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

Table of Content

    Volume 6 Issue 3
    26 June 2001
    Study in vitro of antimicrobial activity of domestic sparfloxacin
    WANG Rui, FANG Yi, LIU Gui-Yang, CHEN Qian, FANG Xiang-Qun, LIU Qing-Feng
    2001, 6(3):  196-199. 
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    Aim To study in vitro the antibacterial activity of domestic sparfloxacin (SPLX) and compare it with other four quinolones including lomefloxacin (LMLX), ciprof lox acin (CPLX), ofloxacin(OFLX) and enox acin(ENX).Methods Minimal inhibitory concentrations(MIC) were determined by means of agar disk dilution method.The susceptibility was defined acco rding to NCCLs.Results SPLX was the most active one in the quinolones against all tested st rains. Its MIC90 was less or equal to 2 mg·L-1, while the MIC90 of LMLX、CPLX、OFLX and ENX were 16、 16、16 and 32 mg·L-1, respecti rely.The geomet ric means of MIC (MICg) of SPLX (0.179 mg·L-1) were significant lower than MICg of LMLX、OFLX and ENX and slightly lower than that of CPLX.The susceptible rate of G+ cocci was 100%, significantly higher than that of controlled quinolones.Conclusion The antibacterial spectrum of SPLX is wider and the activity against clinical isolates is higher than that of other quinolones.
    Apoptosis of hepotoma cell line BEL-7404 induced by extracts of solanum lyratum thumb
    SHAN Chang-Min, HU Juan-Juan, DU Guan-Hua
    2001, 6(3):  200-203. 
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    Aim To study the biological effect of extracts of solanum lyratumthumbon inducing apoptosis of BEL-7404 cell line.Methods The BEL-7404 cells were cultured in DMED medium and treated with extract of solanum lyratum thumb and then were observed with microscope and their DNA was assayed by the method of gel.Results Treatment by ex tract of solanum lyratum thumb could induce the cells to reveal atypical apoptotic appearance.Their DNA was fracted and a ladder pattern characteristic could be found by the elect ropho resis.The extract of solanum lyratum thumb show the same effects as paclitaxol. Conclusion solanum lyratum thumb can induce apoptosis in BEL-7404 cells.
    Dynamic observation of the effects of polyporus polysaccharide on intracellular calcium in cultured human T24 cells with laser scanning confocal microscopy
    ZHANG Guo-Lai, ZENG Xing, MEI yu-Ping, HE Shen-Qi, ZANG Xin-Mei, HUANG Yu
    2001, 6(3):  204-206. 
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    Aim To investigate the relationship between polypo rus polysaccharide (PUPS) and changes of int racellular calcium in human T24 bladder cancer cells. Methods Human T24 cells were cultured with PUPS and intracellular calcium level was measured with the fluorescent Ca2+ indicato r calcium crimson- AM and the laser scanning confocal microscopy.Results After human T24 cells were treated with a low dose of PUPS (0.2 mg·L-1), the int racellular calcium was decreased; while with PUPS (> 1.0 mg·L-1), the int racellular calcium became increased, and kept on ahigher level.Conclusion PUPS participates in the process of calcium message transduct ion.
    Biphase actions of galanin antagonists at different doses on galanin-evoked outward-current of trigeminal nucleus neurons in rats
    SHI Ming-Yi
    2001, 6(3):  207-210. 
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    Aim To observe the effects of galanin (Gal) antagonist M35 or M40 at different concentrations on the Gal-evoked outward-current in principal trigeminal nucleus (PrV) neurons.Methods The technique of whole-cell patch-clamp was used to record the change of membrane current.Results At doses of M35 0.01, 0.03 and 0.1 μmol·L-1, the Gal-evoked outward- current decreased by 53.1%, 40.4% and 27.2%, respectively.While M35 1 and 3 μmol·L-1, the current increased by 16.2% and 38.4%.At doses of M40 0.01 and 0.03 μmol·L-1, the current increased by 93.7% and 68.4%, while for M40 0.3, 1 and 3μmol·L-1, the current decreased by 49.2%, 69.9% and 87.2%, respectively.Conclusion M35 at low concentrations antagonizes the effect of Gal and at high concent rations acts as a Gal receptor agonist. Whereas M40 in high doses antagonizes the effect of Gal and in low doses exerts an autagonistic action. There may be different Gal subtype receptors in the same PrV neuron.
