Table of Content

Volume 4 Issue 3
26 September 1999

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Antitumor effects of docetaxel alone and in combinat ion with batimastat in human giant cell carcinoma of the lung model

GU Bin, WU De-Zheng, LIANG Yue-Qin, LU Huan-Zhang, GAO Hong-Zhi

1999, 4(3):  185-190. 

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Aim To study the effect of docetaxel alone and in combination with batimastat (BB-94)on human giant cell carcinoma of the lung (PG).Methods and Results Growth curve analysis, MTT assay and clonogenic assay were used to determine the cytotoxic effect of docetaxel or/and BB-94 on PG cell in vitro.The results showed that docetaxel but not BB-94 had a significantcy to toxicity, and the effect of docetaxel was not enhanced by BB-94.In early stage PG tumor model, obvious antitumor effect of docetaxel or doxorubicin doxorubicin given iv at maximum tolerated dose(MTD, docetaxel 20 mg·kg^-1, dox orubicin, 6 mg·kg^-1)every 4 days for 3 injections(q4d×3), even of BB-94 (30 mg·kg^-1, ip, qd×20)was observed. Tumo rg rowth inhibition was greater for Docetaxel-bat imastat (97.3 %)than for doxorubicin-batimastat (86.5 %), docetaxel (92.0 %), doxorubicin (74.0 %)and BB-94(31.0 %).Docetaxel also showed active against advanced stage PG tumor in dose-dependeNTManner, and was more effective at MTD than do xorubicin with 4/5 regression, 55.8 day stumor growth delay and 2.8 log 10 tumor cell kill.Conclusion Docetaxel is an effectivecy to toxic new drug against PG tumor, and BB-94 can enchance the antitumor activity of docetaxel.

TAA-1 in treatment of experimental rabbit endocardit is induced by α-hemolytic streptococcus

ZHANG Chun-Fen, WANG Qing, ZHANG Jin-Ping, DONG Hai-Xin, LI Jian-Mei, XING Qin, LUN Xue-Qing, YANG Lei, LIU Shan-Tin

1999, 4(3):  191-194. 

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Aim The curative effect of TAA-1, a new component of Amethy stoidin, on rabbit endo cardit is induced by α-hemolytic streptococus was observed.Methods A sterile polythelene catheter was inserted through the right carotid artery of rabbits into the ventricle and 24 h after the operation, every rabbit was given 109CFU α-hemolytic streptococcus from earvein.After 24 h, the animals were divided into two groups.Animals in the control group were treated with NS, 0.2 ml · kg^-1 and in the treatment group with TAA-1, 0.25 mmol · kg^-1, ipqd for 7d.All the animals weRescarified, somet issues of the heart were used for examination of the histological changes and some for observation of the aortic and ventricale neoplasm.Results In the treatment group, the neoplasms weResmaller. Both the count of organisms in blood and neoplasm and the injury degree of myocardium were much less than in the control group.Conclusion TAA-1 has curative effect to endocarditis induced by α-h emolytic streptococcus.

Effects of sasanquasaponin on activities of Ca²⁺-Mg²⁺-ATPase and Na⁺-K⁺-ATPase and contents of Na⁺,Ca²⁺,Mg²⁺ in myocardial mitochondria in ischemic rats

HUANG Qi-Ren, CAO Shou-Yi, LI Ping, PENG Wei-Jie, HE Ming, LIU Huan-Bin

1999, 4(3):  195-197. 

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Aim and Methods To observe the effects of sasanquasaponin(SQS)on the activities of Ca²⁺-Mg²⁺-ATPase and Na⁺-K⁺-ATPase and the contents of Na⁺, Ca²⁺ and Mg²⁺ in ischemic myocardial mitochondria of rats, my ocardiali schemiarat model was induced by subcutaneous injection of isoprote renol (ISO, 4 mg · kg^-1)and some model rats were given SQS (0.2 mg · kg^-1)once daily for 3 days.Results As compared with those in the control, myocardial mitochondrial Mg²⁺ content was markedly reduced, while the contents of Na⁺ and Ca²⁺dramatically increased and the activities of Ca²⁺-Mg²⁺-ATPase and Na⁺-K⁺-ATPase were decreased significantly in ischemic rats administering SQS(0.2 mg · kg^-1, iv).Conclusions QS has cytopretectiveef ect by antagonizing the overload of Na⁺, Ca²⁺ in ischemic myocardial mitochondria.

