Table of Content

Volume 6 Issue 2
26 April 2001

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Effect of N-acetylcysteine on NF-κB in lung tissue and BALF of rats undergoing acute and chronic smoking

MO Hong-Ying, ZHONG Nan-Shan, ZHENG Jing-Ping, LONG Qi-Cai

2001, 6(2):  103-106. 

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Aim To assess the effect and mechanism of Nacetylcy steine (NAC, antioxidant) on nuclear factor- κB (NF-κB) in lung tissue and bronhial alveolar lavage fluid (BALF) of rats undergoing acute and chronic smoking. Methods All Wistar rats were divided randomly into three groups: control group, smoking group and intervention group. The latter two groups were applied to observing NF-κB expression during different periods (1, 2, 7, 14, 60d). Western-Blot assay was used to analyze the activation of NF-κB. Results The first and second day the expression of NF-κB in lung tissue (36.9 ±8.1 and 36.9 ±8.0) and in BA LF(24.0 ±6.1 and 21.2 ± 5.8) rose significantly comparing with that in the control groups (7.3 ±2.8 and 5.7 ±2.6) respectively (P <0.01), but fell to the normal range of control at the seventh, fourteenth and sixtith days of smoking. NAC significantly inhibited the higher NF-κB expression comparing with that in the related control smoking groups, but not inhibited the normal NF-κB expression in the rest groups. Conclusion NAC, through inhibiting activation of NF-κB during the early smoking stage and further blocking the activation of pro-inflammatory cytokines, may play a role in pathogenesis of airway inflammation of COPD.

Inhibitory mechanisms of diazepam on macroscopic sodium currents in rat sympathetic ganglion neurons

ZHENG Ji-Jian, ZHUANG Xin-Liang, DU Dong-Ping, MAO Qing-Hong, XU Guo-Hui

2001, 6(2):  107-110. 

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Aim The effects of diazepam on the whole-cell sodium currents in rat sympathetic ganglion neurons were studied to investigate the mechanisms by diazepam mediates hypotension. Methods Whole-cell patchclamp recordings were performed on enzymatically isolated rat superior cervical sympathetic gang lion neurons. Results Diazepam dose-dependently blocked the whole-cell sodium currents. Under a V_t of 0 mV and a V_h of 80 mV 0.3 μmol·L^-1 diazepam reduced sodium peak currents by 14.76 %(P <0.01), with a mean IC₅₀ values of 6.06 μmol·L^-1 (r =0.99, P <0.01); The blockade was also potential- dependent (P <0.05), under a holding potent ial of 60 mV, the mean IC₅₀ value was 4.60μmol·L^-1, 3.0 μmol·L^-1 diazepam reduced the peak values of IV curve by 48.94 % and caused 10 mV shift of I-V curve to depolarized potentials, a 0.89 mV shift of voltage-dependent activation curve to depolarized potentials (P <0.05) and a 20.12 mV shift of the steady-state inactivation curve to more hyperpolarized potentials (P <0.01). Following diazepam administration, the conditioning pulse potential at which half-maximal channels were inactivated (V_1/2), was changed from -64.13 mV to -84.25 mV and the test potential at which half-maximal channels were activated (V_1/2), was changed from -24.64 mV to -23.75 mV. Conclusion Clinically relevant concentration of diazepam has a significant inhibition on sympathetic ganglion neurons. This inhibition is dose-dependent and potential-dependent and relevant to the inactivation of sodium channel. The circulation depression of diazepam may be relevant to the direct suppression of sympathetic ganglion neurons.

Effects of total extract of astragalus (TEA) on the proliferation and the production of collagen of hepatic stellate cells

SONG Shao-Gang, YANG Yan, CHEN Min-Zhu

2001, 6(2):  111-113. 

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Aim To study the effect s of total extract of astragalus(TEA) on activating the primary cultured hepatic stellate cells (HSC) and synthesizing collagen. Methods Livers of adult rats were perfused by pronase E and collagenase in situ, HSC and Kupf fer cell (KC) were isolated by centrifugation with 18 % Nycodenz. The subcultured HSC w ere induced by Kupffer cell conditioned-medium(KCCM) and were incubated with 5 ~ 80 mg·L^{-1 TEA for 6 days. The proliferation of the cells was measured by 3H-TdR and the production of collagen by 3H-Proline. Results TEA (10 ~ 40 mg·L-1) could suppress the proliferation of hepatic stellate cells and TEA (40 ~ 80 mg·L-1) could suppress the production of collagen. Conlusion The suppression of hepatic stellate cell proliferation and the collagen’ s production by the TEA may be one of the mechanisms for depressing the hepatic fibrosis by the TEA.}

Observing study on virazole and interferon resisting respiratory synthesis virus in vitro

SHENG Xiao-Rong, FEI Zhi-Jie, WU Yi-Lun

2001, 6(2):  114-116. 

