Table of Content

Volume 2 Issue 1
26 March 1997

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Efficacy of tablet huperzine-A on memory and cognition in patients with benign senescent forgetfulness

Xu Sisun, Xie Haibao, Du Zunming, Tong Zhenhua, Shi Qichang, Lu Keming, Li Shulan, Lin Bing

1997, 2(1):  1-3. 

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Aim To evaluate the efficacy and safety of tablet huperzine-A(Hup)in patients with benign senescent forgetfulness.Methods Using multicenter, prospective, double-blind, parallel, placebo controlled and randomized method,50 patients were administrated orally 0.15mg (3 tablets)Hup and 50 patients were given po 3 tablets of placebo bid for 4 wk.All patients were evaluated with Wechsler memory scale, mini-mental state examination scale,treatment emergency symptom scale, and measured BP,HR,ECG, EEG, ALT, AKP, BUN, Cr, Hb, WBC, and urine routine.Results Seventy four percent of patients treated with Hup (37/50)showed improvements in their memory (P<0.01)and cognitive functions(P<0.01).The efficacy of Hup was better than placebo(40%,20/50)(P<0.05).No severe cholinergic side effect was found.Conclusion Hup is an ideal drug for symptomatic treatment of patients with benign senescent forgetfulness.

Tolerance test of D-propranolol and its effect on sugar, lipid metabolism and sex hormone levels by intravaginal administration in rats and rabbits

Lu Renkang, Pang Shoujing, Yuan Dexiang, Qin Jinxi, Xu Lan, Zhu Qisun

1997, 2(1):  5-7. 

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Aim To study the tolerance of D-propranolol and is effect on sugar lipid metabolism and sex hormone levels by intravaginal administration in rats and rbbits.Methods 1.Rabbit group:three rabbits were given D-propranolol suppository (each suppository contain D-propranolol 60mg and opporture amount polyethanediol)by vaginal insertion, q.d. for 10 days. 2.Rat group:12 rats were given D-propranolol solution (40mg/ml)0.2 ml by direct injection into rat vagina q.d. for 56 days and blood samples were collected for measurement of blood sugar, lipids and sex hormone levels every 2 weeks.Immediately after killing all subject animals.Vaginal tissues were examined by macroscopy and microscopy.Results In the rabbits and rats group, no marked lesions of vaginal tissues were observed and the tissues did not significantly differ from those in the control group (P>0.05)and in rats group were slightly affected, i.e.mucosa edema and /or congestion but all those changes could be tolerated ,and there were no changes in blood sugar, lipids and sex hormones after treatmetn with D-propranolol for 8 weeks.Conclusions The results suggested that D-propranolol is safe when used in vagina.

Pharmacokinetics and bioavailability of naproxen sustained release capsule in normal men

Liu Changxiao, Gu Yibao

1997, 2(1):  9-11. 

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Aim The two-crossover trial was employed to compare the pharmacokinetics and bioavail-ability of naproxen sustained release capsule (SRC)with that of the standard tablet (ST)in healthy volunteers.Methods In single dose study, each of 10 volunteers received 500 mg naproxen in either of the two forms and in steady state study, 8 volunteers each received either 500 mg- SRC once daily (250 mg b.i.d.).The serum naproxen concentrations were deter-mined by a HPLC method.Results After single dose of the two forms, the area under curve (AUC)values of the the two forms were similar or equivalent.The peak concentrations (C_max)and peak time (T_peak)of two forms were different, the C_max and T_peak of SRC were 85.5 ug/ml and 6.0h, respectively;the C_max and T_peak of ST were 140.4μg/ml and 3.2h,respectively.In steady-state study, The steady state was achieved on day 3.At steady state, the C_max, C_max/C_min ratios and degree of peak-trough fluctuation (DF)during SRC administration were lower than those during ST administration.Conclusion The naproxen SRC showed its sustained release effect, therefore, it should provide patients with a convenient, efficacious dosage form of naproxen that maintains therapeutic naproxen levels in blood.

The Comparision of Combined Postantibiotic Effects Induced by Amoxacillin Plus Gentamicin or Netilmicin

Wang Rui, Liu Guiyang, Zhou Liang, Fang Yi, Chen Qian, Liu Qingfeng

1997, 2(1):  13-15. 