    Nitric oxide inhalation and propofol injection in treatment of rabbits with oleic acid-induced acute lung injury
    LI Juan, CHEN Kun-Zhou, SUN Rui-Yuan
    2001, 6(3):  211-214. 
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    Aim To observe effects of inhalation of nitricoxide and intravenous propfol on pulmonary oxygenation and perfusion in rabbits with acute lung injury (ALI) induced by oleicacid.Methods Nineteen healthy adult rabbits were anesthetized with tracheotomy, and then vent ilated mechanically.Four animals were selected as normal control.The others were induced into ALI (0 h) by pulmonary injection of oleic acid (60 mg·kg-1) and then randomly allocated into three groups:(1) control group (n=5, receiving ventilation only);(2) NO group (n=5, inhaling NO at 20 ppm);and (3) propofol group(n=5, receiving intravenous propofol 2 mg·kg-1·h -1).The mean systemic arterial pressure (SAP), heart rate (HR), PaO2, PaCO2 and Qs/Qt were recorded in the time of baseline, 0 h and 2 h.X-rays of chests were given and wet-to-dry lung weig htratio (W/D) was determined after the treatment.Results 2 h after the administ ration, the mean PaO2 (>95 mmHg, P<0.05) and PaO2/FiO2 (>300, P<0.05) were significantly improved and Qs/Qt (16%, P<0.05), W/D reduced significantly in the NO group, but not in the propofol group.Conclusion NO inhalation, used for ALI in early stage, can safely and effect ively improve pulmonary circulation, gas exchange, pulmonary oxy genat ion and perfusion, decrease pulmonary edema, and slow down the progress of lung injury.Propofol does not show any influence on oxygenation and pulmonary arterial pressure.
    Inhibitory effect of domestic leuprorelin acetate microspheres on experimentally induced endometriosis in rats
    XU Xin-Hong, GUO Ling-Hong, GONG Qin-Yan, CHEN Lin-Ai, YAO Ming-Hui
    2001, 6(3):  215-217. 
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    Aim To study the effect of leuprorelin acetate microspheres (LE-ms)on endometriosis in rats, and compare the efficacy of material drug (LE), domestic and imported LE-ms (enanton).Methods Endomet riosis was induced by endomet rial implant in rats.Then the animals were treated with LE (20 μg· kg-1·d-1×28 d, sc), enanton(20 μg·kg-1·d-1, sc) and domestic LE-ms (2, 20, 200 μg·kg-1·d-1, sc). Results Implants in control group continued to grow, while those in groups treated with drugs shrinked signif icantly, and domestic LE-ms could produce dose-dependent inhibitory effect on the growth of endometrial implant in rats.Conclusion The domestic LE-ms at the single dose of 20 μg·kg-1·d-1 has the same effectiveness as enanton and routine injection with the same does of LE for 28 days.
    Pharmacokinetic study of bicyclol in thirty health volunteers
    JI Yan-Yan, CHENG Neng-Neng, YAO Guang-Bi
    2001, 6(3):  218-221. 
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    Aim To observe the pharmacokinetic profiles of oral administration of bicyclol in 30 healthy volunteers. Methods Thirty healthy volunteers were randomized into 25 mg, 50 mg and 100 mg groups.They were given bicyclol in a single dosage or multiple dosages before and after meal respectively.The plasma concentration of bicyclol was assayed by the high performance liquid chromatograply (HPLC).The pharmacokinetic parameters were analysed by 3p97 softwere. Results The feature of pharmacokinetics conformed to one compartment model and a first order elimination. For the three dose groups of 25, 50 and 100 mg, the values of t(1/2)ka were (0.84±0.68)、 (0.33±0.09)and (1.19±10.9)h, respectively; the values of t(1/2)ke were (6.26±6.24), (6.17±2.01) and (4.66±1.21)h, respectively;Vd/F (455.02±135.35), (622.94±325.37) and (688.83±308.14)L;CL/F (93.45±67.66)、 (83.31±71.97)、(104.30±45.76)h.Between single dose and mult iple dosages, the pharmacokinetic parameters had no significant difference, showing there was no accumulation in the body.Before and after meal, the values of cmax were (151.26±39.00) and (222.64±43.22)μg·L-1, respectively (P<0.01), but the AUC0~∞ had no significant difference,which was probabily related to the lipo troph of bicyclol.Conclusion Bicyclol has alinear pharmacokinetic feature.The absorption of bicyclol is influenced by food.
