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    药物研究
  • 药物研究
    LIU Yan;WANG Haixia;HUANG Lijun;ZHANG Yifei;XU Jing;TIAN Wei
    ABSTRACTObjectiveTo investigate the influence of traditional Chinese medicine preparations on rat liver CYP3A4 activity in vitro.MethodsThe rat liver microsomes were prepared from rat livers. The reaction time,protein content and midazolam concentration in the microsomal incubation was optimalized respectively; the metabolism of midazolam and activity were measured by HPLCMSMS;IC50 and Ki of ketoconazole, xuezhikang,tongxinluo and zaoren ansheng capsule in microsomal incubated system were determined after incubation with the midazolam(CYP3A4). ResultsThe optimum protein content of rat liver microsomes for kinetic analysis was 0.4 g•L1 with 4 μmol•L1 midazolam at 37 ℃ for incubation up to 5 min.The IC50 of ketoconazole, xuezhikang and tongxinluo was (3.4±0.2),(25.1±0.3),(56.2±0.3) mg•L1,respectively,but the IC50 of zaoren ansheng capsule was greater than 150 mg•L1;The Ki of ketoconazole, xuezhikang and tongxinluo was (1.7±0.1),(25.0±0.2),(50.0±0.3) mg•L1,respectively. ConclusionThe model of liver microsomes for evaluation of the influence of traditional Chinese medicine preparations on CYP3A4 activity is established. xuezhikang and tongxinluo have weak inhibitory effect on rat CYP3A4 in vitro.
  • 药物研究
    LIU Xinyun;GAN Chunying;YANG Jinxia;DI Wei;CHEN Lan
    ABSTRACTObjectiveTo study the cutaneous absorption enhancement of Ntrimethyl chitosan(TMC60) on ganciclovir gel. Methods The ganciclovir gel with 1% TMC60 as absorption enhancer was prepared. The enhancement of TMC60 was studied by using Franz diffusion cells in vitro and stability penetration rate[J, μg•(cm2)1•h1] as indicator, in comparison to the same concentration of azone and chitosan(CS). ResultsJ values of ganciclovir gels without or with azone, TMC60 and CS as enhancer was 3.822 1, 4.098 4, 4.205 5 and 4.356 9 μg•(cm2)1•h1, respectively. Compared with the blank group, TMC60 significantly enhanced transdermal permeation of ganciclovir(P<0.05). While no significant difference was found compared with azone and CS(P>0.05). ConclusionTMC60 could enhance cutaneous absorption of ganciclovir.
  • 药物研究
    WANG Yanyan;ZHANG Jinwen;GUO Jieru;TANG Fei;ZHANG Xiaoqiong;ZHANG Yonghui;
    ABSTRACTObjectiveTo study effects of different extracts from Roots of Uraria crinita on kidneyYANG deficiency mice induced by hydrocortisone.MethodsKidneyYANG deficiency mice were induced by hydrocortisone,effects of different extracts from roots of Uraria crinita were observed by observing physical signs,measuring antioxidative stress ability and reproductive organ weights.ResultsTotal ointment,acetic ether extract and nbutanol extract significantly enhanced appetite,increased body weight,promoted growth and development,raised spleen and thymic weight index,prominently alleviated reproductive organs’ atrophy,obviously eliminated fatigue,and enhanced antioxidative stress ability of mice.ConclusionRoots of Uraria crinita can improve the life quality of KidneyYANG deficiency mice,the acetic ether extract and nbutanol extract are the major active extracts on kidneyYANG deficiency.