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Aim The postantibiotic effects(PAEs)induced by Amoxacillin(AMPC)alone or com-bined with gentamicin(GM)or netilmycin(NTL)were studied.Methods The PAEs were determined by the spectrophotometric method.Results The PAEs induced by AM- PC alone to S.aureus and E.faecalis were long;whereas to E.coli, the PAEs were poor.PAEs induced by GM or NTL alone to Gram-positive cocci were longer than to Gram-negative bacilli.The PAEs of NTL were more obvious than those of GM.The PAEs of AMPC combined with 4x MIC of GM or NTL were all synergic or additive, and the combined PAEs to Gram-positive cocci were longer than to Gram-negative bacilli.The combined PAEs of AMPC plus NTL were more obvious than plus GM.Conclusion It is suggested that the rational prelonged dosing intervals in combinations of AMPC with two aminoglycosides should be recommended.

Study on the serum bactericidal activity and clinical effects of cefotaxime in patients with hematopathy and infection complication

Wang Rui, Chen Qian, Chen Mengli, Lou Fangding, Zhu Jun, Han Xiaoping, Tan Cie, Pei Baoxiang, Wang Aizhen

1997, 2(1):  17-19. 

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Aim The serum bactericidal action (SBA)of cefotaxime and its clinical effect were observed and compared with two schedules of antimicrobial chemotherapy in patients with hematopathy complicated by infection.Methods Thirty patients in 3 groups were treated with cefotaxime (CTX), piperacillin plus amikacin (PIP + AN)and cefoperazone (CPZ)respectively.The SPA was determined by microdiluted method and the clinical effect was judged according to the records of symptoms and clinical effect was judged according to the records of symptoms and clinical findings recorded before and after treatment.Results In comparison with CPZ and PIP + AN, CTX had better SBA and longer antimicrobial time.As to against defferent strains of infection-causing bacteria the SBA of CTX to Ps aeruginose and E cloacea was weak, while PIP + AN had a broader antimicrobial spectrum, but the antibacterial time of PIP was short.Among the three antimicrobials there was no statistical defference in clinical effect.Conclusion To enhance the efficacy and reduce adverse reaction the dosing time should be regulated.It is recommended that piperacillin and cefoperazone be given three times daily, cefotaxime twice a day and amikacin once a day.

In vitro postantibiotic effects induced by cefoperazone alone and in combination with sulbactam

Liu Guiyang, Wang Rui, Fang Yi, Cheng Qian, Liu Qingfeng, Zhou Liang, Qin Yanbing

1997, 2(1):  20-22. 

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Aim The postantibiotics effects (PAEs)induced by cefoperazone (CPZ)alone were to be compared with those induced by a 1:1 combination of CPZ and sulbactam(SBT).Methods Ail the clinical isolates selected, including every six isolates of E.coli, S.aureus, Proteus and P.aeruginosa, were proved to be beta-lactamase-producing strains by the Nitrocefin Test.The PAEs were determined by means of measurement of transmittance using AVANT AGE Microbiology System.Results Longer PAEs induced by the combination of CPZ and SBT were observed in each concentration, even in lower CPZ concentrations (1/2 and 1 MIC), the PAEs were significant longer than by CPZ alone.Conclusion The results suggest that the efficacy of CPZ combined with SBT is stronger than that of CPZ alone against the infections caused by beta-lactamase-producing isolates.

The study on postantibiotic effects induced by three penicillins in vitro

Qin Tingbin, Wang Rui, Liu Guiyang, Liu Qingfeng, Fang Yi, Chen Qian, Zhou Liang

1997, 2(1):  24-26. 

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Aim To study the postantibiotic effects(PAEs)in vitro induced by three penicillins.Methods The PAEs induced by Cloxacillin (CXL), Amoxacillin(AM)and Mezlocillin (MZL)against three species of bacteria were determined by spectrophotometric method.Results Marked PAEs were found, even in the sub-MIC concentration of these penicillins and there was a strong concentration-dependence.Negative PAEs were defined, however,when AM and MZL were used against gram一negative bacilli.Conclusion The results suggested that longer dosing interval, especially when penicillins were used against gram -positive coccus, should be recommended.