    Increased effects of verapamil combined with NaHCO3 by aterial infusion in patients with solid maligant tumors
    FAN Ping-Sheng, HU Bing, SUN Xin, ZHUANG Jian-Sheng, LIN Xin-Min, JI Chu-Shu, LIU Ru-Hua, HU Li-Yuan, WANG Xiao-Yan, LI Ji-De, BAI Hu, ZHU De-Fa, FENG KeHai, WANG Shi-Cun, CHEN Fei-Hu
    2001, 6(3):  222-224. 
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    Aim To observe the increased effects of verapamil combined with NaHCO3 by tumors arterial infusion in patients with solid malig nant.Methods Ninety-two patients were randomly assig ned to four groups. Group A was infused with anti-cancer agent s;group B with NaHCO3 and anti-cancer agents;group C with NaHCO3, IL-2, IFN-αand anti-cancer agents, and group D was given NaHCO3, verapamil, I L-2, IFN-αand anti-cancer agents.The efficacy was evaluated after the aterial interventional chemotherapy (1 time/mon× 2) in group A, B, C and D.Applying Seldinger penetrating technique, the drugs were infused at some proper concentrations as follow s:5% SB 80 -100 ml, NS 30 ml, IL-2 400~600(×103) U, IFN-α1~3 (×103) U, verapamil 10 -15 mg, ADM 50-60 mg, DDP 100 mg or MMC 10 mg or DPT 50 mg, 5-Fu 1.0 -1.5, verapamil 5 -10 mg with in 15 min.Results Partial remission (PR) in group B was significantlyhig herthan that in group A;PR in group D was higher than those in group A, B and C.Conclusion Arterial infusion of NaHCO3 combined with verapamil into malignanttumors can increase the efficacy of anti-cancer agents and IL-2, IFN-α.
    Analyzing subfraction particle size of low density lipoprotein and its susceptibility to in vitro oxidation in patients with chronic renal failure
    HU Bing, WANG Jun-Jun, CHEN Ning-Nan, ZHUANG Yi-Yi
    2001, 6(3):  248-251. 
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    Aim To study the size and susceptibility of low density lipoprotein (LDL) particles in patients with chronic renal failure (CRF).Methods Plasma LDL in 30 CRF patients and 26 control subjects were analyzed by 2%~16% non-denaturing poly acrylamide gradient gels.The continuous monitoring of LDL oxidation by absorbance measurement at 234 nm was performed to analyze the susceptibility of LDL to Cu2+ mediated oxidation in CRF patients.Results In LDL particle diameters no dif ference was found between the CRF patients and control subjects[(26.35±0.59) nm vs (26.41±0.95) nm, P>0.05]. The dist ribution of LDL subfraction pat tern also had no difference between two groups.LDL particle diameter was neg atively correlated with plasma t riglycerides (r=-0.26, P<0.05).However, the lagtime in the test for LDL oxidizabilty in CRF patients was signif icantly sho rter than that in the controls [(56.2±23.7) minvs (97.3±41.2) min, P<0.05].Conclusion Circulating LDL in CRF patients was more susceptible to oxidation in vitro than that of controls.This may be associated with increased risk for coronary artery disease.
    Clinical analysis of intravenous infusion of fibrinolytic agent in the treatment of acute cerebral infarction
    BAO Zheng-She
    2001, 6(3):  252-255. 
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    Aim To evaluate the clinical efficacy and safety of thrombolytic therapy for acute cerebral infarction. Methods Twenty-eig ht patients with acute cerebral infarction in the thrombotytic group were given an intravenous infusion of urokinase at the dose of 2 000 000 U and 30 patients received conventional therapy in the control group.Results Of the 28 cases, 4 recovered and 8 were markedly effective within 24 hours, while none of the 30 patients was effective. After 14 days, 12 patients in the thromboly tic group and one in the convent ional therapy group cured.The effective rate in the thromblytic group was higher than that in the conventional therapy group.Statist ical dif ference was found between the two groups. Conclusion Early int ravenous thromboly tic therapy with urokinase shows remarkable efficacy for acute cerebral infarction.