Archive

• 01 May 2007 Volume 26 Issue 5

    

  ---

  特约稿
  药物研究
  儿科用药专栏
  药物与临床
  药物制剂
  药品质量控制
  用药指南
  

• Select all
  |

特约稿
• Select
  特约稿

  Discussion on Clinical Dosage Form Factors and Drug Rational Use in Hospital

  DING Yufeng

  2007, 26(5): 447-450.

  Download PDF ( )   Knowledge map   Save

  ABSTRACTObjectiveIn terms of the definition of dosage form in pharmaceutics and biopharmaceutics，probing into the related factors affecting drug rational use，a new mode of influencing factors about drug rational use is introduced and the concept of clinical dosage form factors is proposed. The definition, the studied aspects, the clinical technical demand, the impact on the rational drug use and the role in the rational drug use of clinical dosage form factors are discussed in detail. It should be highly considered on clinical dosage form factors in hospital, and the related studies on clinical dosage form factors and drug rational use should be focused, the informationgathering and informationservice should be strengthened，so as to widen the pharmacy service area, improve the quality of pharmacy service in hospital and facilitate the clinical rational drug use.
药物研究
• Select
  药物研究

  Optimum Technology for Synthesizing Dexamethasone Hemisuccinate by Orthogonal Test

  LIU Xinyou;ZHOU Siyuan;MEI Qibing;CHENG Jianfeng;ZHANG Yan

  2007, 26(5): 451-453.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo explore the synthetic technology of dexamethasone hemisuccinate (DSH) by orthogonal test.MethodsDSH was synthesized with dexamethasone and succinic anhydride, using 4Dimethylaminopyridine (4DMAP) as catalyst. The synthetic technology was optimized by orthogonal test with two factors and three levels, with the yield of DSH being the criteria . The factors were the molar ratio between succinic anhydride and dexamethasone and the molar ratio between 4DMAP and dexamethasone.ResultsThe molar ratio between 4DMAP and dexamethasone was the main factor affecting the yield of DSH and the molar ratio between succinic anhydride and DSH was the minor one. The optimum molar ratio among dexamethasone, succinic anhydrate and 4DMAP was 1.0：2.0：0.5. The yield of DSH from optimum technology was 97.72%. HNMR and IR results showed that the obtained product was what we wanted and its purity was above 99.0%. ConclusionThe optimum technology for synthesizing DSH raised the yield of DSH in large scale and the technology was stable and easy to control

• Select
  药物研究

  Downregulation of 5-lipoxygenase Expression in Pancreatic Cancer Cell by Triptolide

  WU Shenbao;ZHOU Guoxiong;ZHANG Hong;HUANG Jiefei;MA Pengcheng;E Qun;WEI Qun;DING Xiaoling

  2007, 26(5): 454-457.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the effect of Triptolide on 5lipoxygenase(5LOX) expression and apoptosis of human pancreatic cancer cell. MethodsThe immunocytochemical staining and RTPCR were employed to detect the expression of 5LOX in the pancreatic cell line SW1990. The apoptotic index of SW1990 was determined by flow cytometry (FCM) .ResultsThe pancreatic cell line SW1990 expressed 5LOX, but the normal pancreatic cells did not. TL inhibited 5LOX expression and promoted SW1990 cell apoptosis in a dose dependent manner (P＜0.01). The cell apoptosis was correlated to the expression of 5LOX (P＜0.01). ConclusionTL is able to inhibit 5LOX expression and facilitate the cell apoptosis in pancreatic cancer cell line SW1990.
• Select
  药物研究

  Effect of Arsenic Tioxide on MRP Expression in A549/R Cell Line of Human Lung Cancer