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Aim To observe the effect of recombinant human interferon and verazole used alone or in combination in resisting respiratory synthesis virus (RSV) in vitro. Methods RSV strains were proliferated with Hela cells in Eagles solution on a 96-hole plate. The recombinant human interferon and virazole were diluted to different concentrations and were separately added in the dose of 100 μl to each hole of the plate. After 48 hours cultured, the concentrations of the drugs for inhibiting cytopathogenic effect (CPE) of RSV were determined. Results When the concentration of interferon was ≥5 U·ml^-1 and virazlole ≥ 24 μg·ml^-1, respectively, the effect of the two drugs on inhibiting the CPE of RSV was remarkable and was improved with their concentration increasing. When the concentrations of the two drugs were lower than that of their effect respectively, their united use also had obvious effect in resisting the virus. In addition, the different using methods of interferon have also different results. Conclusion Both recombinant human interferon and virazole are effective in inhibiting RSV in vitro and will bring about better effect when used in combination.

Effects of phenytoin on plasma cytokines and endothelin during brain ischemic reperfusion in rats

DAI Wei-Juan, GUO Zi-Lin, LIU Hong, SONG Ai-Qin, WANG Chuan-Gong, LIU Shan-Ting

2001, 6(2):  117-118. 

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Aim In this study, cytokines and end othelins were investigated to determine the changes of TNFα, IL- Ⅰβ and ET1 after brain ischemic reperfusion and the effects of phenytoin sodium on TNFα, IL-Ⅰβ and ET₁. Methods The animal models of the focal middle cerebral arteral is chemic reperfusion were established in Wistarrats. Phenytoin sodium was administered by intravenous injection. The plasma levels of TNFα, IL-Ⅰβ and ET₁ were measured by radioimmunoassay. Rusults The levels of TNFα, IL-Ⅰβ and ET₁ in plasma were elevated after 1 h brain ischemia and 1 h reperfusion in rats. Phenytoin sodium could significantly reduce the content of TNFα, IL-Ⅰβ and ET1 in plasma. Conclusion The results indicate that TNFα, IL-Ⅰβ and ET1 participate in cerebral ischemia reperfusion lesion, which can be reduced by phenytoin sodium. Phenytoin sodioum may protect nerve cells from injury through inhibiting TNFα, IL-Ⅰβ and ET₁ production.

Pharmacokinetics and relative bioavailablity of domestic penicillin V dispersion tablet

Q IU Fu-Rong, MAO Guo-Guang, SUN Hua, DAI Ming, ZENG Zhao-Hong, CHENG Bo, ZHONG Qiu, MA Yue-Ming

2001, 6(2):  120-122. 

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Aim To study pharmacokinetics and bioavailablity of domestic penicillin V dispersion tablet in healthy volunteers. Methods According to the crossover design, each volunteer in two groups was orally given a single dose (0.75 g) of domestic penicillin V dispersion tablet or imported penicillinV tablet alternately and the plasma concentrations were determined by RP-HPLC. The pharmacokinetic parameters were obtained by using ATPK program and calculated on the basis of open single compartment model. Results After a single oral dose (0.75 g), the t_1/2(ke) was (0.75 ±0.10) h and (0.70 ±0.14) h, the c_max was (8.44 ±2.40) mg·L^-1 and (8.75 ±3.04) mg·L^-1 at (0.56 ± 0.11) h and (0.63 ±0.17) h and AUC_0~4 was (8.44 ±2.40) mg·h·L^-1 and (8.75 ±3.04) mg·h·L^-1 for two formulations, respectively. Relative bioavailability of domestic penicillin V dispersion tablet was (90.50 ±8.84) %.Conclusion The result shows that the two formulations are bioequivalent.

Pharmacokinetics and bioavialability of nimesulide dispersible tablet

FU Ying-Jun, DAI Qun, JIANG Min, XIONG Yu-Qing

2001, 6(2):  123-125. 

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Aim To study the pharmacokinetics and bioequivalence of nimesulide dispersible tablet and its normal tablet. Methods 20 healthy volunteers were treated with a single oral dose of domesticc nimesulide dispersible tablet or normal tablet (control) in a randomized crossover study and the plasma drug concentration was determined by HPLC. Results The plasma concentration-time curve was fitted to the one-compartment model. The pharmacokinetic parameters obtained were: c_max (3.91 ±0.74) μg ·ml^-1, t_(1/2) β (3.40 ±0.78) h, t_max (3.15 ±0.67) h, AUC_0~24 (31.92 ±6.36) μg·ml·h^-1, there was no significant difference between the active and control groups. The relative bioavailability obtained was (96.43 ±8.41) %.Conclusion The pharmacokinetic profile for the 2 tablets was similar so it may be concluded that they are bioequivalent.

