24 were 2644.6±472.8 μmol·h^-1·L^-1, 1.4±0.6 h,235.8±47.3 μmol·L^-1 and 277.5±125.6, respectively. CONCLUSION: The method is simple and accurate, and it can be used determining tolbutamide and its metab-olites in biological samples. Tolbutamide is mainly excret-ed through urine in form of carboxytolbutamide and hydroxytolbutamide.

Research on primary culture model of pancreatic islets in rats

ZHANG Ya-Li, XIAO Mei-Fang, TAN Huan-Ran

2004, 9(11):  1231-1235. 

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AIM: To develop a simple, convenience, and inexpensive method on primary culture model of pan-creatic islets in rats for the study of anti-diabetic drugs. METHODS: The pancreases of SD rats were separated from the pancreatic duct with cold HankJ s solution and picked. Then the pancreases were cut into pieces and re-peatedly digested by collagenase at 37 ℃ for the short du-rations of the experiment. The isolated islets were identi-fied by dithizone staining and the viability was evaluated by trypan blue staining. Pancreatic islets were incubated in RPMI 1640 or DMEM for 14-16 h, then they were transferred to new culture plates with the same medium mentioned above. Determination of insulin content of su-pemate and cell lysate and the experiment of insulin se-cretion by stimulation of glucose and implantation of mice with STZ-induced diabetes were used for evaluated the function of islets. RESULTS: The viability of isolated pancreatic islets was more than 95% and the purity of cultured islets was about 85 %. The insulin synthesis, se-cretion and sensitivity of islets stimulate by glucose which were cultured in RPMI 1640 were higher than that in DMEM. The levels of blood glucose recovered to normal in type 1 diabetic mice after islets implantation. CON-CLUSION: The islets got in this study have higher purity and viability with the nonnal biological activity for about 7 days by this method and they can be used as a cell model for the study of diabetes in vitro.

Effects of rAAV/rSTAP on mRNA level of interstitial collagenase in rat stellate cells

LI Xin-Yan, XU Rui-An, WANG Guang-Ji, XIE Hai-Tang, ZHAO Xiao-Chen, CHEN Miao

2004, 9(11):  1236-1238. 

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AIM: To observe tlie effects of rAAV/ rSTAP on mRNA level of interstitial collagenase in rat stellate cell. METHODS: Recombinant adeno-associated virus including STAP gene was constructed and obtained. The stellate cells were isolated from SD rat5 s liver and cultured in DMEM medium. The effects of STAP on the level of interstitial collagenase were measured by RT-PCR. RESULTS: The level of interstitial collagenase in rAAV/rSTAP treated cells increased significantly com-pared with that in control group. CONCLUSION: rAAV/rSTAP can up regulate the expressions of interstitial collagenase mRNA and may be associated with anti-hepat-ic fibrosis.

Effects of noradrenaline on blood supply of femoral head in dogs

LU Xiao-Hu, LIU Xin-Qiong, XIAO De-Ming, LU Hong, XU Zhong-Shi

2004, 9(11):  1239-1242. 

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AIM: To observe the changes of the hip in means of injecting 2‰ noradrenaline (NA) into the hip joint cavity and study the pathogenesis of transient sy-novitis of hip. METHODS: Forty 2-3 months old dogs were divided into 10 groups,and 2‰ NA was injected into the hip joint. ^99mTC-MDP triphasic imaging was used to observe the local blood supply of femoral head, intra-articular pressure was determined, and patholoyical changes were observed to understand the natural course of the disease process. RESULTS: Injecting 2‰ noradrena-line resulted in transient contraction of blood vessels in femoral head and after 3 hours blood vessels begun to ex-pand, exudation of hip joint caused an increase of pressure in hip joint. This process continued for 2 weeks. There was no necrosis of synovium and femoral head. The whole process resembled transient synovitis of hip in the clinical manifestation. CONCLUSION: Injecting 2‰ noradrenaline results in extension and congestion of hlood vessels. An increase of pressure in hip joint causes tran-sient ischemia in femoral head. The whole process resem-hles transient synovitis of hip in the clinical manifesta-tion.Noradrenaline may play an important role in the pathogenesis of transient synovitis of hip.

