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91.
    
Poorly soluble drugs constitute more than 60% of currently marketed pharmaceuticals with over two-thirds of promising new chemical entities failing to enter a clinical setting due to solubility issues. Although oral formulations have made some impact, alternative enhancement strategies for administration of such molecules are actively sought. Over the last decade, innovation on a global scale has enabled the expansion of the frontiers of microarray patches (MAPs) further than ever before. Initially designed to load low doses of hydrophilic and potent therapeutic agents, MAPs are now becoming a viable strategy for the immediate and long-acting delivery of poorly soluble drugs through the skin. This together with the advantages of transdermal administration over the oral and parenteral routes, make of MAPs an appealing platform for the development of products with increased patient compliance. Undoubtedly, MAPs will soon become a readily available therapeutic alternative, and experts from academia, industry and regulatory bodies are working together aiming to facilitate the progression of MAPs toward safe and effective clinical use. This review aims to highlight the ability of MAPs to deliver poorly soluble actives, discuss the mechanisms behind in-skin drug absorption, and evaluate the future direction of the field.  相似文献   
92.
    
Introduction: Hemodialysis patients frequently receive vancomycin for treatment of gram‐positive bacterial infections. This drug is most conveniently administered in outpatient dialysis units during the hemodialysis treatment. However, there is a paucity of data on the removal of vancomycin by high‐flux polyamide dialyzers. Methods: This is a prospective crossover study in which seven uninfected chronic hemodialysis patients at three dialysis units received vancomycin 1 gram intravenously over one hour immediately after the dialysis treatment (Phase 1), and vancomycin 1.5 grams during the last hour of dialysis treatment using a polyarylethersulfone, polyvinylpyrrolidone, polyamide high‐flux (Polyflux 24R) dialyzer (Phase 2). There was a three‐week washout period between phases. Serial serum vancomycin concentrations were used to determine the removal of vancomycin when administered during dialysis. Findings: Dialysis removed 35 ± 15% (range 18‐56%) of the vancomycin dose when administered during the last hour of dialysis. The calculated area under the curve (AUC) of vancomycin levels for 0‐44.5 hours from the start of infusion were similar between the two phases (AUCPhase 1 884 ± 124 mg‐hr/L, mean ± SD; AUCPhase 2 856 ± 208 mg‐hr/L; P=0.72). Serum vancomycin concentrations immediately prior to the next dialysis treatment following vancomycin administration were also similar between the two phases (13.1 ± 2.7 mg/L in Phase 1 and 12.3 ± 3.3 mg/L in Phase 2; P=0.55). Discussion: When using a polyarylethersulfone, polyvinylpyrrolidone, and polyamide high‐flux HD membrane with a 24R Polyflux dialyzer, vancomycin can be administered during the last hour of dialysis if the dose that is prescribed for intra‐dialysis dosing is empirically increased to account for intra‐dialytic drug removal.  相似文献   
93.
In order to control the silver content in the preparation process of platinum group anti-cancer drugs, we put two kinds of color reagent to color in the production process of the platinum anti-cancer drugs by UV spectra measurement to control drugs production of platinum anticancer, thus we could control the silver content in the drugs so that it meets the pharmacopoeia standards of US and European  相似文献   
94.
The removal of beta blockers and psycho-active drugs was investigated in a representative conventional German WWTP by long-term measurement campaigns along different biological treatment processes. The activated sludge treatment with an elevated SRT of 18 d was the only process which led to a significant removal of certain beta blockers and psycho-active drugs. The removal efficiency was below 60% for all compounds except for the natural opium alkaloids codeine and morphine being removed by more than 80%. Primary biological transformation and sorption onto sludge as the main removal mechanisms were examined in lab-scale batch experiments. Sorption onto activated sludge was found to be negligible (<3%). The biological transformation could be described by pseudo-first order kinetics and the transformation constants kbiol were used to predict the removal of beta blockers and psycho-active drugs in an activated sludge unit with a model. For most compounds the removal efficiencies measured on the full-scale WWTP were within the 95% confidence intervals predicted by the model. The results from full-scale measurements and modeling indicate that biological transformation in the nitrification tank together with parameters such as the sludge retention time and the temperature is crucial regarding the biological transformation of beta blockers and psycho-active drugs in conventional WWTPs.  相似文献   
