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bupivacaine
相关语句
  布比卡因
    IMPROVED PROCESS FOR SYNTHESIS OF BUPIVACAINE HYDROCHLORIDE
    盐酸布比卡因合成工艺改进
短句来源
    Chiral Separation of Verapamil and Bupivacaine by Capillary Electrophoresis
    维拉帕米和布比卡因的毛细管电泳手性拆分
短句来源
    Synthesis of Bupivacaine Hydrochloride by Triphosgene
    三光气法合成盐酸布比卡因
短句来源
    Preparation and physical and chemical characteristic evaluation of bupivacaine human serum albumin microspheres
    盐酸布比卡因人血清白蛋白微球的制备工艺及其理化特性研究
短句来源
    Pain-alleviating effect of bupivacaine polylactic acid microspheres in rabbits
    布比卡因聚乳酸微球在家兔体内的缓释效应(英文)
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  “bupivacaine”译为未确定词的双语例句
    ① Change of bupivacaine concentration: Plasma bupivacaine concentration in Group A reached the peaked quickly after subutaneous injection with the high concentration of 2.466 4 mg/L, then declined quickly.
    ①血药浓度变化结果:注射组血药浓度迅速达到峰值,且浓度较高,为2.4664mg/L,随后浓度快速下降。
短句来源
    (2) Preparing for Bupivacaine Hydrochloride:①2-pipecolic acid was reacted with 1-butyl bromide to give 1-butyl-N-butyl-pipecolate, the latter amidated with 2,6-dimethylaniline that used NaH to form bupivacaine, bupivacaine was reacted with HCl aqueous to give Bupivacaine Hydrochloride.
    单纯形优化法寻找最佳反应条件,丁基化反应收率92%,酰胺化反应收率55%,总收率50%。 ②在罗哌卡因合成方法基础上,以中间体1-N-(2,6-二甲苯基)-2-哌啶甲酰胺为原料,与溴丁烷发生丁基化,反应收率93.5%;
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  相似匹配句对
    Synthesis of Bupivacaine Hydrochloride by Triphosgene
    三光气法合成盐酸布比卡因
短句来源
    IMPROVED PROCESS FOR SYNTHESIS OF BUPIVACAINE HYDROCHLORIDE
    盐酸布比卡因合成工艺改进
短句来源
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  bupivacaine
Effects of levobupivacaine and bupivacaine on rat myometrium
      
Objective: To study the effect of levobupivacaine and bupivacaine on the contractility of isolated uterine muscle strips from pregnant and non-pregnant female rats.
      
In the myometrium from non-pregnant rats,-logIC50 of levobupivacaine and bupivacaine were 4.85 and 4.25 respectively.
      
In the myometrium from pregnant rats, similar concentrations of levobupivacaine and bupivacaine were observed,-logIC50 were 2.7 and 2.9 respectively.
      
Levobupivacaine produced an increase in amplitude of contractions, while bupivacaine showed an increased trend in frequency.
      
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OBJECTIVE To prepare bupivacaine human serum albumin microspheres (Bupi-HSA-MS)by two different methods and compare the physical and chemical characteristics of the two products. METHODS The emulsifing heat-denatured method and high voltage electric electrostatic heat-denatured method were used to prepare Bupi-HSA-MS using uniform design. The effect of preparing condition on particle size, release rate, drug content and drug entrapment efficiency were researched. High performance capillary electrophoresis(HPCE)was...

OBJECTIVE To prepare bupivacaine human serum albumin microspheres (Bupi-HSA-MS)by two different methods and compare the physical and chemical characteristics of the two products. METHODS The emulsifing heat-denatured method and high voltage electric electrostatic heat-denatured method were used to prepare Bupi-HSA-MS using uniform design. The effect of preparing condition on particle size, release rate, drug content and drug entrapment efficiency were researched. High performance capillary electrophoresis(HPCE)was established to determine the release of Bupi-MS. RESULTS The result showed that particle size and the drug entrapment efficiency were affected by stirring rate (P<0.01) and drug/HSA concentration ratio evidently (P<0.01). The release experiment showed that the release rate was faster with smaller particle size and the release mode of Bupi-HSA-MS with large particle size could be described by Higuchi equation better, and that of small particle could be described by First order equation. High voltage electric electrostatic heat-denatured method increased the drug entrapment efficiency, decreased the burst effect and improved the reproduction ratio of preparation. The span of particle size was decreased from 1.98 to 0.52, the drug entrapment efficiency was increased from 50.87% to 91.62% with the new method compared with emulsifing heat-denatured method. CONCLUSION High voltage electrc electrostatic heat-denatured method is a simple and feasible method for preparing Bupi-HSA-MS.