Influence of fluvastatin on MMP-2, TGF-β₁ and left ventricular remodeling in rats with heart failure

MA Jing, WANG Hong, HA Dai-Wen, XU Jiang

2004, 9(11):  1243-1247. 

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AIM: To investigate the influence of fluv-astation on matrix metalloproteinase-2 (MMP-2) and transforming growth factor beta-1 (TGF-β₁) in the devel-opment of left ventricular remodeling and. heart failure of rats after myocardial infarction (MI) and the mechaiiisms of left ventricular remodeling and heart failure after myo-cardial infarction. METHODS: 67 male Spragiie-Dawley (SD) rats were randomly divided into three groups: the sham group, the MI group and the MI + statin group. The MI model was induced by ligating the left anterior de-scending coronary artery. After 24 hours of ligation, ani-mals in the MI + statin group were treated-with fluvastatin (4 mg·kg^-1·d^-1), and animals in the sham group and the MI group were treated with placebo. Rats were sacri-ficed 3 days, 4 weeks and 8 weeks after treatment. The content of MMP-2 protein (by Western-blot) and the ex-pression of TGF-β₁ were detemiined, and the collagen vol-ume fraction (CVF) and the ratio of type I to HI colla-gen (by immunohistochemistry) in the noninfarcted zone were assessed. Left ventricular function was measured at different times. RESULTS: Tlie levels of MMP-2 and TGF-pj in the noninfarcted zone were significantly higher in the MI group and the MI + statin group than that in the sham group (P < 0.05), but it was significantly lower in the MI + statin group than that in the MI group (P<0.05) 3 days,4 weeks and 8 weeks after treatment. Compared with the MI group,left ventricular function of rats in the MI + statin group was significantly improved. CVF and type I/IE collagen ratio in the MI + statin group were significantly lower than that in the MI group (P < 0.05) 4 weeks and 8 weeks after treatment. CONCLUSION: Fluvastatin can relieve the destmction of the col-lagen network and deposition of redundant reactive colla-gen in cardiac muscles through decreasing the MMP-2 and TGF-β₁ of cardiac muscle in the noninfarcted zone. Fluv-astatin can prevent and reverse the left ventricular remod-eling and improve the cardiac function.

Effects and mechanisms of intraarticular injection of doxycycline on experimental osteaarthritis in rabbits

SHANG Liang, CHEN Liao-Bin, ZHENG Xian-Nian, WANG Peng

2004, 9(11):  1248-1252. 

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AIM: To investigate the effects and mechanisms of intraarticular injection of doxycycline on experimental osreoarthritis in rabbits. METHODS: An animal model of osteoarthritis in knee of rabbits was es-tablished by intraarticular injection of papain. 2 mg or 4 mg of doxycycline was injected (intraarticular) once a day in four weeks. The degeneration of articular cartilage, Mankin's marks of the cartilage tissue,the expression of MMP-13, the release of nitricoxide (NO) and the activity of total nitricoxide synthase (NOS) and inducible nitri-coxide synthase (iNOS) of the joint fluid were tested sub-sequently.RESULTS: In the osteoarthritis model group, the Mankin,s marks and the expression of MMP-13 ob-servably increased, and spectrophotometric analysis showed the high concentration of the release of NO and high activity of NOS and iNOS in the joint fluid (P < 0.01). The cartilage surface was irregular with an abun-dance of fissures visibly by the naked eye, and the wear and degeneration of cartilage including osteophytes were found. Injection of 0.2 mg·d¹ doxycycline obviously de-creased the Mankind marks, the expression of MMP-13, the contents of NO and the activity of NOS and iNOS (P <0.01), and it alleviated the wear and degeneration of cartilage including the fissures and the formation of the osteophyte in the same time. Injection of 0.4 mg·d^-1 doxycycline more obviously strengthened the changes above. CONCLUSION: Intraarticular injection of doxy-cycline can delay the process of osteoarthritis, and the ef-fect is related to the dosage of the doxycycline: better ef-fect followed larger dosage. The mechanisms are related to inhibiting the level of NO, the activity of total NOS and iNOS activity and the expression of MMP-13.