95.
目的了解基本型乡镇卫生院辖区居民家庭所备存的药物、医药器械及便携式药包情况,为设计适合农村居民使用的便携药包提供参考。方法采用单纯随机抽样与整群抽样相结合的方法,对河北、江西与甘肃3个基本型卫生院所辖139户居民的家庭常用药品与药械配备及放置情况进行了调查与分析。结果基本型乡镇居民家庭常用药物的配备率依次为:感冒药最高为63.3%、创口贴40.3%、风油精36.7%、清凉油36.0%、高血压用药23.0%、碘酊18.0%、糖尿病用药2.2%、其他24.5%。家庭常用药械的配备率依次为:体温计最高为44.6%、棉签39.6%、血压计8.6%、注射器7.2%、其他16.5%。家庭常用药品及药械主要存放在固定抽屉达48.9%,只有4.3%的家庭拥有特定的放置药品与药械的便携式药包。结论基本型卫生院辖区农村居民家庭药品配备率较高,且多数为非处方药;家庭医用器械配备率不高,家庭便携式药包配备率极低,药品与医用器械存放的随意性较大,可能成为不合理用药的隐患。宜加强农民家庭自备药使用的教育与管理,提高便携式药包配备率,逐步改善家庭不合理用药。  相似文献   
96.
Here presented for the first time is the enantioselective biodegradation of amphetamine and methamphetamine in river microcosm bioreactors. The aim of this investigation was to test the hypothesis that mechanisms governing the fate of amphetamine and methamphetamine in the environment are mostly stereoselective and biological in nature. Several bioreactors were studied over the duration of 15 days (i) in both biotic and abiotic conditions, (ii) in the dark or exposed to light and (iii) in the presence or absence of suspended particulate matter. Bioreactor samples were analysed using SPE-chiral-LC-(QTOF)MS methodology. This investigation has elucidated the fundamental mechanism for degradation of amphetamine and methamphetamine as being predominantly biological in origin. Furthermore, stereoselectivity and changes in enantiomeric fraction (EF) were only observed under biotic conditions. Neither amphetamine nor methamphetamine appeared to demonstrate adsorption to suspended particulate matter. Our experiments also demonstrated that amphetamine and methamphetamine were photo-stable. Illicit drugs are present in the environment at low concentrations but due to their pseudo-persistence and non-racemic behaviour, with two enantiomers revealing significantly different potency (and potentially different toxicity towards aquatic organisms) the risk posed by illicit drugs in the environment should not be under- or over-estimated. The above results demonstrate the need for re-evaluation of the procedures utilised in environmental risk assessment, which currently do not recognise the importance of the phenomenon of chirality in pharmacologically active compounds.  相似文献   
97.
目的 通过开展抗菌药物临床应用专项整治活动,探讨南昌大学第一附属医院介入手术围术期预防用药的合理性.方法收集该院2013年3-5月住院的1 160例10种介入手术病例的抗菌药物使用情况,并对其合理性进行分析.结果 永久或临时起搏器安置/更换术、椎间盘射频消融术的预防使用抗菌药物的使用率分别是87.95%、83.33%,其他8种介入手术的使用率都为0.结论 该院介入手术围术期抗菌药物的使用率已趋达到卫生部的标准,呈整体合理趋势.加大对医护人员的培训和监督力度,能够明显改善抗菌药物用药不合理的局面.  相似文献   
98.
色谱技术是天然产物研究中重要的分离和纯化方法。本文介绍了色谱法,并综述了其在中药标准品制备中的应用,最后对此进行了展望。  相似文献   
99.
The adsorption effect of esomeprazole (ESP) and lansoprazole (LP) on corrosion behavior of copper in 1 M HNO3 solution was investigated using potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and weight loss measurements. The experimental results indicate that both ESP and LP inhibited the corrosion of copper in nitric acid solution and the inhibition efficiency increased as the concentration of the compounds increased. EIS measurements confirmed that the charge transfer resistance increases on increasing the inhibitor concentration. Polarization measurements showed that the inhibitors are of mixed type. From the weight loss measurements, the inhibition efficiency of the inhibitors was found to vary with concentration, immersion time, and temperature. The adsorption of inhibitors on the copper surface follows Langmuir isotherm. The surface morphology was examined by scanning electron microscope and atomic force microscope. Further, the computational calculations are performed to find a relation between their electronic and structural properties.  相似文献   
100.
    
A topoisomerase-DNA transient covalent complex can be a druggable target for novel topoisomerase poison inhibitors that represent a new class of antibacterial or anticancer drugs. Herein, we have investigated molecular features of the functionally important Escherichia coli topoisomerase I (EctopoI)-DNA covalent complex (EctopoIcc) for molecular simulations, which is very useful in the development of new antibacterial drugs. To demonstrate the usefulness of our approach, we used a model small molecule (SM), NSC76027, obtained from virtual screening. We examined the direct binding of NSC76027 to EctopoI as well as inhibition of EctopoI relaxation activity of this SM via experimental techniques. We then performed molecular dynamics (MD) simulations to investigate the dynamics and stability of EctopoIcc and EctopoI-NSC76027-DNA ternary complex. Our simulation results show that NSC76027 forms a stable ternary complex with EctopoIcc. EctopoI investigated here also serves as a model system for investigating a complex of topoisomerase and DNA in which DNA is covalently attached to the protein.  相似文献   
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