Table of Content

Volume 12 Issue 1
26 January 2007

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New era of individualized pharmacotherapy

LIU Zhao-qian, ZHOU Hong-hao

2007, 12(1):  1-6. 

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Along with deep scientific research and continual development of pharmacogenetics and pharmacogenomics, the new era of individual pharmacotherapy will come true in the future. The genetic variations of drug related proteins including drug metabolism enzymes, drug transport proteins, and drug active receptors and or targets are basic factors resulting in individual and ethnic differences in drug response. Choosing the suitable drugs and dosages according to genotypes of drug related proteins in patients will furthest improve the pharmacotherapy efficacy and reduce the adverse drug reaction and toxic effect of drugs.

Progress and research in pharmacogenetics of oral antidiabetic drugs

ZHANG Wei, WANG An, ZHOU Hong-hao

2007, 12(1):  7-10. 

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Diabetes mellitus is a metabolic disease influenced by numerous genes and environmental factors. The genetic polymorphisms of drug-metabolizing enzymes, transporters or receptors play very important roles in the metabolism and therapeutical efficacy of oral antidiabetic drugs.In this review, we summarized the effects of genetic polymorphisms of certain CYP450 enzymes, transporters or receptors on the drug metabolism and efficacy of oral antidiabetic drugs including sulfonylureas, thiazolidinediones, meglitinide analogues, biguanides and α-glucosaccharase inhibitors.

Relationship among base, objective and clinical trial design in development of new traditional Chinese medicine and natural drugs

CHENG Long

2007, 12(1):  11-13. 

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The relationship was described among base, objective and clinical trial design in the development of new traditional Chinese medicine, and natural drugs in this paper.It will provide a reference for researchers to develop the type of drugs.

Progress in research on animal models of chronic nonbacterial prostatitis

QIAN Bo-chu, SHI Hong, ZHENG Xiao-liang

2007, 12(1):  14-18. 

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Chronic nonbacterial prostatitis is a common urologic condition which is difficult to be treated effectively. Little is known about the etiology and pathogenesis of the disease. Preparation of the animal model of chronic nonbacterial prostatitis is an effective method to research the pathogenesis of the disease and development of new drug. Different animal models have distinctive traits, therefore, it is crucial to select suitable animal models for researching human diseases. In the review, the progress in the research on animal models of such disease is discussed.

Advancement of toll-like receptor 4

ZHAO Bao-sheng, HUO Hai-ru, JIANG Ting-liang

2007, 12(1):  19-22. 

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Toll-like receptors are main receptors for the innate immune system to recognize pathogenic microorganisms and thus educe very important effect in the innate immune reactions. Toll-like receptor 4 (TLR4)is one of the major receptors which mediates the signal' s transmembrane transduction, and is of great important to the infective inflammation caused by Gram-negative bacteria.Recently, more and more researchers paid close attention to TLR4 and its signal transduction mechanisms. This review describes the signaling transduction of TLR4, the relationships between TLR4 and lipopolysaccharide(LPS), TLR4 and diseases, confirms the significance of TLR4 research.

Comparison of inhibitory effects of CPU-86017 and its optical derivates on mouse blood pressure and rat aortic contraction

FENG Yu, YANG Lin, DAI De-zai, ZHANG Can, DAI Yin

2007, 12(1):  23-27. 