Effects of 1-menthol and azone on percutaneous penetration of bifonazole in vitro

LIU Huan-Long, FENG Xiao-Long, WANG Xin-Yu

2004, 9(11):  1253-1255. 

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AIM: To investigate the effects of pene-tration enhancer 1-menthol and azone on percutaneous ab-sorption of bifonazole in vitro. METHODS: Percutane-ous penetration experiment was performed on device in vitro and deposit effect was observed by vivo perception. Orthogonal function spectrophotomery was used for obliter-ating the interferance of absorption RESULTS: Azone (1%) had a significantly effect on percutaneous absorption of bifonazole. The lag times were shortened and the deposit effect was increased by azone. CONCLUSION: Azone can enhance the percutaneous absorption of bifon-azole. Menthol can not enhance the percutaneous absorp-tion of bifonazole, but it can increase the deposit effect.

Effects of SB203580 on airway inflammation and Thl/Th2 cytokines in mice with asthmatic

HUANG Cui-Ping, Yang He-Ping, ZHANG Zhen-Xiang, GUO Yan-Kun

2004, 9(11):  1256-1259. 

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AIM: To investigate the effects of SB203580, a special inhibitor of p38 mitogen-activated protein kinase (p38 MAPK), on the airway inflammation and Thl/Th2 cytokines, IFN-y/IL-4 in mice with asth-matic. METHODS: Thirty mice were randomly divided into 3 groups: normal control group, asthmatic group and SB203580 group. The concentrations of IFN-7 and IL-4 in bronchial alveolar lavage fluid (BALF) were measured by ELISA, The number of inflammatory cells in BALF and the changes of histropathology were observed. RE-SULTS: In asthmatic group, the number of inflammatory cells and the concentration of IL-4 in BALF were higher and the concentration of in BALF IFN-ywas lower than those in normal control group(P < 0.01). In SB203580 group, the number of inflammatoiy cells and the concen-tration of IL-4 in BALF were lower and the concentration of in BALF IFN-ywas higher than those in asthmatic group (P < 0.01). Meanwhile, the histropathology damage was alleviated in SB2035 80 group. CONCLUSION: SB203580 can decrease the aggregation of airway inflam-matory cells and correct the imbalance of IFN-y/IL-4.

Pharmacokinetics and effect of dauricine on electrocardiogram in Beagle dogs

SHI Shao-Jun, GU Shi-Fen, CHEN Hui, ZENG Fan-Dian

2004, 9(11):  1260-1263. 

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AIM: Toestablishapliannacokinetio pharmacodynamic (PK-PD) model to analyze the relation between the plasma concentration of dauricine and the ef-fect on electrocardiogram (ECG) in 4 Beagle dogs. METHODS: 8 hours after intravenous administration of 6 mg·kg^-1 dauricine, blood was serially sampled and the effect on electrocardiogram was measured. The plasma concentration of dauricine was measured by HPLC-ultravi-olet method. The time courses of plasma concentration and the effects of dauricine were analyzed with 3P97 pro-gram and PK-PD parameters estimate program · RE-SULTS: The plasma concentration-time course followed a 2-compartment open model. The mean distribution half-life (t_1/2α) was 0.049±0.016 h and terminal elimination half-life (t_1/2β) was 2.7±0.6 h. The maximal decrease in heart rate (HR) was (26.4±6.1)%,whereas the maximal increase in PR, QRS, and Q-Tc intervals were (33,7±10.0)%,（35.6±12.0)% and (25.5±9.4)%, respectively. All peak effects were appeared ap-proximately 10-15 minutes after intravenous administra-tion of dauricine. Effect on electrocardiogram was ana-lyzed by the effect-link sigmoid model. CONCLUSION: The PK-PD model can successfully characterize the relation between the plasma concentrations of dau-ricine and the effect on electrocardiogram.