Study on the pharmacokinetics of acetaminophen in six healthy volunteers

XU Bin, HE Ping, TAO Yong, XU Ping-Bo, ZHANG Guo-You

2001, 6(2):  126-128. 

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Aim To study the pharmacokinetics of acetaminophen (Ace) in healthy volunteers and total recovery of its metabolites in urine. Methods 1.0 g Ace was administrated o rally in 6 fasted healthy males; saliva and 24 h urine were collected regularly for the determination of Ace, glucuronide-Ace (GA) and sulfate-Ace (SA) levels by using HPLC. Results Ace in saliva showed that t_1/2 was (2.50 ± 0.29) h, CL was (10.3 ±1.6) L·h^-1, k was (0.28 ±0.03), AUC was (98.9 ±16.7) μg·h·ml^-1, V_d was (44.4 ±16.5) L; GA and SA in 24 h urine and in total recovery were (3.4 ±0.7) %, (37.5 ± 10.2) %, (24.5 ±15.5) % and (70.4 ±7.7) % respectively. Conclusions Compared with those reported by researchers in western countries, t_1/2 of Ace prolonged 25 % and total elimination was only 50 % of theirs. It seemed that low hepatic glucuronide metabolism might be an important facto r for prolongation of t_1/2 of Ace.

Study on relative bioavailability of aniracetam capsules

WANG Chuan-Ping, REN Jin-Min, JIA Xiao-Dong, JIN Yi-Ran, ZHAO Shu-Fan, JIANG Jun-Kang

2001, 6(2):  129-131. 

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Aim The relative bioavailabilities of aniracetam capsules were studied. Methods The blood concentrations of the main metabolite of aniracetam, Nanisoyl- GABA (ABA), were determined by RPHPLC after a single oral dose of 400 mg aniracetam of test(capsules) or reference(capsules) drugs was given separately to 12 volunteers in an open randomized cross-over test. Statistical software’s 3p87 w ere used for the calculation of results. Results After taking a single oral dose of 400 mg aniracetam test capsules and reference capsules, thd AUC_0~t of aniracetam of the two formulations were (781.0 ±169.5) μg·min· ml^-1 and (792.3 ±156.6) μg·min·ml^-1; t_max were (40.9 ±9.7) min and (37.3 ±11.5) min; c_max of ABA were (10.4 ±3.0) μg ·ml -1 and (10.5 ± 3.0) μg ·ml^-1. The result s of statistical analysis showed that there were no significant difference in the AUC_0~t, t_max and c_max of ABA between the formulations (P <0.05). The relative bioavailability of aniracetam capsule was (99.4 ±14.4) %. Conclusion The two aniracetam capsules were bioequivalent.

Characteristics of myocardial blood flow distribution in patients with angina pectoris and normal coronary arteriograms

CHEN Shao-Liang, DUAN Bao-Xiang, WU Xiang, ZHANG Xiao-Ling, YE Fei, HU Zuo-Ying

2001, 6(2):  132-137. 

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Aim To evaluate microvascular function and its relation to the genesis of chest pain and S T segment depression during exercise in patients with syndrome X. Methods Changes pacing-induced in transmural myocardial blood f low distribution were quantitatively assessed by 2-dimensional myocardial contrast echocardiog raphy. Myocardial blood flow distribution before and after pacing stress was assessed by measuring the ratio of the endocardial to epicardial gray level (ie, endo/epigray level ratio) in the territory of the left anteior descending coronary. Results Of 25 patients w ith a history of chest pain and normal coronary arteries with the negative ergonovine test, 11 had exercise-induced chest pain and ST segment depression(syndrome X), and 14 did not (controls). Pacing-induced chest pain and ST segment depression were observed in syndrome X, but not in controls. The endo/epigray level ratio in syndrome X significantly decreased after pacing (form 0.98 ±0.10 to 0.76 ±0.17, P <0.01), but not in controls (from 0.97 ±0.08 to 0.99 ±0.08, P >0.05). Conclusion Abnormal myocardial blood flow distribution may play an important role in exercise induced chest pain and ST segment depression in these patients.

Clinical study on antihypertensive effect trough to peak ratio of nifedipine GITS

LI Yu-Jie, MAI Wei-Yi, ZENG Qun-Ying, LIAO Xiao-Xing, WANG Li-Chun, Chen Guo-Wei

2001, 6(2):  138-141. 