Comparision of pharmacokinetics of tacrine between young rats and aged rats

Yin Xiaoxing, Tang Xingchuen, Yan Mei, Hu Gang

1997, 2(1):  27-29. 

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Aim To compare the pharmacokinetics of tacrine (THA)between young rats and aged rats.Methods After ig and iv THA 8 mg/kg,the plasma THA concentrations in rats were determined by reversed phase HPLC.The compartment model and the pharmacokinetic parameters were calculated by CAPP software.Results The concentration-time curve was de-scribed by a two-compartment open model.The concentrations of THA in aged rats were much higher than those in normal rats.After iv administration, the main pharmacokinetic paramaters in young rats such as T_1/2α,T_1/2β and AUC were 10±6 min, 60±6 min, and 34±13g/ min·L, while those in aged rats were 18±3 min, 98±19 min, and 55±7 g/ min·L, re-spectively.After ig THA,the values of T_1/2α,T_1/2β,AUC, Gm and T_p in young rats were 7±2min,63±8 min,12±5 g/ min·L, 130±58 μg/L, and 19±2 min,while those in aged rats were 9±1 min, 98±28 min, 24±10 g/min·L,218±72 μg/L,23+2 min, respectively.The parameters were significant differences between the two kinds of rats (P<0.05 or P<0.01).Conclusion The absorption, distribution and elimination of THA in aged rats were slower than those in young rats.

Effect of Irbesartan on vascular wall cell proliferation after balloon denudation in rat iliac artery

Cheng Xunmin, He Guoxiang, Wang Guochao

1997, 2(1):  30-32. 

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Aim To study the effect of Irbesartan on neointimal proliferation in vivo after vascular injury.Methods Iliac arteries of Wistar rats were injured with a 2 French balloon catheter.Irbesartan (30mg/kg.d or 10mg/kg.d)or vehicle was given by gavage from 1 day before to 14 days after balloon injury.Morphometrical changes in the injury iliac artery were analyzed.Results Irbesartan significantly inhibited the increase of cell count in injured vessel wall, intimal thickening and vascular smooth muscle cells proliferation in a dosage-dependent relationship.The cellular density of the neointima was not affected by Irbesartan.Conclusion The results indicate that Irbesartan may reduce neointima formation after blloon injury and therefore it may be capable of preventing testenotic lesions after angioplasty in humans.

Curative effect of tongpitang combined with methotrexate on rheumatoid arthritis

Gao Jiajun, Tong Dachun, Zhu Lulai, Wang Hemin

1997, 2(1):  33-35. 

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Aim The efficacy of Tongpitang (a recipe consisting of 19 Chinese medicinal herbs)decoction in combination with methotrexate (MTX)against rheumatoid arthritis (RA)was to be observed.Methods Tongpitang (once daily)and MTX (7.5mg once weekly)were prescribed to 79 patients with RA for 3 months as a course.Serving as control, other 40 cases of RA were prescribed Fengshiye (a traditional Chinese medicinal preparation)combined with MTX.Eighteen cases from the Tongpitang group and nine cases from the control group were supplementally injected with Fengsiling.Results In comparison with the control, Tongpi-tang combined with MTX gave significant efficacy in relieving joint swelling and pain, shortening the morning stiffness, restoring IgG, IgM and IgA and dropping sedimentation.The negative conversion rate of rheumatoid factors reached 67.75%.There was no side- effect during hormone administration or rebound phenomeonafter stoping it.Conclusions Compared with single MTX of Fengshiye plus MTX, Tongpitang in combination with MTX gives the best curative effect in the treatment of rheumatoid arthritis.

Protective mechanism of sodium ferulate against gentamicin - induced nephrotoxicity in Renal tubular cells

Huang Yunjian, Liao Lisheng

1997, 2(1):  37-39. 

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Aim To investigate the effect of sodium ferulate(SF), a compound derived from Chinese herbs，on gentamicin (GM)nephrotoxicity in renal tubular cells.Methods Alanine aminopeptidase (ALT), catalase (Cat), and N-acetyl-β- glucosaminidase (NAG)activities, DNA synthesis, cytosolic free calcium concentration, and morphological alterations were observed in gentamicin-induced damage to cultured primary renal proximal tubular cells.The protection of SF to damages was observed too.Results In GM group, ALT and Cat activities decreased, NAG activity invreased;besides, DNA synthesis decreased and cytosolic free calcium concentration increased.Electronmicrosope observation revealed an extensive vacuolization in proximal tubular cells and formation of myeloid bodies in lysosome.Simultaneous administration of SF with GM could markedly improve the values of parameters mentioned above and the histological damages.Conclusion SF can protect renal proximal tubular cell from GM nephrotoxicity.