Effects of ligustrazini and L-arginine on hepatocellular energy metabolism in rabbits with reperfusion injury after ischemia

WANG Wan-tie, JIN Ke-Ke, WANG Wei, CHEN Xi-Wen, XU Zheng-Jie, XU Yai-Xiao, PAN Xue-Rong, XIE Ke-Jian

2004, 9(11):  1264-1267. 

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AIM: To study the effects of ligustrazini (LGT) and L-arginine (L-Arg) on hepatocellular energy metabolism in the rabbits with reperfusion injury after he-patic ischemia and its mechanisms. METHODS: 40 rab-bits were randomly divided into 4 groups (n=10 in each), hepatic ischemia-reperfusion (HIR) group, HIR + LGT group (B), HIR + L-Arg group (C) and HIR + LGT + L-Arg group (D). The contents of adenosine triphosphate (ATP), adenosine diphosphate (ADP), ad-enosine monophosphate (AMP),total adenylic acid num-ber (TAN), energy charge (EC), malondialdehyde (MDA), superoxide dismutase (SOD), nitric oxide prod-ucts (N0₂^-/N0₃^-), thromboxane B₂ (TXB₂), and 6-ke-to-prostaglandin F_1α (6-keto-PGF_1α) ratio in the liver tis-sue were measured at 45 minutes after reperfusion. RESULTS: The contents of ATP, NO, 6-keto-PGF_1α and SOD activity of the liver tissue in B, C, and D groups were higher than those in HIR group (P < 0.05 or P < 0.01), the contents of MDA, TXB₂ and TXB₂/6-keto-PGF_1α ratio of the liver tissue in B,C, and D groups were lower than those in HIR group (P<0.05 or P<0.01). CONCLUSION: The combination usage of LGT and L-Arg can improve the hepatocellular energy metabolism in the reperfusion injury after liver ischemia by decreasing oxygen free radical level, raising NO level and correcting TKA₂/PGI₂ imbalance.

Preparation of isoliquiritigenin liposome and its inhibitive effects on prolif-eration of human cervical cancer cells in vitro

ZHANG Jing, YANG Jing, WU Ji-Liang, ZHANG Lin, ZHAN Chun

2004, 9(11):  1268-1272. 

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AIM: To study the effects of isoliquiritig-enin (ISL) liposome on the proliferation of human cervical cancer cells in vitro. METHODS: ISL liposome was prepared by filmultrasonic technique. The liposome and free ISL were separated by Sephadex G-25 exclusion chro-matography and the encapsulation rates were determined. The growth inhibitive effects on cell proliferation were evaluated by trypan blue exclusion and MTT method. RESULTS: The particle size of ISL liposome was 233.1 nm and the span was 0.74. The encapsulation rate was (70.83±2.5) % and the liposome was stable. ISL lipo-some (5-80μmol·L^-1) inhibited the proliferation of hu-man cervical cancer cells in a concentration-and time-dependent manner, and the inhibitive rates of HeLa and SiHa cells reached the maximum at d 3 of culture (the maximum inhibitive rate was 83.44% and 96.14%). The IC₅₀ of HeLa and SiHa cells which were exposed to ISL liposome for 48 h was 34.24 and 29.82 μmol·L^-1, respectively, and which were exposed to free ISL for 48 h was 75,39 and 69.33 μmol·L^-1, respectively. CONCLUSION: This formulation and technology are stable and practical. The ISL liposome can significantly inhibit the proliferation of human cervical cancer cells in vitro.