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AIM: To compare the effects of III Class antiarrhythmic CPU-86017 ( p-chlorobenzyl-tetrahydroberberine) and its 12 optical derivates on mouse blood pressure and rat aortic contractile activity. METHODS: Zh-005 to zh-008 are 4 stereoisomers of p-nitrobenzyl-tetrahydroberberine, and zh-009 to zh-012 are 4 stereoisomers of N-benzyl-tetrohydroberberine.In this study, CPU-86017 or zh-005-zh-012 at dose of 3 mg/kg were i.v.in anaesthetized mice, and the blood pressure was monitored by arterial cannulation for 3 hours.CPU86017 or zh-001 to zh-004 (the 4 stereoisomers of CPU-86017) was administered in gradient dosage to rat aorta in vitro for evaluation the effects on aortic contraction induced by Phe and KCl. RESULTS: The least potency on blood pressure of CPU-86017 and zh-005-zh-012 was found by iv zh-006, which suggested the least side effect. By study of the inhibitory effects on rat aortic contraction of CPU86017 and zh-001 to zh-004, we found that the stereoisomers showed a stereoselectivity on suppressing the receptor related Ca²⁺ channel ( ROC), but not the voltage dependent Ca²⁺ channel (VOC). CONCLUSION: The configuration of C-13a in the structural formula of p-chlorobenzyl-tetrahydroberberine might be dominant to its affinity to α1A receptor.

Effects of glucagon-like peptide-1 prodrug on glycemia control in non-diabetic mice

MA Xue, HUI Hong-xiang, LIU Zhen-guo, WU Yu-mei, MENG Jia, LUO Xiao-xing

2007, 12(1):  28-31. 

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AIM: To study the effects of proglucagonlike peptide-1, a long-acting prodrug glucagon-like peptide-1, on regulations of blood glucose levels and insulin secretion in non-diabetic mice. METHODS: Pro-GLP-1 was administered via scroute.Blood glucose levels were measured using a blood glucose meter.Plasma insulin concentrations were determined by ELISA. RESULTS: In C57BL 6 mice, native GLP-1 and Pro-GLP-1 decreased blood glucose, but Pro-GLP-1 had a more evident action.A single injection of Pro-GLP-1 dose-dependently reduced higher glucose following glucose load at least 3 h,and it had no effect on normal blood glucose.Moreover, it dose-dependently stimulated insulin secretion and significantly improved glucose tolerance after glucose challenge. CONCLUSION: These results demonstrate that Pro-GLP-1 facilitates a dose-dependently significant and prolonged glucose-lowering effect.

Synergistic protective effect of picrosideⅡand NGF on PC12 cells against oxidative stress induced by H₂O₂

ZHANG Xiao-dong, LIU Jian-wen, LI Ting, CAO Yan, GUO Ming-chuan

2007, 12(1):  32-37. 

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AIM: To study the synergistic protective effect of picroside Ⅱ and NGF for the oxidative stress on PC12 cells induced by hydrogen peroxide (H₂O₂). METHODS: The fluorescent probe 6-carboxy-2', 7' -dichlorodihydrofluorescein (CDCFH) was used to assess the intracellular reactive oxygen species (ROS) level, and MTT assay, morphological observation as well as lactate dehydrogenase (LDH) leakage were conducted to measure cellular injury. RESULTS: The H₂O₂-induced cytotoxicity was significantly attenuated in the presence of picroside Ⅱ (25 μg/mL) and NGF (2 ng/mL).Cultures with this combined treatment possessed decreased level of ROS while increased cell survival, as compared to that of picroside Ⅱ or NGF alone-treated cells.Accordingly, it was concluded that their synergistic protective activities against oxidative stress in vitro were demonstrated in various aspects including reversing morphological changes, enhancing the ability of cell proliferation and ROS scavenging. CONCLUSION: Such action supports the therapeutic potential of picroside Ⅱ and NGF in treating nervous disorders based on their synergistic effect.

Effects of NS398 on cell cycle and related cyclin-dependent kinase inhibitors p21^waf1/cip1 and p27^kip1/pic2 in human pancreatic carcinoma cells

CHEN Qi-kui, HAN Ji-ao, CHEN Jing-wu, HUANG Zhi-qing, ZHU Zhao-hua

2007, 12(1):  38-42. 