  CHENG Jing;FENG Jueping;WANG Yaping;LI Min;KONG Qingzhi

  2007, 26(5): 457-460.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the effect of arsenic trioxide (As2O3) on the reversal role of drug resistance and the expression of MRP in human lung cancer cell line A549/R . MethodsThe comcentration of intracellular ADM was detected by fluorescence spectrofluorometry. The expression of MRP gene was assessed in As2O3treated A549/R cells by semiquantitative RTPCR. ResultsAs2O3 in noncytotoxic dose could significantly increase the intracellular accumulation of ADM in A549/R cell line and derease the medium inhibition concentration (IC50). The overexpression of MRP mRNA was observed in A549/R cell line and this was significantly suppressed in As2O3treated A549/R cells. ConclusionAs2O3 can partically reverse the resistance to ADM in A549/R cell line and this effect may be related to the variation of MRP gene expression.
• Select
  药物研究

  Construction of Immortalized Precartilaginous Stem Cells from Neonate Rats by Transfection with Simian Virus 40 T Antigene Gene

  HU Weihua;GUO Fengjing;ZHANG Shuwei;CHEN Anmin;DING Ran

  2007, 26(5): 460-464.

  Download PDF ( )   Knowledge map   Save

  Objective To establish immortalized precartilaginous stem cells(PSCs) from neonatal SD rats in vitro for the further related research on the differentiation mechanism and clinic application of precartilaginous stem cells. MethodsBy using LipofectamineTM2000, a gene transfection reagent, plasmid pCMVSV40T/PUR containing the simian virus 40 large T antigene gene(SV40Tag) was transfected into the primary cultured PSCs isolated by immuniomagnetic beads coasted with the second antibody. Colonies were isolated by puromycin selection and expanded by many passages. Investigate the capability of differentiation of the transfected cells. The expression of SV40Tag in expanded cell lines was identified by immunocytochemistry method and RT-PCR. ResultsA particular anti-puromycin cell clone was acquired, which was confirmed as fibroblast growth factor receptor3(FGFR3) positive PSCs. The total RNA were isolated from the positive cell clones, and a 588 bp fragment, which was specific for the SV40T antigene gene, was amplified. The transfected cells were expanded to immortalized cell strain, named as immortalized precartilaginous stem cells(IPSCs). The population doubling time of IPSCs was （22.98±2.77） h, no significant effect of subculture, freezing and recovering had been found. ConclusionPrecartilaginous stem cells could be isolated from neonatal SD rats, cultured in vitro, and immortalized through the transfection of pCMVSV40T/PUR.
• Select
  药物研究

  Purification of Fructus Gardeniae Gardenside by Ultrafiltration Membrane Technology

  RAO Shuangchao;SHI Zhaohua;HUANG Zhijun;YUAN Ming;ZHANG Qiongguang;WU Muqin;XIONG Dengke

  2007, 26(5): 464-466.

  Download PDF ( )   Knowledge map   Save

  ObjectiveAIM To explore the possibility for application of ultrafiltration membrane technology to purify Fructus Gardeniae Gardenside. MethodsChoose orthogonal experiment design to optimize the technology, evaluated by the average flux through membrane, pecentage of Gardenside through membrane and percentage of Gardenside in dissoluble solid materials. Four main factors were chosed, such as liquid content(A),Operate Pressure(B),Liquid Temprature(C),Liquid Flow(D).ResultsThe outcome was the best when the optimization terms matched A2B1C3D3(liquid content: 0.12 g·mL-1，Operate Pressure :0.15 MPa，Liquid Temprature: 40 ℃，Liquid Flow :15 mL·min-1).ConclusionThe technology of ultrafiltration membrane to purify Fructus Gardeniae Gardenside is simple and reliable with good purifying effect.
• Select
  药物研究

  Orthogonal Test Optimizing the Method of Extracting Polysaccharide from Dendranthema Mrifolium Tzvel. with Water and Ethanol

  MA Li;CHEN Wen;ZHANG Songan;ZHENG Ni;ZHANG Yu;CHEN Dongsheng;CHEN Huating

  2007, 26(5): 467-468.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the optimal method of extracting polysaccharide from Dendranthema mrifoliumTzvel. Et Zhao with Water and Ethanol. MethodsThe factors affecting polysaccharide extration were studied by Orthogonal test, and the relative percentage content of polysaccharide was determined with sulfuric acidphenol method.ResultsThe optimal method of extracting the polysaccharide was as follow: water dunking time 2 h, temperature of water 100 ℃, extracting with chloroform once, concentration of alcohol 80%.ConclusionThis method is the optimal route for extracting the polysaccharide. This work provided a basis for its further study.
• Select
  药物研究