  • 药物研究
    LIU Mei;WANG Qingwei;LIU Xueying;SUN Yangyang;HUI Guangfei;CUI Qianbin;LI Hui
    ABSTRACTObjectiveTo study the transdermal characteristics of star anise oil and its percutaneous penetration enhancement for ibuprofen. MethodsTo establish a method for determination of ibuprofen and anethole, the major constituent of star anise oil by HPLC. Fetal skin was used as permeation barrier in vitro. The transdermal properties of the star anise oil and its effect on percutaneous penetration of ibuprofen were investigated by using Franz diffusion cells. ResultsThe permeability coefficients of star anise oil at 0.5%, 1.0%, 2.0% were (1.675 ± 0.331),(4.048 ± 0.579),(5.352 ± 0.166) μg•(cm2)-1•h1, respectively. The permeability coefficients of ibuprofen with star anise oil at 0.0%, 0.5%, 1.0%, 2.0% were (9.416±1.260),(7.803±1.128),(9.495±0.749),(7.334 ± 0.885) μg•(cm2)-1•h1, respectively. ConclusionsStar anise oil and ibuprofen could well penetrate through fetal skin in a dose dependent manner. Star anise oil does not show transdermal enhancing effects, while inhibits the percutaneous absorption of ibuprofen in vitro.
  • 药物研究
    XU Shali;LI Zhongming;LI Hani;XUE Cunkuan
    ABSTRACTObjectiveTo explore the effects of valerian extracts on bile acid metabolism and liver damage caused by high cholesterol  high sugar high fat diet. Methods①24 white rabbits with big ears were randomly divided into 3 groups(n=8 each). The rabbits were fed with high cholesterol  high fat  high sugar diet except those in the normal group with pellet feed. The treatment group was intragastrically given with valeriana extracts 30 mg•kg1 daily. The serum pyruvate aminotransferase(ALT), serum total cholesterol(TC), total bile acid(TBA) content, bile flow and TC phospholipids TBA content, gallstone formation, liver histological test and aortic plaquelike porridge were analyzed later. ②24 Wistar rats were randomly divided into 3 groups(n= 8), which were fed with high cholesterol  high fat  high sugar diet, except for those in the normal group with basal diet. The treatment group were fed with valerianaextracts 50 mg•kg1 daily, the control group was given with the equal volume of 0.9% sodium chloride solution. The serum TC, TBA and liver histology were observed. Results①Compared with the control group, common bile duct flow and solids content were increased significantly(P<0.01) in the treatment group, TBA concentration in bile was elevated obviously(P<0.05), serum TBA was predominantly lower(P<0.05), gallstone formation was significantly less(P<0.05), liver injury was significantly alleviated. ②The serum TBA in rats was dropped(P<0.05) in the treatment group compared with that in the control, and the liver injury was attenuated. ConclusionValeriana extracts could increase the TBA content of bile, improve TBA/TC stone formation, lower the serum TBA concentration and significantly reduce the liver injury.
  • 药物研究
    HAN Yan;WANG Qingwei;ZHANG Yan;LIU Xinyou;QIN Hua;DU Xiaoyan
    ABSTRACTObjectiveTo study the antibacterial effects of eugenol and essential oil from Eugenia Caryophyllata against helicobacter pylori in vitro.MethodsThe essential oil was obtained by steam distillation. The concentration of eugenol was determined by HPLC. MIC against helicobacter pylori of eugenol, essential oil from Eugenia Caryophyllata and aqueous extract of Eugenia Caryophyllata except essential oil were determined in vitro with ampicillin as a control drug. ResultsThe range of MIC against 8 helicobacter pylori was 1.25-2.50 μg•mL1 for ampicillin, 5.00-10.00 μg•mL1 for the essential oil, 2.50-5.00 μg•mL1 for eugenol. The aqueous extract showed no inhibitory effect against helicobacter pylori. ConclusionThe main active component from Eugenia Caryophyllata against H. pylori is eugenol of essential oil.