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AIM: To investigate the effects of selective cyclooxygenase-2 (COX-2) inhibitor, NS398, on cell cycle and related cyclin-dependent kinase inhibitors p21^waf1/cip1 and p27^kip1/pic2 in human pancreatic carcinoma cells. METHODS: SW1990 human pancreatic carcinoma cells were treated with NS398 (100 μmol/L), prostaglandin E2 (PGE2, 10 nmol/L) and their combination, respectively.The inhibitory effects of NS398 on SW1990 cell were detected by using MTT assay.The cell cycle was measured with flow cytometry.The level of intracellular PGE2 was determined with ELISA.The mRNA of p21^waf1/cip1and p27^kip1/pic2was detected by semi-quantitative RT-PCR.The expression of p21^waf1/cip1 and p27^kip1/pic2 protein was detected by Western blotting analysis. RESULTS: NS398 inhibited the growth of SW1990 cell and decreased level of intracellular PGE2 in a dose-dependent manner.NS398 caused cell accumulation in G0 G1 phase that was 11 % higher than control.The mRNA and protein of p21^waf1/cip1and p27^kip1/pic2were up-regulated by NS398.PGE2 stimulated cell growth, but factorial experiment showed that 10 nmol/L of PGE2 could not antagonize inhibitory effects of cell growth, cell cycle distribution, transcription and expression of COX-2, p21^waf1/cip1 and p27^kip1/pic2 induced by NS398 in SW1990 cells. CONCLUSION: The results suggest that selective COX-2 inhibitor, NS398, can induce inhibitory effects of cell growth and G0 G1 cell cycle arrest in SW1990 cells by upregulation of p21^waf1/cip1 and p27^kip1/pic2 and may be not dependent of PGE2 pathway.

Signal transduction mechanism of inhibition of elemene on proliferation induced by recombinant human epidermal growth factor in lens epithelial cell

HUANG Xiu-rong, QI Ming-xin, HU Yan-hong, YAN Jing, WU Zheng-zheng, MA Lan

2007, 12(1):  43-46. 

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AIM: To investigate the effects of elemene(Ele) on intracellular concentrations of calcium([Ca²⁺]_i), cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lens epithelial cell (LEC) of proliferation induced by recombinant human epidermal growth factor (rhEGF), and the mechanism of signal transduction of inhibiting proliferation. METHODS: Proliferations of LEC were induced by rhEGF;[Ca²⁺]_i concentrations of LEC were determined by spectrofluoremeter;The intracellular concentrations of cAMP and cGMP were measured by radioimmunoassay. RESULTS: (1) [Ca²⁺]_i of LEC in the Ele group increased obviously compared with the proliferation group(P<0.01);(2) Concentrations of cAMP of LEC in the proliferation group decreased compared with the control group.Concentrations of cGMP of LEC in the proliferation group increased compared with the control group (P<0.01);(3) Concentrations of cAMP of LEC in the Ele group increased significantly compared with the proliferation group.Concentrations of cGMP of LEC in the Ele group decreased compared with the proliferation group(P<0.01). CONCLUSION: Elemene inhibits proliferation of LEC by means of signal transduction of [Ca²⁺]_i, cAMP, cGMP and interaction of multiple signal transduction, which may be the cellular and molecular mechanism of Ele inhibiting/LEC proliferation and preventing after cataract.

Ischemic preconditioning attenuates ischemia-reperfusion-induced abnormality of Na⁺-K⁺-ATPase protein expression in hearts

WANG De-guo, CHU Yue-feng, KE Yong-sheng, YANG Yu-wen

2007, 12(1):  47-51. 

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AIM: To study the role of Na⁺-K⁺-ATPase in the protective mechanism of ischemic preconditioning (IP) on myocardial ischemia and reperfusion injury. METHODS: Ligation of anterior descending branch of rat hearts for 30 min (ischemia) and reperfusion for 60 min were for establishing the model of ischemia reperfusion (I R), and 5 min of ischemia and 10min of reperfusion were made for three cycles with a view to preparing IP model.After hemodynamic data were recorded, myocardium sample was processed immediately in order to measure the activity of Na⁺-K⁺-ATPase and Ca₂⁺-Mg₂⁺-ATPase and the changes of protein expression of α1, α2,α3 and β1 isoforms of Na⁺-K⁺-ATPase. RESULTS: IRreduced cardiac contractile and diastolic function, activityof Na⁺-K⁺-ATPase and Ca₂⁺-Mg₂⁺-ATPase, and protein expression of α1, α2, α3 and β1 isoforms of Na⁺-K⁺-ATPase.IP attenuated the reduction of cardiac function, the activities and protein expression of Na⁺-K⁺-ATPaseα1, α2, α3 and β1-isoforms induced by I R.Digilanid Cabolished the effects of IP on Na⁺-K⁺-ATPase. CONCLUSION: The beneficial effects of IP on the prohibition of Na⁺-K⁺-ATPase induced by myocardial ischemia and reperfusion were abolished by cardiac glycoside.ProtectingNa⁺-K⁺-ATPase may play an important role in the mechanism of IP.