  Effect of Melatonin on Myocardial Protection and MEK/ERK Signaling Pathway in Rats after Hemorrhagic Shock

  ZHOU Wenfeng;MING Zhangyin;XIANG Jizhou

  2007, 26(5): 469-472.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the effect and the underlying mechanism of melatonin on myocardial protection in rats after hemorrhagic shock .Methods40 healthy rats were randomlized into 4 groups. The rat model of hemorrhagic shock was established by bleeding from femoral artery. Then the rats were injected through the external carotic vein with 2 mg·kg-1 MT in MTtreated group, 0.9% sodium chloride containing 0.5% ethanol (10 mg·kg^-1) in the control group and nothing in shock model group. The rats in shamopertated group received simple vasular dissection. The contents of TNFα and ICAM1 were studied by ELISA. ERK activity was measured by immunoprecipitation; pERK1/2 and pMEK1/2 expressions were assessed by Western blot. ResultsMelatonin can inhibit the increases of TNFα and ICAM1 in myocardium after hemorrhagic shock. What’s more, the intracellular ERK activity, pERK1/2 and pMEK1/2 expressions were decreased by melatonin. ConclusionMelatonin has protective effect on myocardium after hemorrhagic shock, the mechanism was related with downregulation of MEK/ERK signaling pathway.
• Select
  药物研究

  Prevention of Cyclosporine A （CSA）-induced Chronic Nephrotoxicity with Curcumin in Rats

  FU Yanhong;WU Yonghong;LIU Shenwei

  2007, 26(5): 472-477.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo evaluate the effect of curcumin on cyclosporine A(CSA)induced nephrotoxicity. Methods30 rats were randomized into 4 groups, which included model group, curcumin-treated group and curcumin-prevented group with 8 rats in each, as well as control group with 6 rats. The rat stomach was perfused by olive oil 30 mg·kg-1·d-1 for 4 weeks in control group, CSA 30 mg·kg-1·d-1 for 4 weeks in model group, CSA 30 mg·kg-1·d-1 for 2 weeks followed by curcumin 200 mg·kg-1·d-1 for another 2 weeks in curcumin-treated group, and CSA 30 mg·kg-1·d-1 combined with curcumin 200 mg·kg-1·d-1 for 4 weeks in curcumin-prevented group. The weight before and after CSA medication, the urinary volume［mL·（24 h）-1), serum cretinine, BUN and renal pathological changes after CSA application were recorded. The expression of HO-1and bFGF in rat kidney was examined by immunohisochemistry and RT-PCR. Results In comparison with control group，the results in rat model were as follows: the weight was decreased（P＜0.05）, urinary volume was increased（P＜0.05），BUN and CR were elevated（P＜0.05）. Renal pathological study displayed the typical changes of CSA nephrotoxicity. The expression of HO1 were decreased obviously（P＜0.01）and the expression of bFGF was increased（P＜0.01）. In comparison with model group, HO1 expression was increased （P＜0.01）but bFGF expression was decreased （P＜0.01）in curcumintreated andprevented groups. ConclusionCurcumin could counteract CSAinduced nephrotoxicity, probably through upregulation of HO1 expression and down-regulation of bFGF expression in the kidney.
• Select
  药物研究

  Effect of Panax Nologinoside on VEGF and BMP in Rats with Diabetic Nephropathy

  SHI Yan;TU Qingnian

  2007, 26(5): 477-480.