Effects of rutaecarpine on ulcerative colitis in mice

LIU Bao-Lin, WU Wei-Wei, JIN Chang-Feng, WANG Yin

2004, 9(11):  1273-1277. 

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AIM: To evaluate the effects of rutae-carpine on ulcerative colitis and intestinal movement in experimental animals. METHODS: The mouse model of acute colitis was induced by colonic instillation of dinitro-chlorobenzene (DNCB)/alcohol. Rutaecarpine (10, 30, and 100 mg·kg^-1) were orally administrated to animals for 3 days. Diarrheas, colon weight index, macroscopic damage in the colon were observed and the activity of MPO and the content of PGE₂ in colon were also exam-ined.Meanwhile, the inhibitory effects of rutaecarpine on ileal contraction movement in Guinea pig which was in-duced by acetylcoline or histamine in vitro were exam-ined. RESULTS: The diarrhea and the colon weight in-dex were reduced and the macroscopic damage in the in-flammatory colon was effectively attenuated by mtae-carpine. The elevated level of MPO and PGE₂ were also significantly decreased. Ileal contraction movement in-duced by acetylcoline or histamine in vitro was strongly dose-dependent inhibited by rutaecarpine. CONCLUSION: Rutaecarpine can effectively inhibit the inflamma-tory infiltration, bleeding and proliferation in experimental ulcerative colitis and the movement of intestinal smooth muscle. Rutaecarpine may be an effective drug in treating inflammatory bowel diseases in clinic.

Protective effects of prostaglandin E₁ on ischemia/reperfusion-induced lung injury after lung transplantation in rats

ZHOU Yong-An, LIU Kun, ZHANG Tao, GU Zhong-Ping

2004, 9(11):  1278-1280. 

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AIM: To investigate the protective effects and the mechanisms of prostaglandin E₁(PGE₁) on isch-emia/reperfusion (I/R)-induced lung injury after lung transplantation in rats. METHODS: 36 SD rats were randomly divided into 3 groups (n=12 in each): sham operation group (control group), lung transplantation (LT)group and PGE₁, treatment group. PGEi was admin-istered to the rats through intra-venous way from 10 min before the operation to the end of the reperfusion. The wet/dry ratio of lung, lung permeability index and neutro-phil percentage were detected in bronchoalveolar lavage fluid (BALF). Superoxide dismutase (SOD) and malond-ialdehyde (MDA) of lung tissue were measured by color-imetry.Serum level of tumor necrosis factor a(TNFα) was detected by enzyme-linked immunosorbent assay (ELISA). RESULTS: The wet/dry ratio of lung, lung permeability index and neutrophils percentage in BALF and MDA content of lung tissue in LT group were higher than those in control group(P < 0.01). SOD activity of lung tissue in LT group was lower than that in control group(P < 0.01). Administration of PGE₁, improved the indexes above (P < 0.01). Serum level of TNFα in-creased after lung transplantation compared with the con-trol group. However, PGE₁ treatment reduced the serum levelof TNFα(P<0.01). CONCLUSION: PGE₁ can protect the lung function against I/R injury after lung transplantation. The mechanism is related to its anti-oxi-dative effect and the inhibition of TNFα release and neu-trophils activation.

Effects of fluvastatin on expression of intercellular adhesion molecule-1 after myocardial ischemia-reperfusion in rabbits with hyperlipidemia

QIN Jin-Mei, YANG Bo, LI Jian-Jun, CHEN Li, DAI Shu-Hua

2004, 9(11):  1281-1284. 