Effect of fluvastatin on expression of adhesion molecule and matrix metalloprpteinase-9 induced by lysophosphatidylcholine in human umbilical vein endothelial cell

LI Jian-zhe, CHEN Po-jing, CAI Zhi-chun, LIMin, WANG Chen-jing, WU Jian-hua, FANG Yun-xiang

2007, 12(1):  52-56. 

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AIM: To observe the effect of fluvastatin on the expression of adhesion molecule and matrix metalloproteinase-9 (MMP-9) induced by lysophosphatidylcholine (LPC). METHODS: The HUVECs were incubated with LPC for 0, 12, 24 and 48 h to detect the expression of adhesion molecule and MMP-9.The HUVECs were incubated with fluvastatin of different concentration for 20 min before incubated with LPC for 24 h.The expression of NF-κBp65, intercellular adhesion molecule-1 (ICAM-1) and (vaseular cell adhesion molecule-1, (VCAM-1) was detected by immunohistochemical method, and the mRNA expression of MMP-9 was detected by RT-PCR. RESULTS: LPC could significantly induce the expression of ICAM-1, VCAM-1 and MMP-9.NF-κBp65 protein and ICAM-1 expressions were related in linear correlation, as well VCAM-1 and MMP-9 expresions.Fluvastatin could inhibit the aboving effects in a concentration-dependent manner. CONCLUSION: The NF-κB activation which is induced by LPC enhances the ICAM-1, VCAM-1 and MMP-9 expressions, while fluvastatin is able to inhibit these effects.

Bcl-XL siRNA sensitisizes cisplatin-resistant human lung adenocarcinoma cells A549 to cisplatin

HUANG Ze-xiang, LIU Li-juan, YAO Shu-qiong, LEI Xiao-yong, ZHU Bing-yang, TANG Sheng-song, LIAO Duan-fang

2007, 12(1):  57-61. 

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AIM: To investigate the effect of Bcl-XL siRNA on apoptosis and drug sensitization in cisplatin-resistance human lung adenocarcinoma cell line A549/DDP and to determine the inhibitory effect of the Bcl-XL siRNA on the expression of Bcl-XL gene in cells A549/DDP. METHODS: Bcl-XL siRNA and negative siRNA plasmid vector were stably transfected into A549/DDP cells.Drug sensitivity of the cells to cisplatin ( DDP) was analyzed with MTT and flow cytometry.Spontaneous apoptosis of cells was detected by AO/EB dyeing.RT-PCR and Western-blot were used to detect the target gene expression. RESULTS: MTT results showed that Bcl-XL siRNA transfectants had a higher cell inhibition rate than negative siRNA or untreated cells after treated with 0.2, 2, 20, 200 μg/mL DDP.Moreover, flow cytometry results demonstrated that Bcl-XL siRNA cells had increased apoptosis rate after addition of 20 μg/mL DDP.Spontaneous apoptosis of cells were significantly increased in Bcl-XL siRNA stable transfectants.The mRNA and protein expression level of Bcl-XL in Bcl-XL siRNA stable transfectants were obviously reduced compared with negative siRNA transfectants or untreated cells, moreover, Bcl-XL siRNA increased the activity of active caspase-3. CONCLUSION: siRNA targeting Bcl-XL gene can specifically down-regulate Bcl-XL expression in A549 DDP cells, increase cell spontaneous apoptosis and sensitize cells to DDP.Bcl-XL siRNA may be a potential therapy agent against human lung adenocarcinoma.