  • 呼吸系统疾病用药专栏
  • 呼吸系统疾病用药专栏
    XU Xilin;MAO Mei;XIONG Shengdao;FU Zuhong
    ABSTRACTObjectiveTo investigate the clinical characteristics and drug resistance of Pseudomonas aeruginosa pulmonary infection and provide guidance for clinical use. Methods124 cases of pulmonary infection caused by Pseudomonas aeruginosa were reviewed and the susceptibility to Pseudomonas aeruginosa was detected with KirbyBauer method. ResultsThe patients with humoral immune and respectory defense dysfuction were susceptible to Pseudomonas aeruginosa attacking. It was showed that the Pseudomonas aeruginosa sensitive drugs were tazobactampiperacillin, cefepime,amikacin,imipenem, cefoperazonesulbactam and ceftazidime, Pseudomonas aeruginosa resistence drugs were cefotaxime, cefoperazone, and piperacillin. ConclusionThe clinical susceptibities to Pseudomonas aeruginosa should try to be avoided and antibiotics for therapy ought to be rationally selected by drug sencitive tests.
  • 呼吸系统疾病用药专栏
    WANG Zeng;WENG Lin;YOU Jun;CHENG Bin
    ABSTRACTObjectiveTo investigate the changes of serum levels of tumor markers during chemotherapy of single pemetrexed or combination with platinum in patients with advanced nonsmall cell lung cancer(NSCLC). Methods102 advanced NSCLC patients who experienced more than 2 cycles of chemotherapy by pemetrexed single agent or combination with platinum were retrospective analyzed. The changes of CEA, CA125, CYFRA211, NSE, SCC and changes of chest CT scan were recorded before and after chemotherapy. ResultsAfter chemotherapy, tumor markers like CEA, CA125, CYFRA211, NSE and SCC were decreased, in which CEA, CA125 and CYFRA211 diminished 19.3%(P<0.05), 24.8%(P<0.05), and 18.5%(P<0.05), respectively. It was suggested that the correlation between tumor marker response (TMR)and imagingbased response (IBR) of CEA and CA125 was positive; the correlation between TMR and IBR of CYFRA211 was also positive; that between TMR and IBR of CEA, CA125 and CA199 joint inspection was positive as well. ConclusionSerum CEA, CA125 and CYFRA211 represent reliable markers for chemotherapy efficacy on patients with advanced NSCLC. Monitoring changes of serum levels of tumor markers would benefit for assessment of chemotherapy efficacy, which is simple, economic and useful in clinical settings.
  • 呼吸系统疾病用药专栏
    LUO Hong
    ABSTRACTObjectiveTo evaluate the effecacy and safety of varenicline on smoking cessation intervention for patients with chronic obstructive pulmonary disease(COPD).Methods50 nicotinedependent patients with COPD were divided into therapeutic and control groups.In a randomized, doubleblind, placebocontrolled study, patients in the therapeutic group received varenicline 0.5~2.0 mg•d1.Patients were followed up for 12 weeks after treatment.ResultsWeek 9-12 CAR was significantly higher for varenicline(13) versus placebo(8); CARs through 12 weeks posttreatment(weeks 9-24) were 8 with varenicline and 5 with placebo.The 7day PP was 14 with varenicline versus 8 with placebo at week 12, and 9 versus 6 with placebo at week 24.Reports of depression, depressed mood, and depressive symptoms were similar for both treatment groups.ConclusionVarenicline is an efficacious and well tolerated pharmacologic treatment for smoking cessation among patients with mild moderate COPD.
  • 药物与临床
  • 药物与临床
    MA Yongchun;WANG Heqiu;JIN Weidong;WANG Naixin
    ABSTRACTObjectiveTo assess the efficacy and safety of oxcarbazepine and lithium carbonate for treating manic episode. Methods70 patients with manic episode were randomly divided into oxcarbazepine group(n=34) and lithium carbonate group(n=36). The patients in oxcarbazepine group were treated with 0.6-1. 8 g•d1 oxcarbazepine, and those in lithium carbonate group were treated with 0.5-1.5 g•d 1 lithium carbonate, on the base of atypical antipsychotics therapy. All patients were assessed by BeckRafaelsen manic scale(BRMS) for 6 weeks. ResultsBRMS in two groups significantly decreased after treatment for 6 weeks(P<0.01). BRMS of oxcarbazepine group was significantly lower than that of lithium carbonate group at the end of 1st and 2nd week after treatment(P<0.05). The efficacy rate of oxcarbazepine group and full remission rate after treatment were significantly higher than those in the lithium carbonate group(P<0.05). Similar side effects was found between two groups(P>0.05). ConclusionCombination of oxcarbazepine and atypical antipsychotics are more effective than lithium carbonate and safe.
