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  • 01 September 2015 Volume 34 Issue 9
      

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  • ZHAO Ying,MU Xin,DU Guanhua
    As an essential part of modern medical service,pharmaceutical care gains more and more attention in the field of medication.The goal of pharmaceutical care is to effectively control rational administration of drugs,improve the therapeutic efficacy and avoid adverse drug reactions.Pharmacology,as the key basis of pharmacy,directly determines the level of pharmaceutical care.Therefore,development of pharmacology,especially for the clinical pharmacology,plays an important role in enforcing capability of clinical pharmacists.In this article,we summarized the functions of medical care in medical practice based on the Chinese medication.Authors described the relationship of pharmacology and medical care in the medication for cancer,infectious diseases,and chronic diseases.Authors proposed that the rational drug administration under the guidance of pharmacology is the core point to evaluate the quality of clinic pharmaceutical care,and the final goal of which is to increase the benefit of medication and guide the training of pharmacists in China.
  • ZHAI Fengguo,ZHOU Fubo,LI Houzhong,GUO Sufen,LIN Feng,GUAN Lixin
    Objective To explore the effects of gross saponins of Tribulus terrestris L.on inflammatory reaction and permeability of blood-brain barrier in rats following cerebral ischemia-reperfusion injury and their potential mechanisms. Methods Sixty SD rats were divided into sham operation group,model control group,gross saponins of Tribulus terrestris L.at low-dose (10 mg·kg-1)and high-dose groups(30 mg·kg-1).Cerebral ischemia -reperfusion model was established with suture emboli method in middle cerebral artery of rats.Neural injury scores,the contents of Evans blue (EB) and myeloperoxidase( MPO) activities in rat brain were measured 24 hours after the cerebral reperfusion post 2 h ischemia.Content of tumor necrosis factor-α (TNF-α) in rat brain was detected by ELISA; expression levels of matrix metalloproteinase-9(MMP-9) in rat brain was determined by Western blot. Results Compared to the model control group,the neurological deficit scores were significantly decreased(P<0.05),MPO activities and EB contents decreased(P<0.05 or P<0.01)in the treatment groups.The expression levels of TNF-α were significantly lower in the treatment groups(0.760±0.110) mg·g-1 and (0.670±0.073) mg·g-1 compared to (0.920±0.128) mg·g-1 in the model control group (P<0.05 or P<0.01).The MMP-9 expression levels were (1.770±0.181)% and(1.480±0.146)%,significantly lower than(2.200±0.186)% in the model control group(P<0.01). Conclusion Gross saponins of Tribulus terrestris L.exert neuroprotective effects on cerebral ischemia-reperfusion injury in rats through inhibiting the inflammatory reaction and decreasing the permeability of blood-brain barrier,which may be associated with the decrease of the TNF-α content and downregulation of the MMP-9 expression.
  • RABIGUL Islam,YULTUZ Mamat,MAHSUTJAN Kadirt,SIRAPIL Abay
    Objective To study anti-psoriasis effect of Munziq Sawda on mouse model. Methods We established the mouse tail scale epidermis and psoriasis-like skin inflammation model by applying 5%propranol hydrochloride emulsion on mouse ears,and then observed body weight,thymus and spleen index,measured IL-10 ,IL-17,IL-23 secretion in serum with ELISA method,and also detected istopathological changes of the skin of tail and ears in mouse. Results No obvious abnormalities were found of general condition and body weight (P>0.05)during the experiment period in the Munziq Sawda treated groups(2,4,8 g·kg-1) ; Compared with the model control group,2 g·kg-1 Munziq Sawda decreased thymus index(2.841±1.211)vs(1.903±0.885) mg·g-1 (P<0.05); Munziq Sawda at 2,4,8 g·kg-1 did not obviously impact on the serum level of IL-10,IL-17 and IL-23 ( P>0.05); Munziq Sawda 2,4,8 g·kg-1 promoted the formation of epidermis granular layer in mouse tail and improved histopathological changes of the mouse ear skin. Conclusion Munziq Sawda has therapeutic action on experimental psoriasis model.