  Download PDF ( )   Knowledge map   Save

  Objective To explore the protective mechanism of Panax Nologinoside ( PNS) on kidneys in diabetic rats by investigating the effect of PNS on VEGF and BMP7 in rats with diabetic nephropathy.Methods50 male Wistar rats were randomized into 5 groups, which included normal group (N group), diabetes model group (DM group), low dose PNStreated group (PNSL group), high dose PNStreated group (PNSH group) and captopriltreated group (C group). Type 1 Diabetes rat model was established by injection of streptozotocin. The rat stomach was perfused with tap water, tap water, PNS 100 mg· kg·d1, PNS 200 mg·kg·d1 or captopril 50 mg· kg·d1 in Group N, DM, PNSL, PNSH or C, respectively. Four weeks later the fasting blood glucose (FBG), 24 h microalbuminuria , VEGF and BMP7 level in kidney were examined in each group.ResultsFBG, 24 h microalbuminuria and VEGF expression were markedly increased, but BMP7 expression was greatly decreased in DM model group. All the parameters observed except overexpression of BMP7 were significantly reduced in PNSH group.ConclusionPNS exerted protective effect on diabetic nephropathy probably via reduction of VEGF and elevation of BMP7.
• Select
  药物研究

  Bioequivalence Evaluation of Domestic Cefalexin Tablets Compared with the Same US Product in Chinese Healthy Volunteers

  WU Jianhong;YANG Yuanrong;CUI Jin;LI Huarong;GAO Fengxi;HU Gang;HUANG Lingsheng;ZENG Fandian

  2007, 26(5): 480-483.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo study the relative bioavailability in Chinese healthy volunteers of the test cefalexin tablets (QINGYUAN HUANENG PHARMACEUTICAL CO., LTD.CHINA ) compared with the reference cefalexin tablets (Teva Pharmaceutical Industries Ltd) and to evaluate the bioequivalence of these two products. MethodsThe bioequivalence of two products of cefalexin tablet 500 mg was demonstrated in 20 Chinese healthy male volunteers after a single oral administration in a randomized, twotreatment, twoperiod crossover design with a 1 week washout period. The HPLC method was applied for the measurement of cefalexin in plasma samples. ResultsAfter oral administration, the major pharmacokinetic parameters of two products were calculated from the plasma cefalexin concentration time profile. For test and reference products , the time to reach maximum concentration (tmax) was（0.95±0.40）and （0.99±0.33） h, the peak concentration (Cmax) was （19.53±5.20）and （19.03±4.39） g·mL^-1, the half life (t1/2) was （1.03±0.17） and （1.00±0.20） h, the area under the curve to the last measurable concentration (AUC0→6 h) was （33.26±6.60）and （33.39±6.39） μg·h·mL^-1, the area under the curve to infinity (AUC0→∞) was （34.05±6.83）and （34.21±6.86） μg·h·mL1,respectively. The result from comparison of AUC0→6 h of two products indicated the relative bioavailability of test product was （99.8±8.0） % . The 90% confidence interval (90% CI)of AUC0→6 h and AUC0→∞of test product were 96.4 %102.6 % and 96.5% 102.6% , 90% CI of Cmax was 94.6%109.4%. The nonparametric test of Wilcoxon signed rank test on tmax shown no significant difference (P＞0.05) between the cefalexin test and reference tablets.ConclusionBased on these statistical inference and the bioequivalence criteria , it is concluded that the domestic cefalexin tablet and TEVA cefalexin tablet are bioequivalent, and that the two formulations should be considered equally effective and safe in medical practice.
儿科用药专栏
• Select
  儿科用药专栏

  Effect of Allitridin on the Expression of Caspase-3 in Human Embryo Lung Fibroblast Cells Infected by Human Cytomegalovirus