  • 药物与临床
    HU Anyi;LIU Li
    ABSTRACTObjectiveTo study the effect of danhong injection on vascular endothelial function related factors and inflammation factors in patients with unstable angina pectoris(UAP). Methods72 patients with UAP were randomly divided into two groups:treatment group(n=36) and control group(n=36). The control group was given with the conventional therapy, and treatment group was treated with intravenous drip of danhong injection(30 mL danhong injection added into 250 mL 0.9% sodium chloride solution,once a day) for 2 weeks besides the conventional therapy. The level of serum ET1, NO, hsCRP, Fg and TNFα were tested before and after treatment. ResultsThe serum ET1, hsCRP, Fg and TNFα levels in the treatment group were obviously lower than those in the control group(P<0.05), and the level of NO was significantly increased compared with that in the control(P<0.05). ConclusionDanhong injection decreases the level of serum ET1, hsCRP, Fg and TNFα and elevate serum NO, which inhibiting inflammation factors expression and improving the endothelial function of the patients with UAP.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    CHEN Yujie;PI Zhenping;LIU Xinqiao;WAN Dingrong
    ABSTRACTObjectiveTo establish a method to purify and enrich total flavonoids from two Genus Sedum plant drugs(Sedum. sarmentosum Migo. and S. lineare Thunb.) .MethodsThe plant extraction was loaded on the top of macroporous resin column, enriched by ethanol elution, and then loaded on polyamide column and enriched again by ethanol. ResultsThe enriched flavonoids products from Sedum sarmentosum Bunge. and S. lineare Thunb. were remarkably raised by this combining techniques of macroporous resin and polyamide, which were 68.9% and 54.0%, respectively. ConclusionThe method worked well in enriching total flavonoids from two sedum plant drugs.
  • 药物制剂与药品质量控制
    SUN Xuehui;SHI Guobing;HE Jing;ZHAO Minghong;Li Wentao;
    ABSTRACTObjectiveTo establish a determination method for Ginsenoside Rg1 in shenqi wuwei chewable tablets.MethodsDikma DiamonsilC18(200 mm×4.6 mm,5 μm)column was used in HPLC detection.The mobile phase consisted of acetonitrilewater(20:80),with a flow rate of 1 mL•min1,detection wavelength at 203 nm and under room temperature.ResultsThere was a good linear relationship for Ginsenoside Rg1 in range of 2.5-17.5 μg•mL1, the average recovery rate of astragaloside was 94.55% and RSD was 1.3%.ConclusionThis method is accurate, reproducible and sensitive,which can be used for the quality control of compound shenqi wuwei
  • 药物制剂与药品质量控制
    WU Changfu;SHEN Xianling;WANG Zongxi
    ABSTRACTObjectiveTo study on the optimum proportion allocated in the supplementary material of the compound xueya’an sustainedrelease tablets. MethodsThe orthogonal design was used to optimize the concentration of hydroxy propyl methyl cellulose, lactose and microcrystalline cellulose in the compound xueya’an sustainedrelease tablets under three levels test and assess the results. ResultsThe best formulation of the compound xueya’an sustainedrelease tablet was composed of 30% hydroxy propyl methyl cellulose, 30% lactose and 30% microcrystalline cellulose. ConclusionThe compound xueya’an sustainedrelease tablet made under the formulation shows ideal sustainedrelease outcome and the process is simple.