目的 比较不同方法制得布比卡因人血清白蛋白微球的理化特性。方法 采用乳化热固化法和高压电场法制备布比卡因人血清白蛋白微球 ,通过均匀设计考察乳化热固化法制备工艺条件对微球粒径、释药速率、载药量和包封率的影响 ,以高效毛细管电泳法 (HPCE)测定微球的体外释放度。结果 搅拌速度和药物 蛋白浓度比可分别显著影响粒径大小和药物包封率。不同粒径大小微球的释放行为表明 ,随着微球粒径增大 ,其释放行为愈符合Higuchi方程 ,微球粒径愈小 ,愈符合一级动力学释放模式。高压电场法与乳化热固化法制备工艺相比 ,高压电场法制备微球的粒径分布集中 ,跨度由 1 98缩小为 0 5 2 ,包封率由原来的 5 0 87%提高到 91 6 2 %。结论 高压电场法是一种简单、可行的白蛋白微球制备新方法。

Objective: To study the synthesis of Bupivacaine hydrochloride by triphosgene.Methods: Bupivacaine hydrochloride was prepared via chlorination by triphosgene,amidation,butylation and acidification from 2-pipecolic acid.Results: The overall yield was 42.9%.The reactions were carried out under moderate condition with good selectivity.The intermediate can be directly used in the next step without any more purification.Conclusion: The process is easily controlled and there is no pollution to the environment.Therefore,it...

Objective: To study the synthesis of Bupivacaine hydrochloride by triphosgene.Methods: Bupivacaine hydrochloride was prepared via chlorination by triphosgene,amidation,butylation and acidification from 2-pipecolic acid.Results: The overall yield was 42.9%.The reactions were carried out under moderate condition with good selectivity.The intermediate can be directly used in the next step without any more purification.Conclusion: The process is easily controlled and there is no pollution to the environment.Therefore,it is suitable for industrial manufacture.

目的:研究三光气法合成盐酸布比卡因。方法:以三光气作为氯化剂,由2-哌啶甲酸经酰氯化、酰胺化、丁基化、成盐得盐酸布比卡因。结果:盐酸布比卡因合成总收率为42.9%。合成反应条件温和,选择性好,得到的中间体可直接用于后续反应。结论:本方法操作简单,污染少,适合工业化生产。

BACKGROUND: Bupivacaine is widely used to alleviate post-operation pain and cure acute and chronic pain caused by inflammation or cancer. Its analgesic time cannot meet the request that drug is released slowly to prolong the analgesic time in clinic. OBJECTIVE: To detect the alleviating effect of bupivacaine polylactic acid microspheres taking high molecular polymer-polylactic acid as vector in rabbits with high performance liquid chromatograph (HPLC) and traditional skin test method. DESIGN: A completely...

BACKGROUND: Bupivacaine is widely used to alleviate post-operation pain and cure acute and chronic pain caused by inflammation or cancer. Its analgesic time cannot meet the request that drug is released slowly to prolong the analgesic time in clinic. OBJECTIVE: To detect the alleviating effect of bupivacaine polylactic acid microspheres taking high molecular polymer-polylactic acid as vector in rabbits with high performance liquid chromatograph (HPLC) and traditional skin test method. DESIGN: A completely randomized controlled animal experimental study. SETTING: School of Pharmacy, Second Military Medical University of Chinese PLA MATERIALS: Sixteen New Zealand rabbits, weighing (2.58±0.17)kg were used in this experiment. INTERVENTIONS: The experiment was carried out at the Department of pharmaceutics, School of Pharmacy, Second Military Medical University of Chinese PLA between September and November 2002. ① Animal models were established according to traditional skin test method.② Totally 16 New Zealand rabbits were randomly divided into 2 groups : Group A and Group B, with 8 in each one. 5 mg/kg bupivacaine parenteral solution was injected subcutaneously in Group A, 5 mg/kg bupivacaine polylactic acid microspheres were implanted between subcutaneous tissue and sarcolemma in Group B. We took 1.5 mL blood from ear border vein at 5, 10, 20, 30, 45 minutes, 1, 2, 3, 4, 6, 8, 12 and 24 hours after administration of bupivacaine parenteral solution respectively in Group A and another 1.5 mL at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 3 6, 48 and 60 hours after admistration of bupivacaine microsphere powder for index detection. ③ HPLC method was used to detect the concentration and releasing effect of bupivacaine in blood serum. MAIN OUTCOME MEASURES: Concentration change of bupivacaine in blood serum and efficacy diameter of local anesthetic. RESULTS:All the 16 rabbits entered the stage of result analysis. ① Change of bupivacaine concentration: Plasma bupivacaine concentration in Group A reached the peaked quickly after subutaneous injection with the high concentration of 2.466 4 mg/L, then declined quickly. Plasma bupivacaine concentration in Group B was relative stable, reached a peak much slowly after subcutaneous implantation, with peak concentration of 0.778 1 mg/L, and the plasma bupivacaine concentration maintained a relative low level , the mean retention time was obviously prolonged (P < 0.05). ② Alleviating effect of bupivacaine: The analgesic time was significantly longer in the bupivacaine microsphere group than in the bupivacaine parenteral solution group (P < 0.05). CONCLUSION: Bupivacaine polylactic acid microspheres have sustained release effects in rabbits. Fu Q, Wang XH, Zou Z, Yu Y, Gao S, Zhong YQ, Zhang H.Pain-alleviating effect of bupivacaine polylactic acid microspheres in rabbits.Zhongguo Linchuang Kangfu 2006;10(25):181-3(China) INTRODUCTION Bupivacaine is widely used to alleviate post-operation pain and cure acute and chronic pain caused by inflammation or cancer. Although its analgesic effect is 2-3 folds of that of lidocaine, it cannot satisfy patients with prolonged pain. The dosage should be strictly restricted avoid to cardiovascular and central nervous system toxic reaction. Microsphere is a new method of drug preparation. Biocompatibility and corrosion of drug and high molecular polymer vector make the drug have sustained releasing effect and long efficacy. We made bupivacaine polylactic acid microspheres by using polylactic acid, which was a kind of high molecular polymer. Prolonged and sustained effect might achieve after microspheres powder was implanted under the skin before it was sutured after surgery. We tried to provide experimental proof for clinical usage of microspheres by comparing the pharmacokinetic and pharmacodynamic effects between bupivacaine polylactic acid microspheres and bupivacaine parenteral solution.