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AIM: To investigate the effects of fluvas-tatin on expression of intercellular adhesion molecule-1 af-ter myocardial ischemia-reperfusion in rabbits with hyper-lipidemia. METHODS: 30 rabbits which were gastric perfusion administered intralipid were randomly divided into 3 groups (n=10 in each); IR (ischemia-repeifu-sion) group, S (sham-operation) group and F (fluvastatin 10 mg·kg^-1) group. Electrocardiography and cardiac function were recorded during the experiment. At the end of reperfusion, ischemic area and infarct size were defined by Evans blue and triphenyltetrazolium chloride staining. The expression of ICAM-1 in myocardium was measured by RT-PCR. RESULTS: After ischemia-reperfusion, the expression of ICAM-1 mRNA in myocardial and infarct size decreased and cardiac function significantly improved in F group compared with IR group. CONCLUSION: The increase of expression of ICAM-1 mRNA in myocardi-al may be one of the important factors in inducing myocar-dial ischemia-reperfusion injury. The myocardial protec-tive mechanism of fluvastatin maybe attribute to its effect on decreasing the expression of ICAM-1 mRNA in myo-cardial.

Therapeutic effects of Taizhi'an capsules on hyperlipidemia in rats

WU Nan, ZHANG Qing-Shu, ZHANG Yue-Fei, MAO Yi-Qing, LI Qing-Yi, RUAN Yuan, LING Hu, GAO De-Lul, TAN Huan-Ran

2004, 9(11):  1285-1288. 

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AIM: To observe the effects of Taizhi5 an capsules on reducing the hyperlipidemia in rat models, and to explore the mechanisms and the side-effects of Taizhi'an. METHODS: Hyperlipidemia animal models were set up by normal diet and high cholesterol diet in rats. The concentrations of serum lipid were detected by full automatic biochemical instrument. RESULTS: Taizhi'an obviously reduced the concentration of serum total cholesterol, triglycerides (TG) and increased the contents of LPL. Taizhi'an had no obviously influence on the concentration of glutamic oxaloacetic transaminase (GOT). CONCLUSION: Taizhi'an capsule can de-crease the hyperlipidemia. Its mechanism is related to the regulation of lipid metabolism and improvement of the concentration of LPL (lipoprotein lipase).

Effects of Fr. A in Guizhi Tang on the excretion of PGE₂ and its signal transduction components in cerebral microvascular endothelial cells stimulated by IL-1

JIANG Nan, HUO Hai-Ru, Li Lan-Fang, GUO Shu-Ying, JIANG Ting-Liang

2004, 9(11):  1289-1292. 

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AIM: To investigate the effects of Fr. A, an antipyretic active fraction extracted from Guizhi Tang, on the excretion of PGE₂ and its signal transduction com-ponents in cerebral microvascular endothelial cells (rCMEC) stimulated by IL-1. METHODS: Fr. A-containing rat serums were prepared. The PGE₂, PLA₂, COX and NO were measured by radioimmunoassay, enzyme reaction substrate assay, ELISA and colorimetry, respectively. RESULTS: When administration of Fr. A-containing serum, contents of PGEj and NO, the activity total COX and of COX-2 were significantly decreased in rCMEC. But the activity of sPLA₂ was not significantly decreased. CONCLUSION: Fr. A can affect the level of PGE₂ by iniluencing the main elements of COX and NO in PGE₂ signal transduction passway.

Effects of low-dose theophylline on differentiation of naive T lymphocyte

NIE Han-Xiang, GUO Wei, YANG Jiong

2004, 9(11):  1293-1296. 

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AIM: To investigate the effects of low-dose theophylline on differentiation of the naive T lympho-cyte.METHODS: Naive T lymphocytes and monocytes were isolated from cord blood in neonate. Theophylline (10 mg·L^-1) was added in naive T lymphocytes and monocytes which stimulated by PHA (200 mg·L^-1) for 3 days, and the differentiation of T cells was analyzed by flow cytometry. Cytokines were measured by enzyme linked immuno-sorbent assay (ELISA). RESULTS: Theophylline significantly promoted differentiation from Thl cells to naive T cells (P < 0.05), but it had no sig-nificant effect on differentiation to Th2. The ratio of Thl/Th2 was increased (P < 0.05). The production of IL-4 and IL-5 were lower and IFN-y was higher than that in the control group (P < 0.05). CONCLUSION: Low-dose theophylline can modulate the differentiation of naive T cells and exert its anti-inflammatory effect.