Lipid peroxidation injury of liver after ischemia-reperfusion and protection effect of vitamin C

WANG Wan-Tie, LIN Li-Na, XU Zheng-Jie, LI Dong, WANG Zong-Min

1999, 4(3):  198-200. 

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Aim To explore the treating effect of vitamin C(VitC)on lipid peroxidation injury of liver after ischemiz-reperfusion.Methods A model of hepatic ischemia-reperfusion in rabbits was established to invest igate the alterat ions of lipid peroxide by measuring malo ndialdehyde (MDA)and vitamin E (VitE)in plasma or liver t issue, and to observe the morpholog icachanges of hepatocytes. A large dose of VitC was given to the model aninals to observe its preventing and treating effects on lipid peroxidation injury of the liver (VitC in a dose of 0.25 g ·kg^-1).Results The degree of lipid peroxidation was streng thened and the morphological changes of hepatocy tes were more obvious during hepatic ischemia-reperfusion when VitC was given before ischemia and before reperfusion, respectively, the degree of lipid peroxidation was remarkabley weakened and the abnormal changes of hepatocytes weResig nificantly at tenuated.Conclusion VitC in a dose of 0.25 g · kg^-1 would inhibit or ameliorate lipid peroxidation injury of liver after ischemia-reperfusion.

Comparative study on bioavailability and bioequivalence of clarithromycin disperse tablets and limaixian tablets in healthy volunteers

GUO Rui-Chen, WANG Ben-Jie, XU Wei-Fen, LI Bo, ZHANG Qing-Yin, MA Xiao-Hui

1999, 4(3):  202-204. 

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Aim The bioavailability and bioequivalence of clarithromycin disperse tablets (as test preparation)and Limaixian tablets (as reference preparation)weRestudied in 8 healthy volunteers with a double-cross design test.Methods The serum concentrations of clarithromycin after a sig le oral dose of 500 mg of the test preparation or reference preparation were determined by microassay method. Datum were analysed with 3p97 pharmacokinetic programme and two-one sidedt test and (1-2α)confidence interval analysis.Results The Ka, t_1/2 (α), t_1/2(β), C_max, AUC (0 ~ ∞)of the two preparations were 0.7843 and 0.5893 h^-1, 1.7324 and 2.3140 h, 4.1449 and 3.8635 h, 2.2308 and 1.8742μg ·ml^-1, 17.7410 and 16.2751 μg · h ·ml^-1, respectively.The relative bioavailability of clarith romycin desperse tablet was 106.21 %.Conclusion The bioequivalence of AUC between test and reference preparations, phases and subjects shows no significant differences (P>0.05).

Effects of total parenteral nutrition on pharmacokinetics of netilmicin

YUAN Cheng, JIA Nuan, FENG Lin, XUE Zuo-Ying, LIANG Zhu

1999, 4(3):  206-208. 

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Aim The pharmacokinetics of netilmicin(NTM)in the patients receiving total parenteral nutrition (TPN)was studied.Methods Seven patients with intestines fistula under TPN and seven patients in control group received 5 mg · kg of NTM by iv infusion in 0.5 h.NTM concent rations in serum and urine were determined by a high performance liquid chromatog raphy-indirect photometric determination (HPLC-I PD)method.Pharmaco kinetics parameters were computed with the 3p87 program.Results After intravenous administration of NTM 5 mg ·kg^-1, the NTM chromatog raphy peakconcent ration in serum was insignificantly lower in the TPN group than that in the control group (P>0.05), but the N TM level in the TPN group became higher than that in the control group (P>0.05)at 5th hour and significantlyhig her at 12 th hour after beg inning of administration (P<0.05).The reclamations of original shape NTM in urine were (52±13)% in the TPN group and (63±13)% in the control group. Pharmacokinetics calculations were disposed to two-compartment open-system model with t_1/2(β)=(5.8±1.6)h, Vc =(0.47±0.15)L · kg^-1 in TPN and t_1/2(β)=(3.5±1.4)h, Vc =(0.28±0.09)L ·kg^-1 in the control.Conclusion There is a marked drop in the removing rate of N TM from body.