Meta-analysis:influence of Utillin “s” on human CD₈⁺T cells

XU Yong-qiang, RUI Jing, LIU Chang-bao, CHEN Rong

2007, 12(1):  62-65. 

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AIM: To study the influence of Utilin“s” on human CD₈⁺ T cells. METHODS: Papers about the subject were searched from electronic documental databases.RevMan4.2 software was used for Meta-analysis during the procedure of evaluating, and SASv9.0 software was used to draw the funnel plot. RESULTS: Eight papers were found, and there was no statistical difference in CD₈⁺T cells between before and after using Utilin “ s”(P =0.12). CONCLUSION: No evidence suggests that the Utilin “ s” has significant influence on human CD₈⁺T cells.

Radioprotective effect of rhTPO on mice and MO7e cells

SU Ying-jie, LI Jing, YAO Ming-hui, GONG Qin-yan

2007, 12(1):  66-71. 

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AIM: To study the therapeutic action of homemade rhTPO on thrombocytopenia of irradiated C57 mice and the effect of homemade rhTPO on apoptosis of MO7e cells induced by irradiation. METHODS: The male C57mice underwent total body irradiation(TBI) with a single 4 Gy dose using a 137Cs γ-rays source, and the blood samples were taken at different time points pre- and post-irradiation by cutting tails, and the platelet counts were determined.MTT assay was used to measure the rate of irradiated MO7e cells.The apoptosis of MO7e cells was observed with flow cytometer and E.M.microscopy. RESULTS: RhTPO (4.5-18μg/kg) dose-dependently rose the circulating platelet counts of C57 mice reduced by irradiation and its effect was more powerful and faster than that of rhIL-11.In vitro, rhTPO 10 and 100 μg/L obviously increased the viability rate of MO7e cells and reduced the apoptosis rate of MO7e cells upon irradiation. CONCLUSION: The homemade rhTPO has the capability of reducing the damage of hematopoietic system in irradiated mice, decreasing the apoptosis rate of MO7e cells upon irradiation and increasing the viability rate of MO7e cells.rhTPO has significant protective effect on mice and MO7e cells against irradiation injury.

Effects of losartan on expression of matrix metalloproteinase-2,JNK1/2 and proliferation in cardiac fibroblast

XIAO Yun-bin, QIN Xu-ping, QIN Li, LIAO Duan-fang, HUANG Hong-lin

2007, 12(1):  72-77. 

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AIM: To elucidate the effects of losartan on the expression of matrix metalloproteinases-2, JNK1/2 and proliferation in cardiac fibroblast. METHODS: Neonatal rat cardiac fibroblasts were cultured.The cells proliferation was determined by MTT.To determine effects of Ang Ⅱ on JNK1/2 activity, cells were incubated (for 0,2, 5, 10, 30, 60, 120 min) in serum-free media with Ang Ⅱ, and the other group fibroblasts were exposed to serum-free media with or without Ang Ⅱ and losartan (Ang Ⅱ 100 nmol/L, Ang Ⅱ 100 nmol/L +losartan 100 nmol/L, losartan100 nmol/L, losartan for 45 min before).Cells protein was collected with MBST buffer.The relative abundance of MMP-2, JNK1/2 and p-JNK1/2 in cells was determined by immunoblotting.The secretion of MMP-2 in media of cell culture was determined by ELISA. RESULTS: Ang Ⅱ increased the proliferation of CFB in a dose-dependent manner, whereas losartan decreased the proliferation of CFB stimulated by Ang Ⅱ in a dose-dependant manner, too (P<0.05).The relative abundance of JNK1/2 was highest in Ang Ⅱ of the 2-minstimulated group.Ang Ⅱ increased expression of JNK1/2 andMMP-2 protein (P<0.05), on the contrary, losartan inhibited JNK1/2 and MMP-2 protein expression. CONCLUSION: Ang Ⅱ induce the increase of proliferation of CFB, expression of JNK1/2 and MMP-2 in CFB, and losartan inhibits these effects of Ang Ⅱ.