  • WANG Xiaofeng,ZHOU Jian
    Objective To explore the effect of oleanic acid on key enzyme activity in insulin-resistant HepG2 cells. Methods The HepG2 cells were divided into normal control,model control,metformin,and oleanic acid groups.Glycogen content in insulin-resistant HepG2 cell model were detected by hepatic glycogen test kit upon treatment with oleanic acid.Activities of glucokinase ( GK) ,phosphoenolpyruvate carboxylase kinase (PEPCK),and glucose-6-phosphatase (G-6-Pase) were assayed by the glucose 6-phosphate dehydrogenase coupling colorimetric,lactate dehydrogenase coupling colorimetric and ammonium molybdate constant phosphorus methods. Results The oleanic acid enhanced glucose consumption,lowered the activity of G-6-Pase and PEPCK by 54.8% and 18.8%,respectively,and increased the activity of GK and glycogen content in also insulin-resistant HepG2 cells by 100.6% and 98.6%,respectively. Conclusion The oleanic acid play a role in lowering PEPCK and G-6-Pase activities and inhibiting glucogenesis,resulting in the reduction of endogenous glucose in the cell.In addition,it can augment the activity of GK,accelerate the process of glucolysis,increase the glycogen content,and alleviate insulin resistance of HepG2.
  • XU Yuanping ,GAO Ling ,SONG Xiaohui,ZHOU Qian
    Objective To investigate the time and dose dependent effects of 17 β-estradiol(E2) on eNOS phosphorylation and nitric oxide (NO) production from bovine aortic endothelial cells (BAECs). Methods The BAECs were cultured in 24-well flat plate.The dose dependent rapid induction of NO release by E2 in the BAECs was explored,and the non-genomic mechanism was studied.Each experiment was repeated for 3 times.The NO level was quantified by the electron spin resonance spectroscopy(ESR)method,and the phosphorylation of eNOS were determined by Western blot. Results NO release increased time dependently from BAECs after treatment with E2 at 100 nmol·L-1 at 1,5,10 and 15 min,and the effect peaked at 10 min.There were dose dependent effects of NO production as well as eNOS phosphorylation after treatment with E2 at different concentrations for 10 min,and the effect was the most obvious at the concentration of 100 nmol·L-1.Upon treatment with equal volume of saline,E2 and actinomycin D (25 μg·mL-1) for 10 min,the NO release was(5.38±2.35),(10.59±3.28)and(10.68±3.31) nmol·mg-1,respectively,and the eNOS phosphorylation level was 0.36±0.03,0.98±0.08 and 0.99±0.08,respectively.Compared with 0.9% sodium chloride solution,the NO release and eNOS phosphorylation were significantly increased in E2 treated cells(all P<0.05). Conclusion 17 β-estradiol at 100 nmol·L-1 induced eNOS phosphorylation as well as NO production from bovine vascular endothelial cells through non-genomic mechanism.The effect peaked at 10 minutes.
  • DIAO Chunyan,MA Jiangwei,MI Le,ZHAO Naiqian,WANG Libin,LIU Xueying
    Objective To develop an HPLC-MS/MS method for quantitative determination of PA-824 in rat plasma and to study the pharmacokinetics of PA-824 in rat after oral administration. Methods An HPLC-MS/MS method was developed and validated for determination of PA-824 in rat plasma using metronidazole as internal standard.The proteins in plasma samples were precipitated with methanol,and PA-824 was enriched for analysis by HPLC-MS/MS.An Inertsil ODS3 C18 column (150 mm×4.6 mm,5 μm) was applied with mobile phase composed of methanol- 0.03% triethylamine (TEA) in water (90:10) ,at a flow rate of 0.5 mL·min-1 and column temperature of 30 ℃.Quantitation was performed on a triple quadrupole mass spectrometer applying electrospray ionization technique and operating in multiple reaction monitoring (MRM) and positive ion mode with transitions at 360.1/175.0 for PA-824 and 172.0/128.0 for metronidazole.The concentration of PA-824 in plasma was tested after oral administration at various time points and the data were processed with software DAS.2.0. Results The standard calibration curve for spiked rat plasma containing PA-824 was linear over the range of 0.1-10.0 μg·mL-1 .The recoveries obtained for PA-824 were greater than 92.13%.Intra-day and inter-day coefficient of variation were less than 6.6%.After oral administration,the main pharmacokinetic parameters were AUC(0-t):(3 297.503±320.958)mg·L-1·min-1,AUC(0-∞):(3 558.315±338.860) mg·L-1·min-1,tmax:(360.000±64.143) min,Cmax:(3.5±0.3)mg·L-1. Conclusion The method is rapid,accurate,simple,and successfully applied in a pharmacokinetic study of fixed dose oral administration of PA-824 in rats.