  SUN Taotao;FANG Feng;ZHEN Hong;SHU Sainan;LIU Jin;ZHOU Yufeng;LI Ge

  2007, 26(5): 493-496.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the effect of allitridin on the expression of caspase3 in human embryo lung fibroblast cells (HELs) infected by human cytomegalovirus (HCMV), in order to explore the partial mechanism of allitridin against HCMV from the view of apoptosis.MethodsHELs were infected by HCMV AD169 strain with high multiply of infection (MOI=2.5) and low MOI (0.25), respectively. According to the maximum tolerance concentration (MTC) of allitridin to HELs (9.6 μg·mL-1), 9, 6 and 3 μg·mL-1 were determined as the high, medium and low dosage of the drug. The level of caspase3 protein in each group was analyzed by using western blot assay at 72 h after viral infection and/or drug treatment. ResultsThe normal HELs only expressed caspase3 P32. Whereas, the expression of caspase3 P32 increased after HCMV infection. Moreover, active fragment of P17 of caspase3 appeared, and the expression of P17 in high MOI group was obviously stronger than that in low MOI group. Compared with infected controls, the active fragment of P17 was upregulated in low MOI HELs treated with allitridin, and the ratio of P17 versus P32 also significantly increased. On the contrary the active fragment of P17 was downregulated in high MOI HELs treated with drug, and the ratio of P17 versus P32 decreased as well. ConclusionHCMV infection could induce the apoptosis of HELs, and this effect was more intense in high MOI group than that in low MOI. Allitridin could upregulate the apoptosis of low MOI HELs, while downregulate that of high MOI cells, supposing that the former was inclined to eliminate the virus from the infected cells, and the latter might protect the cells from injury caused by excess cellular apoptosis. This suggests the regulation of allitridin on HCMVinfected cells was the dual effect.
• Select
  儿科用药专栏

  Population Pharmacokinetics of Phenobarbital in Epileptic Children

  WANG Gang;LIU Bin;LIANG Jingfen

  2007, 26(5): 496-500.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo investigate the population pharmacokinetics（PPK）of phenobarbital (PB) in epileptic children. MethodsThe data from 298 epileptic children who took phenobarbital were collected. The PPK parameters were estimatied by CPKDP program with Ｂayesian’s feedback and Iterative two stage method. ResultsThe main parameters of the PPK including Ke,Vm, and CL were 0.351 h1、0.452 L·kg1 and 5.135 L·h1·kg1, respectively, in phenobarbital alone group. They were not influenced by the children’s sex, stature, adjuvant drug administration or drugtaking duration. The epileptic children’s age, body weight, and combination of vaproic sodium(VPA), phenytion（PHT）, clonazepam（CNP）, topiramate(TPM), carbamazepine (CBZ) were all important determinants of the clearance(CL) of PB, which was increased when combination of VPA,CBZ and PHT and decreased when combination of CNP and TPM. Conclusion Based on the PPK model in the epileptic children and referring to the children’s age, body weight, drug dosage and drug combination, the CL of PB was estimated and the in vivo concentration of PB was predicted to direct the indivilized drug administration.
药物与临床
• Select
  药物与临床

  宗刚军,吴刚勇,赵秋良,夏阳,张丽,陈满清,陈景开

  2007, 26(5): 513-514.

  Download PDF ( )   Knowledge map   Save
药物制剂
• Select
  药物制剂

  Improvement in Dissolution Properties of piroxicam by Complexation with βCyclodextrin and PVP

  HU Pengyi;YI Yimu

  2007, 26(5): 530-532.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo study the dissolution of Piroxicam by complexation with β-cyclodextrin and PVP. Methods The sample was prepared by PVP solid dispersion or β-CD complexation and characterized by differential scanning calorimetry. Dissolution of finished products produced with different technology was determined by UV spectrophotometry.ResultsThe result of differential scanning calorimetry indicated that in βCD complexation and piroxicamPVP (1：6，1：8) solid dispersion piroxicam existed as an amorphous form and in piroxicamPVP (1：2，1：4) solid dispersion , Piroxicam was finely crystalline. The dissolution rate of β-CD complexation and solid dispersion with the drugcarrier ratio 1：6 and 1：8 was markedly increased in comparison with that of the physical mixture and piroxicam substance (P<0.01). ConclusionBoth solid dispersion and β-CD complexation can significantly increase the dissolution rate of piroxicam.
• Select
  药物制剂