Comparison of central nervous system effect of diazepam on Chinese Han subjects and Chinese Tong subjects

WAN Jie, ZHOU Hong-Hao, HE Bin

2004, 9(11):  1297-1300. 

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AIM: To compare the central nervous system effect of diazepam on Chinese Han subjects and Chinese Tong subjects. METHODS: Ten subjects of healthy male Tong and ten subjects of healthy male Han were given single oral doses of placebo,7.5 mg diazepam or 15 mg diazepam in a double-blind randomized crossover study. The plasma levels of diazepam, the Digit Symbol Substitution Test (DSST) and the electroencephalographic (EEG) were determined at 0.5, 1, 1.5, 2, 3, and 5 h after administration. RESULTS: The plasma concentra-tions of diazepam in Han subjects were significantly higher than that in Tong subjects at 1-1.5 hours after adminis-tration of 7.5 mg diazepani and at 0.5-1.5 h after ad-ministration of 15 mg diazepam, but they were significant-ly lower at 3-5 houi-s after administration of 15 mg diaze-pam.However, there was no statistical difference between the two ethnic groups in the area under the 5-hour con-centration-time curve after administration of both doses. The decrement of DSST were significantly lower in Han subjects than that in Tong subjects at 1-1.5 h and 3-5 h after administration of 15 mg diazepam, but there was no statistical difference when the decrement of DSST were corrected by the plasma concentrations of diazepam. The individual concentration-response curves were used to cal-culate the concentration of diazepam required to produce a 50 % increase in the percentage of EEG amplitude falling in the range of 12.8 to 31.2 Hz, and there was no signif-icant difference between the Han subjects (543.8±371.7 μg·L^-1) and Tong subjects (547.0±590.7 μg·L^-1) (P>0.05). CONCLUSION: The central nervous system effect of diazepam in Han subjects is simi-lar with that in Tong subjects.

Efficacy of domestic rhG-CSF on leucopenia induced by chemotherapy in patients with gynecological tumors

LI Cong-Zhu, ZHAI Yu-Xia

2004, 9(11):  1301-1304. 

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AIM: To study the effects of different dose of domestic recombinated human granulocyte colony stimulating factor (rhG-CSF) on leucopenia induced by chemotherapy in patients with gynecological tumors. METHODS: 98 patients with gynecological tumors (ovarian cancer 36, endometrial carcinoma 28,cervical cancer 34) were randomly divided into 3 groups. RhG-CSF (domestic) was given at the dose of 75 μg·d^-1, S. C in group A, rhG-CSF (domestic) was given at the dose of 150 μg·d^-1, S. C in group B, and rhG-CSF (import) was given at the dose of 75 μg·d^-1, S. C in group C. RESULTS: The amount of WBC and ANC were in-creased by different dose of domestic rhG-CSF and the im-port rhG-CSF. In first cliemoiherapy, the time when the level of WBC raised higher than 4.0×10⁹ L^-1 were no significant difference among 3 groups (P>0.05). But in repeated chemotherapy, the period of leukopenia recov-ered to normal was shorter in group B than that in group A or group C. The effects of the domestic rhG-CSF on leu-copenia induced by chemotherapy were similar to the im-ported products of same dose. CONCLUSION: Low dose of domestic rhG-CSF (75 μg) can effectively treat the leukopenia caused by postchemotlierapy in patients with gynecological tumors. 150 μg of domestic rhG-CSF is more effective than 75 μg of domestic or import rhG-CSF in treating leukopenia in repeated chemotherapy.

Research on bioequivalence of flunarizine hydrochloride dispersible tablets in healthy volunteers

ZHAO Yan, LIU Zhen-Sheng, LI Zhi-Ping, ZHAO Mei-Ling, QI Fang-Mei, WANG Shao-Hua

2004, 9(11):  1305-1308. 