Effects of Yuxingcao injection on contents of cAMP in hypothalamus and AVP in ventral septal area in fever rats

WANG Hui-ling, CUI Wei, QIN Xin, FAN Shu-duo, LIU Hui-hui

2007, 12(1):  78-81. 

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AIM: To explore the antipyretic mechanisms of Yuxingcao injection in rats. METHODS: The fever model was made by suspension of yeast which was injected hypodemically to the rats.The contents of cAMP in hypothalamus and AVP in ventral septal area(VSA) were measured by radioisotope method. RESULTS: Yuxingcao injection possessed obvious antipyretic effect on fever rats and inhibited the increase of cAMP in hypothalamus and promoted the release of AVP in VSA.Correlation analysis showed that contents of cAMP in hypothalamus and AVP in VSA were positively correlated with the change of body temperature of rats. CONCLUSION: The antipyretic mechanisms of Yuxingcao injection may be due to inhibiting the increase in cAMP in hypothalamus and promoting the release of AVP in VSA, and the effects are dosage-dependence.

Pharmacokinetic-pharmacodynamic modeling and simulation:concepts and basic principles(1)

HUANG Xiao-hui, SHI Jun, LI Jun, XIE Hai-tang, ZHENG Qing-shan, SUN Rui-yuan

2007, 12(1):  82-89. 

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Modeling and simulation (M&S)is an important research field in pharmacokinetics and pharmacodynamics.M&S has evolved from a tool primarily applied to therapeutic drug monitoring to one that plays a significant role in drug development.Technological advances in various fields related to drug development call for more focus on ways to optimize current drug development practices.Recognition of the potential of M&S by regulatory agencies inevitably has a substantial impact on drug development.The objective of the current review is to present some of the basic concepts and principles of M&S.Case studies are presented to illustrate how M&S can facilitate knowledge management and decision making.In this article, introduction, definitions and background information of M&S are discussed.

Chronopharmacokinetics study of levofloxacin in rats

LI Xiao-tian, WANG Hong-juan, WANG Tian-kui, WANG Su-jun

2007, 12(1):  90-92. 

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AIM: To study the chronopharmacokinetics of levofloxacin in rats. METHODS: After levofloxacin was orally given to rats at different times, the concentrations of levofloxacin in plasma and urine were determined by HPLC and the pharmacokinetics parameters were calculated. RESULTS: The mean pharmacokinetic parameters of levofloxacin at 8:00, 16:00 and 24:00 were C_max 2.37, 2.02 and 2.85 mg/L;t_max 0.56, 0.50 and 0.62 h;AUC_0-∞ 11.23, 9.89 and 11.77 mg·h·L^-1;t_1/2 4.23, 3.51 and 4.46 h;CLs 0.39, 0.57 and 0.36 L·kg^-1·h^-1, respectively.The main pharmacokinetic parameters showed no significant difference by oral administration at 8:00, 16:00 and 24:00. CONCLUSION: There was no obvious change in circadian rhythms of levofloxacin in rats.

Pharmacokinetic study of rh-IFNα2a in mice and rats after intravenous and intramuscular administration

LU Li, CUI Ming-xia, WANG Li, ZHANG Bao-lai, WU Yong-jie

2007, 12(1):  93-97. 