Effect of radis astragal l on ICAM-1,CD126 expression and ECM synthesis in human fibroblasts

WANG Yao-Jun, SUN Zi-Qin, QUAN Qi-Zhen, QI Feng, JIAGN Xue-Liang, ZHANG Xiu-Li, WANG Dong

1999, 4(3):  209-210. 

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Aim To explore the ant i-fibrotic mechanism of Radis Astragali, we observed the ICAM-1 and CD126 expression affected by Radis Astragali in human fibro blasts.Methods Different do sages of Radis Astragali were added in the mediums for fibroblast culture.The ICAM-1 and CD126 positive cells were assessed by using flow cytometry.Results Positive rate of ICAM-1 and CD 126 in normal cultural fibroblasts was 82.63±5.94 and 77.95±4.68 respect ively.It decreased in cultural fibroblasts with Radis Astragali.Conclusion Radis Astragali can inhibit the immune-adhensive function of fibroblasts, which may-be one of its anti-fibrotic mechanisms.

Comparative study of effects of china-produced and imported zopiclone in amygdala-kindled rats

ZANG Dong-Lina, XU Qing-Rong

1999, 4(3):  211-213. 

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Aim The effect of China-produced zopiclone and imported zo piclone in amygdala kindled rats were compared.Methods Amygdala kindling model was built in female wistarrats.The kindled rats were given orally china-produced and imported zopiclone in the doses of 1.5, 3 and 5 mg · kg^-1 or veicle (1.25 %mucilag ot ragacanthae), respectively. SeizuReseverity and after discharge duration were oberved before and 30 minutes after adminstration.Result Both china-produced and imported zopiclone weakened the seizuReseverity and decreased the after discharge duration in doses of 3and 5 mg · kg^-1 notably. There was a significant difference between before and after drug treatment (P<0.01), but there was not a significant difference between two drugs at 3 and 5 mg · kg^-1 doses(P>0.05).Conclusion Both china-produced and imported zopiclones inhibited kindled seizures.The intensity of two drugs are equal basically.

Interact ion of ampicillin and chiorogenic acid in urine pharmacokinetics in children

CAI Qing, YUAN Rong-Hua, MENG Jun

1999, 4(3):  214-217. 

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Aim The interaction of ampicillin(AMP) and chiorogenic acid (CHA), a primary component of Shuang huanglianpulv(SHLP)on urine pharmacokinetics in children was observed.Methods After a single ivdrip dose of 60 mg · kg^-1 SHLP or/and 150 mg ·kg^-1 AMP was given to the children infected in respiratory system, the concentrations of CHA and AMP in the urine collected a t varying time point s w ere determined by a high performance liquid chromatography (HPLC).Results Compared with CHA and AMP used alone, there was a decrease (P<0.05)in the discharge rate drugs within 24 h of the two the drugs used in combination from (51.7±15.6) % and (76.3±20.5)% to (42.1±12.2)%and (62.3±19.3)%for CHA and AMP respectively.The values of t_1/2 of CHA and AMP were increased from (3.44±1.14)h and (1.98±0.51)h to (4.33±1.38)h and (2.67±0.75)h(P<0.05).The results led to a decrease in ClR.Conclusion The discharge of CHA and AMP is decreased when SHLP and AMP are used in combination.

Antipyretic and anti-inflammatory effects of Niu Huang Qian Jin San

XU Qing-Rong, LI Na, XU Yong

1999, 4(3):  218-219. 

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Aim The antipyretic and anti-inflammatory effects of Niu Huang Qian Jin San was explored.Methods (1)The anti-inflammatory effect of Niu Huang Qian Jin San was tested by using the method of swelling rat toes;(2)The antipyretic effect of Niu Huang Qian Jin San was determined by the method that colitox in was injected into rabbit's auricular vein.Results (1)Niu Huang Qian Jin San has manifest anti-inflammatary effect. After using the medicinc, there is much more difference of the swelling degree of the rat toes than that of NS(P<0.01).(2)Niu Huang Qian Jin San can streng then the antipyretic effect of aminopyrine CO. There is very remarkable difference of the centigrade temperature rising between the group injected Niu Huang QIan Jin San and the comparison group injected NS.Conclusion Niu Huang Qian Jin San solution has significant antipyretic and anti-inflammatory effects.