  Preparation and Quality Control of Yupingfeng Granules

  WANG Zhichao;DU Rong;LIU Zuxiong;QIN Bei

  2007, 26(5): 533-535.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo prepare yupingfeng granules and set up the quality control technology. MethodsTo extract volatile oil from medical material containing volatile oil by distillation method or from other medical material by boil with water method. And thin layer chromatography was used to identify the medical material. And HPLC was used to determine content of astragaloside Ⅳ. ResultsThe calibration curves for astragaloside Ⅳwere liner within the rang of 10.4～166.4 μg·mL-1; the average recovery rate was 100.3%，RSD=0.45%(n=5). ConclusionThe preparation method is easy to do and quality control method is feasible. It can be used for the quality control of the drug.
药品质量控制
• Select
  药品质量控制

  Determination of the Content of Paeoniflorin in Jiangchi Gel by HPLC

  ZHENG Jing;FANG Shiping;SUN Manchun;WANG Zhiyong

  2007, 26(5): 540-541.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo establish a method for determinating paeoniflorin in jiangchi gel by HPLC. MethodsThe chromatographic conditions were as follows: CLCODS column（5 μm，150 mm×60 mm）used as the stationary phase, and methanolwater (45：55) as mobile phase with a flow rate of 1.0 mL·min1,and the detecting wavelength 230 nm. ResultsA good linearity was obtained within the range of 0.08～0.80 μg·mL-1 of paeoniflorin (r＝0.999 6). The average recovery rate of paeoniflorin was 100.61%(n=6,RSD=0.89%). ConclusionThis method is simple, rapid and accurate which can be used to determine paeoniflorin contents in jiangchi gel.
• Select
  药品质量控制

  Comparison of Schisandrin Contents of Frucuts Schisandrae from Different Origins

  MA Xinfei;YIN Fangzhou;WANG Yunfeng;LI Lin;LU Tulin

  2007, 26(5): 542-543.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo compare the schisandrin contents of Frucuts schisandrae from different Origins. MethodsThe content of schisandrin was determined by HPLC, Lichrospher5C18(4.6 mm×250 mm，5 μm) column in an oven at 30 ℃ with the mobile phase MeOHH2O(6：4) and VWD Dector at 250 nm. ResultsThe content of schisandrin in all samples of Frucuts schisandrae Chinensis were above 0.4%.ConclusionThis method has the advantage of convenience, accuracy and reproducibility.
用药指南
• Select
  用药指南

  Pharmacoeconomic Analysis on Three Different Regimens as Neoadjuvant Chemotherapy for Breast Cancer

  DAI Zhijun;WANG Xijing;WU Wenying;LIU Xiaoxu;JI Zongzheng;KANG Huafeng;XUE Fengjie;XUE Xinghuan

  2007, 26(5): 555-558.

  Download PDF ( )   Knowledge map   Save

  ObjectiveTo evaluate the economical effects of three different regimens as neoadjuvant chemotherapy for local advanced breast cancer. MethodsThe costeffectiveness method in pharmacoeconomics was adopted in the retrospective analysis of three different regimens: CEF、NEF and TAC. (C stands for CTX, E for Epirubicin, F for Fluorouracil, N for Vinorelbine, T for Taxotere). ResultsThe average cost of CEF、NEF、TAC regimens was 5 620. 3，8 133. 7，14 527. 6 yuan, respectively. For primary tumor in the breast , the overall response rate (RR) in three groups was 47.2 %(17/36) ，71.9 %(23/32) and 85.7 % (18/ 21), respectively. Further increase of 1% effective rate requires additional cost of 119.07，113.13，169.52 yuan, respectively. Compared with CEF regimen with the lowest cost, the additional cost for further increase of 1% effective rate was the lowest as 101.76 yuan for NEF regimen. NEF regimen was still the cheapest for achieving the same effect even when the drug fee dropped for 10%. ConclusionNEF regimen is the optimal scheme as neoadjuvant chemotherapy for local advanced breast cancer.