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AIM: To study pharmacokinetic property of rh-IFNα2a after intravenous (i.v.) and intramuscular (i.m.) injection to mice and rats. METHODS: Double antibody sandwich ELISA analysis was used for testing drug concentration in serum, urine, bile and tissues after i.v.and i.m.administration of rh-IFNα2a in mice and rats.Pharmacokinetic parameters were calculated by DAS software.Immunohistochemistry technique was also adopted to evaluate its distribution characters. RESULTS: Pharmacokinetic model of rh-IFNα2a after i.v.and i.m. was consistent with two-compartment and one-compartment open model respectively, both submitting to first-order kinetic elimination.Rh-IFNα2a was predominantly distributed in kidney and lung tissue.The total drug accumulative excretion quantity in urine was 0.121 %of the administered after rh-IFNα2a 8.19 μg/kg i.v.into mice. The total drug accumulative excretion quantity in bile was 0.247 %of the administered after rh-IFNα2a 4.10 μg/kg i.v.into rats. CONCLUSION: Pharmacokinetic models after i.v.and i.m.rh-IFNα2a are two-compartment open model and one-compartment open model, respectively, both with first-order kinetic elimination.

Bioequivalence evaluation of secnidazole tablets in healthy male volunteers

SHI Shao-jun, LI Zhong-fang, WAN Yuan-sheng, CHEN Hua-ting, ZENG Fan-dian

2007, 12(1):  98-102. 

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AIM: To compare the bioavailability of the test and reference formulation of secnidazole (2 g) tablets under fasting conditions. METHODS: This bioequivalence study was carried out in 20 healthy male Chinese volunteers according to a single dose, two-sequence, crossover randomized design.Fifteen blood samples per period were collected over 96 h, and plasma secnidazole concentrations were determined by locally validated high performance liquid chromatography (HPLC) assay and pharmacokinetic parameters were analyzed by the noncompartmental and compartmental methods. RESULTS: Plasma concentration-time profiles were adequately described by a one-compartment open model with first-order absorption.The main pharmacokinetic parameters of secnidazole test and reference tablets were as follows:t_max were (2.30 ±1.06) and (2.28 ±1.10) h, C_max were (49.63 ±6.35) and (46.17 ±4.24) mg/L, t_1/2 were (28.84 ±3.41) and (29.05 ±4.01) h, AUC0-96 were (1832.06 ± 180.15) and (1847.14 ± 204.14) mg·h^-1·L^-1, respectively.The relative bioavailability of test tablets was (99.99 ±11.92) %. CONCLUSION: The results indicate that the two formulations of secnidazole tablets are bioequivalent in the rate and extent of absorption.

Tolerance of ulinastatin in healthy volunteers

WU Cheng-yi, XIAO Feng, GAN Lei, XU Qiang, YU Xiao-qi, SHI Li, ZHENG Qing-shan, SUN Rui-yuan, WEI wei

2007, 12(1):  103-106. 

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AIM: To evaluate the tolerance of healthy volunteers to ulinastatin (UTI) in different doses and confirm its safety dose in vivo. METHODS: 44 healthy volunteers were randomized into single rising dose groups (100, 200, 400, 600, 800, 1000, 1200 kU) and multiple rising dose groups (900 or 1200 kU, tid for 7 days). RESULTS: The maximal tolerance single-dose was 1200 kU, and the maximal tolerance multiple-dose was 900kU. CONCLUSION: UTI was safe at a dose from 100 to 1200 kU in a single administration or at a dose from 300 to 900 kU in multiple administration.

Effect of Metformin on patients with impaired glucose tolerance

CHEN Bi-lian, LIU Hui-xia, PAN Rui-zhe

2007, 12(1):  107-110. 

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AIM: To prospectively study the effect of Metformin and life style education on plasma glucose and the progression of intima-media thickness (IMT)of the common carotid in patients with impaired glucose tolerance (IGT). METHODS: Patients with IGT were randomizely divided into two groups (group A and group B).Patients in group A were educated by healthy life style and patients in group B took Metformin 250 mg three times daily associated with healthy life style education for one year.One year later patients of two groups were measured carotid IMT and oral glucose tolerance test again. RESULTS: At study entry there was no significant difference of plasma glucose and carotid IMT between the two groups.One year later postprandial plasma glucose in group B was significantly lower than that in group A (7.9±1.2 mmol/L vs 8.7 ±1.4 mmol/L, P =0.002)and the increasement of IMT in group B was significantly lower than that in group A (0.001 ±0.010 mm vs 0.006 ±0.014 mm, P =0.042). CONCLUSION: Metformin reduces postprandial plasma glucose and delays the progression of IMT of common carotid.