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Aim To explore the best way of calculating antihypertensive effect of nifedipine GITS on trough to peak ratio (T/PR), and smoothness index (SI) of the drug from ambulatory blood pressure monitoring (ABPM). Methods 32 cases of mild to moderate essential hypertension patients were enrolled and each was given 30 mg of nifedipine GITS once daily. ABPM was repeated for four weeks. ABPM data were analyzed statistically and T/PR calculated by both individual and whole group way. Results The casual blood pressure (CBP) and ABP were lowered by (24 ±12) / (12 ±8) mmHg and (14.5 ±3.9) / (11.2 ±3.0) mmHg. The T/PR by individual w ay was 0.65 ±0.23 for SBP and 0.66 ±0.25 for DBP, while by whole group way 0.62 for SBP and 0.68 for DBP. The smoothness index (SI), a new method for assessing the homogeneity of 24 hour blood pressure reduction by antihy pertensive therapy, was 3.74 for SBP and 3.77 for DBP after treatment. Conclusion Nifedipine GITS lowers blood pressure effectively and smoothly for 24 hours long. Antihy pertensive effects can be reflected by T/PR and SI.

Clinical study of leflunomide in the treatment of patients with active rheumatoid arthritis

LI Xiang-Pei, LI Xiao-Mei, WANG Guo-Sheng, SHAN Shu-Guang, QIAN Long

2001, 6(2):  142-144. 

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Aim To compare the effectiveness and safety of leflunomide (LEF) with those of methotrexate (MTX)in patients with active rheumatoid arthritis (RA). Methods 95 RA patients were randomly assigned to receive LEF or MTX. The patients in the treated group received LEF 20 mg·d^-1 and in the controlled group who received MTX 15 mg/wk totally 12 weeks. Results The total effective rates of the treated group and the controlled group were 90.0 % (n =50) and 95.6 %(n =45)respectively. There was no statistical significance between the two groups in the effectiveness (P >0.05).The adverse react ion rate was 14.0 % (7 case)in the treated group and 15.6 %(7 cases)in the controlled group. There was no significance difference between the two groups (P =0.83).But the adverse reactions were more tolerable in LEF group than in MTX group. Conclusion This study suggests that LEF is an effective and more safe drug for active rheumatoid arthritis in our country.

Clinical study of chunyangzhengqi capsule in treating acute gastro-enteritis

FU Nan-Lin, HUANG Shou-Zheng, GAN Lei, LIU Shang-Quan, GAO Qing-Hua

2001, 6(2):  145-147. 

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Aim To explore the efficacy and safety of Chunyang zhengqi (Chu) capsule in treatment of acute gastro- enteritis. Methods Fifty patients with acute gastro- enteritis (cold and damp syndrome) were randomly divided into a therapeutic group of 30 cases and acontrol group of 20 cases. In the therapeutic group each patient received 2 capsules of Chu capsule, twice daily, while in the control group received 3 grams of Chu pill, twice daily. Results After 3 days of treatment, 8 cases were cured, 15 improved obviously, 4 improved, and 3 improved insignificantly in the therapeutic group. There was no significant difference between the two groups in the total effective rate (90.0 % vs 85.5 %, μ=0.180, P >0.05). Conclusions Chu capsule and pill have similar therapeutic efficacy and safety in treatment of acute gastro-enteritis.

Clinical contrast study of anti-hypertensive drug valsartan vs amlodipine in hypertensive patients with left ventricular hypertrophy

JIANG Zhi-An, ZHANG Xiao-Guang, XIAO Wen-Liang, SUN Ping, LU Xiu-Hua

2001, 6(2):  149-150. 

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Aim To study clinical efficacy of valsartan, in comparison with amlodipine, in hypertentive patients with left ventricular hypertrophy. Methods 65 hypertentive patients with left ventricular hypertrophy is divided into two groups, with 33 cases in valsartan group and 32 cases in amlodipine group Valsartan 80 ~ 160mg and amlodipine 5 ~ 10 mg were taken by the patients in the two groups for 6 months respectively. 24 h ambulatory blood pressure monitoring (24 h ABPM) and color echocardiography were performed in the two groups before and after treatment. Results The parameters of 24 h ABPM (24 h SBP、 24 hDBP、dSBP、dDBP、nSBP、nDBP) and color echocardiography (IVST、PWT、LVMI) after treatment in the two groups were significant decreased compared with those before treatment respectively (P <0.01). However, in the parameters after treatment, there was not significant difference between the two groups (P >0.05). Conclusion Valsartan can lower significantly the blood pressure level and make left ventricular hypertrophy remarkably dispelled in hypertensive patients with left ventricular hypertrophy and has the effect similar to that of amlodipine.