  • LI Li,ZHAI Xuejia
    Objective To develop a method on evaluating the uncertainty during the determination of cefixime in human plasma by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Methods We analyzed various factors that can cause the uncertainty in the whole process of determination,which includ repeatability,weighting,preparation of standard solutions,sample preparation,equipment error and calibration curve fitting.The expanded uncertainty was evaluated by calculating uncertainty of each component and combined. Results The expanded uncertainty for low (80 ng·mL-1),medium (560 ng·mL-1) and high (9 600 ng·mL-1) level of cefixime was 14.93,23.65,137.95 ng·mL-1,respectively (P=95%). Conclusion The uncertainty of determining cefixime in human plasma by HPLC-MS/MS is mainly caused by the calibration curve fitting,repeatability and HPLC-MS/MS error.
  • LIU Yeling,WANG Zhongshi,ZHANG Xu
    Objective To investigate the effect of total alkaloids from Rhynchophylline on hypertensive target organs. Methods 40 spontaneous hypertensive rats (SHRs) were divided into 4 groups as follows: normal control group,positive control with Tianma Goutengyin granule at 750 mg·d-1,total alkaloids from Rhynchophylline at 2.5 mg·day-1 as low dosage,and at 15.0 mg·d-1 as high dosage.All the rats were fed up for 20 weeks,and baroreflex sensitivity (BRS,in ms·mmHg -1)was determined by revised Smyth’s method.Heart,brain and kidney of the rats were sectioned for histological analysis at the end of 20th week. Results In sixteenth weeks,BRS of normal control,Tianma Goutengyin granule group,total alkaloids at low dosage and high dosage were(0.27±0.05),(0.31±0.06),(0.35±0.08),(0.34±0.08) ms·mmHg -1,respectively.BRS in SHR was not decreased except in the normal control group.The treatment groups were superior to the normal control group in structure of heart,but not in the brain and kidney of the rats. Conclusion Total alkaloids from Rhynchophyllinecould protect heart from hypertensive injury.
  • XU Xiaoyan,LI Ying,WANG Wei,WANG Hao,CHEN Wei
    Objective To study the protective effect of total glucosides of Mudan cortex(TGM)on acute myocardial ischemia in mice and its mechanism. Methods The total of 60 mice were randomly divided into 5 groups (n=12),normal control and model control (were given equal capacity of 0.9% sodium chloride solution),and TGM at low,middle,high dose (were given with 50,100,200 mg·kg-1 TGM).The mice were administered once daily for consecutive seven days.After the last administration,the mice in the model control and drug groups were treated by intraperitoneal injection of 15 mg·kg-1 isoproterenol to to make myocardial ischemia animal model.TGM on the T wave and J point on ECG,and serum lactate dehydrogenase (LDH),myocardial tissue superoxide dismutase (SOD),malondialdehyde (MDA) changes was detected,and the extent of myocardial ischemic injury in mice was measured by Nagar-Olsen staining. Results TGM significantly reduced the displacement of ECG T wave and J point,and improved the related biochemical indexes in mice with myocardial ischemia.The activity of LDH[(898.992± 285.108) μmol·mg-1] ,the content of MDA[(11.737 ±5.162) nmol·mg-1]in mice treated with TGM at high dose obviously decreased in comparison to the model controls,and the activity of myocardial SOD[(45.505±20.711) U·mg-1] significantly elevated compared with the model control.It was showed that TGM significantly diminished the areas of cardiac muscles ischemia injured via Nagar-Olsen staining. Conclusion TGM has the remarkable protective effect on acute myocardial ischemia injury in mice.
  • LI Xin,FENG Yuanyuan,SUN Xuanxuan,LI Bing
    Objective To investigate the the molecular mechanism of telmisartan for myocardial remodeling in rats with renovascular hypertention. Methods The renovascular hypertensive myocardial hypertrophy model of rats were established by narrowing the left renal artery.The total of 45 mature male SD rats were divided into sham-operated group(n=15),model control (n=15) and telmisartan group (n=15) randomly.The rats in telmisartan group were treated with telmisartan (10 mg·kg-1·d-1) while those in the sham-operated and model control were reated with the same amounts of distilled water by intragastrical administration .At 8th week of administration,the myocardial structure and function were detected by ultrasonography.The blood pressure was measured by arterial catheterization and calculating the left ventricular mass index (LVMI) .The level of serum calcium and nerve phosphatase (CaN) and the expression of β-myosin heavy chain (β-MHC) mRNA were detected. Results The thickness of left ventricular,ejection fraction[(69.23±1.09)% vs(73.77±3.00)%],fractional shortening[(30.21±2.02)% vs(35.29±0.90)%],LVMI[(2.83±0.14) mg·g-1 vs(2.32±0.11) mg·g-1] were decreased,and the differences were statistically significant (P<0.05).The level of serum calcium and nerve phosphatase (CaN) and the expression of β-myosin heavy chain (β-MHC) mRNA were decreased in telmisartan treated rats,and the differences were statistically significant (P<0.05) when compared with the model control group. Conclusion Telmisartan can improve the myocardial hypertrophy of renovascular hypertensive rats,and it may downregulate the expression of β-MHC by inactivating of the start signal CaN and its downstream signal pathway.