Feasible study on sacroiliac joint internal injection performed under Doppler guidance

JIANG Feng, MEI Yan, FEI Yi-li, SHAO Li-min, YAO Chen, SHAO Yong-liang, SHI Jia

2007, 12(1):  111-115. 

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AIM: To investigate and comparatively observe the feasibility, security and effectiveness of Doppler guidance for therapeutic intra-articular sacroiliac joint injections with compound betamethasone in patients with sacroiliitis (grades Ⅱ-Ⅲ). METHODS: 71 cases with sacroiliitis were randomized into 3 groups:24 in Doppler group (DP), 23 in CT group and 24 in control group.DP and CT group were injected with compound betamethasone (7 mg/mL) into sacroiliac joints in a different guided way and followed up for 90 days.We recorded the related indexes of DASDAI, BASMI and BASFI on 1st, 7th, 30th, 60th and 90th days before and after treatment, and simultaneously measured the finger tips distance, Patrick test “4” and the scores of VAS to sacroiliac joints press. RESULTS: There was statistical difference when DP and CT group were compared with control group (P<0.05) in the indexes of DASDAI, BASMI, BASFI, experiment like number “4” and sacroiliac joints press after 1st, 7th and 30th days' treatment. There was also statistical difference in the comparison of finger tips distance after 1st, 7th and 30th days' treatment (P<0.05).But there was no statistical difference when DP was compared with CT during the 90 days' follow- up.In 47 patients with percutaneous puncture, 2 of DP and 1 of CT failed, the failure rates were 8.3 % and 4.6 %, respectively (P ≥0.05).1 of CT and 1 of control group discontinued observation because of abnormal re-laboratory data.1 of DP, 1 of CT and 2 of control group failed to be followed up. CONCLUSION: This initial experience suggests that with a comparison to CT guidance Doppler-guided therapeutic injection with compound betamethasone to sacroiliac joints is safe, rapid, easy and suitable to be widely used in the lower-level hospital and poverty patients.

Effect of circadian variability of dipper blood pressure induced by valsartan in patients with non-dipper essential hypertension on levels of aldosterone

HU Qun-li, LIANG Qun, CAI Qi-yun

2007, 12(1):  116-118. 

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AIM: To investigate the circadian variability of the dipper blood pressure induced by valsartan in patients with non-dipper essential hypertension, and to observe levels of aldosterone. METHODS: The patients were divided into dipper and non-dipper groups.All patients were treated with valsartan (160 mg/d).The variability of circadian blood pressure were observed, and the levels of plasma aldosterone were monitored, too. RESULTS: After the treatment with valsartan, the systolic and diatolic blood pressure in all patients, either dipper or non-dipper groups, were evidently reduced, especially, the patient with non-dipper essential hypertension had more significant improvement.The circadian variability was appeared.The levels of aldosterone had a significant difference. CONCLUSION: Valsartan has significant effects for the patients with non-dipper essential hypertension.It can induce a circadian variability and recover the dipper blood pressure from non-dipper blood pressure.

Value of construetion of bypass circuit outflow tract in femoral-popliteal arterial grafting operation

HU Ji-qiong, WANG Dao-ming, SI Chun-qiang, XUE Qing-quan

2007, 12(1):  119-120. 

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AIM: To summarize the effect of femoral popliteal arterial graft operation and the influence of construction of bypass circuit outflow tract. METHODS: A retrospective study was performed in 15 cases of femoral popliteal arterial bypass. RESULTS: A femoral popliteal embolism occurred in one patient undergoing simple femoral-popliteal arterial bypass in the early postoperative period and in 2 patients in the long-term followed up.However, the effects of constructing bypass circuit in the same time were very well, and only one patient had chill on the limbs. CONCLUSION: The operative results are better when the construction of bypass circuit is performed in the femoral-popliteal arterial graft operation, further more, a new method is provided for construction of distal end outflow tract.