背景:布比卡因广泛应用于治疗及缓解因手术、炎症、肿瘤等引起的急、慢性疼痛,其镇痛作用时间不能满足临床对药物缓慢释放延长镇痛时间的要求。目的:采用高效液相色谱法和仿豚鼠皮丘法,检测以高分子聚合物——聚乳酸为载体制成的布比卡因聚乳酸微球在家兔体内所具有的缓释效应。设计:完全随机对照动物实验。单位:解放军第二军医大学药学院。材料:新西兰兔16只,体质量(2.58±0.17)kg。干预:实验于2002-09/11在解放军第二军医大学药学院药剂教研室完成。①采用仿豚鼠皮丘法建立动物模型。①新西兰兔16只,随机分为两组,每组8只。注射组皮下注射布比卡因注射液5mg/kg;微球组皮下植入布比卡因微球5mg/kg。注射组兔于射液后5,10,20,30,45min,1,2,3,4,6,8,12,24h及微球组兔于给药后0.5,1,2,3,4,5,6,8,12,24,36,48和60h耳缘静脉采血1.5mL进行指标测定。③高效液相色谱法测定血浆中布比卡因浓度及进行药物缓释作用测定。主要观察指标:血浆中布比卡因浓度的变化和局麻药作用直径。结果:16只兔进入结果分析。①血药浓度变化结果:注射组血药浓度迅速达到峰值,且浓度较高,为2....

背景:布比卡因广泛应用于治疗及缓解因手术、炎症、肿瘤等引起的急、慢性疼痛,其镇痛作用时间不能满足临床对药物缓慢释放延长镇痛时间的要求。目的:采用高效液相色谱法和仿豚鼠皮丘法,检测以高分子聚合物——聚乳酸为载体制成的布比卡因聚乳酸微球在家兔体内所具有的缓释效应。设计:完全随机对照动物实验。单位:解放军第二军医大学药学院。材料:新西兰兔16只,体质量(2.58±0.17)kg。干预:实验于2002-09/11在解放军第二军医大学药学院药剂教研室完成。①采用仿豚鼠皮丘法建立动物模型。①新西兰兔16只,随机分为两组,每组8只。注射组皮下注射布比卡因注射液5mg/kg;微球组皮下植入布比卡因微球5mg/kg。注射组兔于射液后5,10,20,30,45min,1,2,3,4,6,8,12,24h及微球组兔于给药后0.5,1,2,3,4,5,6,8,12,24,36,48和60h耳缘静脉采血1.5mL进行指标测定。③高效液相色谱法测定血浆中布比卡因浓度及进行药物缓释作用测定。主要观察指标:血浆中布比卡因浓度的变化和局麻药作用直径。结果:16只兔进入结果分析。①血药浓度变化结果:注射组血药浓度迅速达到峰值,且浓度较高,为2.4664mg/L,随后浓度快速下降。微球组血药浓度相对较平稳,达峰较晚,峰浓度=0.7781mg/L,且血药浓度一直维持较低水平,平均滞留时间明显延长(P<0.05)。②药效缓释作用结果:发现布比卡因微球组的镇痛作用时间较布比卡因注射液组明显延长(P<0.05)。结论:布比卡因微球制剂在家兔体内具有缓慢释放镇痛效应的作用。

 
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