  • WU Yue,PENG Yan,RONG Peipei,LI Meng,ZHOU Benhong
    Objective To retrospectively analyze the current application of warfarin in hospitalized patients with non-valvular atrial fibrillationand (NVAF),and explore the key role of clinical pharmacists in warfarin medication. Methods A retrospective survey of anticoagulant therapy for 179 hospitalized patients with non-valvular atrial fibrillation in Renming Hospotal of Wuhan University from January to December 2013 was retrived,including the usage of warfarin for NVAF and antithrombotic therapy, the dose of warfarin,international normalized ratio(INR),hemorrhage event and so on.The simple factor like the age,complicated chronic diseases and previous cerebrovascular events on the use of warfarin was explored. Results The total response rate to anticoagulants was 85.6% for patients with high risk of stroke(27.3% with warfarin and 58.3% with antiplatelet therapy),who are recommended to use warfarin,patients were treated with anti-thrombotic therapy.The total of 19.1% of the patients with new-onset atrial fibrillation used warfarin as therapy.The whole monitoring rate of INR was 89.8%,and the good control rate was 11.9%.Univariate analysis showed that some high risk factors such as age and high blood pressure affected the usage of warfarin. Conclusion The anti-thrombotic therapy for NVAF patients in the hospital is good,but usage of warfarin for those with new-onset atrial fibrillation is low,which couldn't reach the INR standard.More attention should be taken by the clinic pharmacists in effective managing the use of anticoagulant to build a safe,economic and effective medication system for warfarin application.
  • LI Xiaojin,YANG Gaisheng,YANG Jiguang,ZHANG Xiaoguang
    Objective To evaluate the feasibility of propofol infusion by a closed-loop system for the titration of anaesthetic in laparoscopic cholecystectomy guided by Bispectral Index (BIS). Methods Forty patients subjected to laparoscopic cholecystectomy randomly allocated into two groups: the control group with opened-loop titratioin of propofol TCI induced at a target of 4 μg·mL-1 and aintained from 2 to 5 μg·mL-1 and the treatment group with closed-loop titration was performed using a proportional differential algorithm.For both groups,the BIS was set at 45-55.Remifentanil TCI was infused at a target of 4 ng·mL-1 and was maintained according to the situation.The change in medial arterial pressure(MAP),heart rate(HR) and BIS were recorded before anesthesia(t0),target BIS of 50(t1),at tracheal intubation(t2),during incision of skin(t3),5 min after the operation(t4),at t5 of gallbladder removing and at t6 of skin suturing.The dose of propofol was calculated. Results Haemodynamic data were similar between groups during the induction.But MAP was decreased significantly at t1,t3,t4,t5 in the control compared with the treatment group (P<0.05).HR changes a lot at t5 in the control compared with the treatment (P<0.05).Total dose of propofol in the treatment group was statistically lower than that in the controls[(110.10±8.34) vs (120.55±6.26) mg; (603.20±116.55) vs (759.50±116.37) mg,P<0.05)]. Conclusion Automated titration guided by BIS for propofol infusion is feasible without increase in haemodynamic adverse effects and is of less propofol consumption in the laparoscopic cholecystectomy.
  • JIANG Jingwei,LU Huarong,MAO Guiqin,ZHU Xuefen,MAO Chenjun
    Objective To investigate the effects of intrathecal different doses of dexmedetomidine hydrochloride in spinal block by ropivacaine hydrochloride . Methods Forty lower limb surgery scheduled for elective under spinal anesthesia,were randomly divided into 2 groups (n=20 each): the control and the treatment groups.The control and the treatment group were intrathecally injected with 4,12 μg dexmedetomidine hydrochloride respectively.The 0.75% ropivacaine hydrochloride 1.5 mL was injected for spinal anesthesia.SBP,DBP,HR,SpO2 and Ramsay Sedation Score were recorded before the spinal anesthesia conduct and thereafter every five minutes.And the onset and duration of block were recorded,adverse reaction like nausea,vomiting and respiratory depression were also observed. Results Compared with the control group,the onset of sensory block was shorter[(6.9±2.6) min vs (8.7±2.9) min] (P<0.05),and the duration of sensory and motor block was longer in the treatment group [(130.8±30.1) min vs (115.9±23.9) min] (P<0.05) and[(145.9±29.0) min vs (130.0±30.1) min] (P<0.05). Conclusion Intrathecal dexmedetomidine hydrochloride at 12 μg improves anesthesia via shortening the sensory block onset and prolonging sensory and motor block,which maintains hemodynamically stable,and does not generate adverse reactions as nausea,vomiting,bradycardia and respiratory depression.