Relationship between cardiac diastolic function and the efficacy of thrombolytic therapy on acute myocardial infarction

Xu Zhimin, Wang Lei, Hu Dayi, Zhai Liang, Wu Yafeng, Liu Xianhui, Liu Jianzhang

1997, 2(1):  41-42. 

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Aim To observe the relation between cardiac diastolic function and the clinical efficacy of Venous thrombolytic therapy on acute myocardial infarction (AMI).Methods In 50 patients.with AMI receiving venous thrombolytic therapy the ratio of velocity area of peak A/ peak E (VA/VE)from mitral flow , left ventricular ejection fraction (LVEF), fractional shortening at minor axis (FS)were measured by Color Dopplet Flow Imeging, HP2500 and clinical cardiac functions were judged by killip grades.Results (1)There were no differencies in age, sex, AMI locations, clinical cardiac function， LVEF, FS and histories of hypertension, diabetes and old myocardial infarction both among 36 cases of reperfusion and 14 cases of nonreperfusion (all P>0.05).(2)The ratio of VA/VE was lowwer in the reperfusive group than that in non-reperfusive group (1.0129±0.3427 us 1.3335±0.4077, P<0.01);patients with VA/VE> 1 less in reperfusive group (47.2% us 85.77%，P< 0.05).Conclusion There might be more protective efficacy on left ventricular diastolic function after IRA reperfusion in AMI cases treated by venous thrombolytic therapy.

Significance of determination of thrombomodulin in kidney-transplanted recipients

Xu Feng, Wu Zhaohui, Zou Henqin, Zhang Zhongyi

1997, 2(1):  43-44. 

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Aim To evaluate the clinical significance of determination of plasma thrombomodulin in kidney-transplanted recipients.Methods The plasma thrombomodulin levels in 19 kidney trans-planted recipients were determined with ELISA method.Results TM levels in group of postoperation normalcy were significantly lower than those in group of cyclosporine nephrotoxicity and group of acute rejection(P<0.01), while the cyclosporine blood concentrations in group of cy-clsoporine nephrotoxicity were significantly higher than those in group of post-operation normalcy and group of acute rejection(P<0.05).Conclusion The determination of thrombo-mudulin may be helpful in distinguinshing cyclosporine nephrotoxixity from acute rection.

Therapeutic drug monitoring of cyclosporine in Kidney-transplanted recipients

Wu Zhaohui, Xu Feng, Zou Hengqin

1997, 2(1):  45-47. 

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Aim To observe the relation between the blood cysclosporine concentration.Methods The therapeutic drug monitoring data of cyclosporine in 97 kidney-transplanted recipients in 8 weeks, from May 1995 to October 1996, were analysed retrospectively.The recipients were sorted in three groups，the normal group, the acute rejection group and the acute toxicity group.Blood cyclosporine concentration was measured by FPIA with monoclonal antibody reagent.Results In normal group, 62 recipients had good kidney function, with average daily dose of cyclosporine 5.2±1.9mg/kg·d, the blood concentration of cyclosporine was 309.85±131.69μg/L ;In acute rejection group, the average daily dose in 26 recipients was 4.8±1.6mg/kg·d, the blood concentration of cyclosporine pending rejection episode was 165.80±123.13μg/L;In acute toxicity group, the average daily.dose in 9 recipients was 6.2±1.0mg/kg·d, the cyclosporine blood concentration pending toxicity episode was 556.51±102.50μg/L.There was no sigificant difference among the three groups on the average daily dose of cyclosporine (P>0.05).However，the blood concentration of cyclosporine in three groups varied greatly and there was significant difference among them(P<0.05，even P<0.01 between acute rejection group vs toxicity group).Conclusion In therapeutic drug monotoring of cyclosporine measurement of blood drug concentration is extremely important.More acute rejection episodes occur with low blood concentration of cyclosporine, while more toxicity episodes happen with high blood concentration.