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AIM: To study the bioequivalence be-tween flunarizine hydrochloride dispersible tablets and capsules in healthy volunteers. METHODS: A single dose of 20 mg flunarizine hydrochloride dispersible tablets and capsules were given to 20 healthy volunteers by a ran-domized,two way cross-over design. Plasma concentra-tions of flunarizine hydrochloride were determined by HPLC. RESULTS: The pharmacokinetic parameters after administration of flunarizine hydrochloride dispersible tablets and contrast flunarizine hydrochloride capsules (20 mg) were as follows: AUC_0-1, 424.27±74.01 and 410.25±72.56 μg·L^-1,C_67.02±14.89 and 67.45±15.68 μg·L^-1,T_max 2.90±0.42 and 2.98±0.47 h, and t_1/2ke9.73±3.15 and 8.89±3.08 h,respectively. The relative bioavailability of the flunaiizine hydrochloride tablets was (104.12±12.23)%. CONCLUSION: Two formations of flunarizine hydrochloride are bioequivalent.

Pharmacokinetics of telmisartan tablets in healthy volunteers by HPLC

JIALin-Jing, WEN Qiang, QIAO Hai-Ling, ZHANG Qi-Tang, ZHANG Li-Rong, GUO Yu-Zhong, GAO Na, TIAN Xin

2004, 9(11):  1309-1312. 

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AIM: To establish an HPLC-fluorimetric method in determination of the concentrations of telmisar-tan in plasma of healthy volunteers and to investigate its pharmacokinetics. METHODS: The chromatographic column was Hypersil C18 column (250 mm×4.6 mm,5 μm). The mobile phase was acetonitrile-pH 5.8 phos-phate buffer (45:55) and the flow rate was 1.0 ml·min^-1. The fluorimetric excitation and emission wave-lengths were set at 305 nm and 365 nm, respectively. The internal standard was a~naphthol. Blood samples were deproteined by adding acetonitrile. The injection volume was 20 μl. RESULTS: The linearity correlation of telm-isartan ranged from 2 to 1 024 μg·L^-1 (r=0.9999) and the precision and stability of the method were fine. The pharmacokinetics of telmisartan was studied in healthy volunteers after oral administration of 80 mg telmisaitan tablets. It showed that the c-t curves of telmisartan con-formed to the two-compartment open model. The main pharmacokinetic parameters of telmisartan were as follows: C_max 0.98±0.44 mg·L^-1; mg·L^-10.83±0.45 h, t_1/2α 1.67±1.26 h, t_1/2β26.00±14.43 h,t_1/2ka0.53±0.86 h,AUC_0-l 3.66±2.10 mg·h ^-1·L ^-1,and AUC_0-∞ 3.98±2.40 mg·h ^-1·L ^-1. CONCLUSION: This is a convenient, sensitive, accurate and reproducible method for determining the concentrations of telmisartan in plasma of healthy volunteers and investigating its pliarma-cokinetics.

Ethic Review in Clinical Research: Subjects Recruitment

WANG Xiu-Qin, XIONG Ning-Ning, LIU Shen-Lin, LI Qi-Yi, JIANG Meng, LIU Fang, ZOU Jian-Dong, XUE Jun, BO Qing-Yan, GAO Wei-Min

2004, 9(11):  1313-1316. 

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Recruitment of eligible subjects is of para-mount importance and probably the most difficult and changeling aspect of a clinical trial. Ethic review of sub-jectsJ recruitment mainly includes the mode of recmit-ment,the selection of subject population, recompense and incentives to subjects. For reviewing of mode of re-cruitment,respect for privacy and voluntary participation, avoiding any possibility of coercion or undue influence must be taken into account; while for reviewing of selec-tion of subject population, apportion of research burdens and benefits must be equally considered among population and the representative of study cohort? The reasonable recompense and free from undue inducement must be con-sidered when reviewing recompense and incentives to sub-jects.