  • LI Guang,LU Juan,LI Xuelan,ZHANG Ning,LIU Bin,CHEN Xi
    Objective To develop a method for content determination of sinensetin,eupatorin,and 3′-hydroxy-5,6,7,4′-tetramethoxyflavone in Orthosiphon stamineus. Methods The determination was carried out on a Symmetry C18 column (4.6 mm×250 mm,5 μm) by HPLC.The mobile consisted of acetonitrile and water containing 0.05% H3PO4 in gradient elution.The flow rate was 1 mL·min-1,the column temperature was 35 ℃,the detected wavelength was set at 365 nm, and the injection volume was 10 μL. Results The peak areas and the sample quantity of the three components presented good linear relationship in the range of 0.50-5.00 μg for sinensetin,0.50-5.00 μg for eupatorin,and 0.05-0.50 μg for 3′-hydroxy-5,6,7,4′-tetramethoxyflavone.The average recoveries were 101.26%,100.28% and 99.66%,respectively. RSD were 1.73%, 0.82% and 1.68%, respectively. Conclusion The method is proved to be simple,accurate and can be used for the quality evaluation of Orthosiphon stamineus.
  • LI Shengqian,FENG Jing,LIU Fu,JIANG Chengping,YANG Yun,XU Xiuhua
    Objective To investigate the application of iohexol in enhanced CT scanning. Methods The total of 623 patients taking iohexol for enhanced CT scanning were sampled to record relevant data for reference.According to evaluation standards for rational use of contrast media,the risk factors,selection of contrast media,medication time,usage and dosage,and drug combination were analyzed statistically. Results Among 623 patients used iohexo for enhanced CT scanning,302 patients had the risk factors of adverse reaction(the incidence rate as 48.48%) and 115 patients received psychological intervention(the incidence rate as 18.46%).And 206 patients had been given with the reasonable fluid therapy before and after angiography(the incidence rate as 33.07%),there were only 124 patients who performed the renal function and urine routine examination 48-72 h before and after angiography(the incidence rate as 19.90%).And 33 patients occured allergic reaction with the incidence rate as 5.30%. Conclusion There existed irrational phenomenon in application of diodone in enhanced CT scanning.It is necessary to further standardize the clinical application of diodone and make complete measures for rational use of diodone.
  • LI Jingjing,WU Xinying,XU Jun,DU Lifen,SONG Hongping,CHEN Guanrong,GU Ye
    Objective To analyze whether routine prophyrlactic antibiotic administration is necessary for the patients undergoing coronary stent implantation. Methods The clinical data of 156 patients from January 2010 to December 2010(prophylactic antibiotic therapy),and 466 patients from January 2014 to December 2014(no-prophylactic antibiotic therapy),who underwent coronary stent implantation, were retrospectively analyzed. The infection rates in two groups were compared. Results The rate of infections related to coronary stent implantation in no-prophylactic antibiotic therapy group and prophylactic antibiotic therapy group, such as surgical site infection (0.2% vs 1.3%,P>0.05)and catheter-related infection(0.6% vs 1.9%,P>0.05), was not significant different(P>0.05). Similarly, the unrelated to coronary stent implantation was not significant different, too(P>0.05). Conclusion Routine prophylactic antibiotic administration is unnecessary for the patients undergoing coronary stent implantation.
  • FU Wei,LIU Dong
    Objective To provide basis for rational drug use of clinical practice by analysis of antidepressants application in Wuhan. Methods Antidepressants were classified according to the structure and mechanism.By using the analytical method of the defined daily dose (DDD) recommended by WHO,authors statistically analyzed the relative data of antidepressants used in 34 hospitals of Wuhan from 2011 to 2013. Results The consumption of the antidepressants had been increased year by year,selective serotonin reuptake inhibitor (SSRIs) and serotonin noradrenergic reuptake inhibitors (SNaRIs) were widely used and presented higher proportion than others in the consumption of antidepressants,the average amount of the sales was 50.49% and 21.81%,respectively.The application of tricyclic antidepressant (TCAs) decreased in Wuhan,the amount of sales for 3 years accounted for 0.56%,0.37% and 0.15%. Conclusion SSRIs and SNaRIs have already become the first-choice drugs in clinic practice because of good efficacy and high safety,other new types of antidepressants have a great potential for development,TCAs are fewly used now.