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991.
Ahmadi F Varshosaz J Emami J Tavakoli N Minaiyan M Mahzouni P Dorkoosh F 《Drug delivery》2011,18(2):122-130
Budesonide is an anti-inflammatory drug of choice for treatment of ulcerative colitis which affects the rectum and a part of or the entire colon. Delivery of budesonide specifically to the colon would increase the efficacy of the drug and reduce the side-effects. The aim of this study was to develop an oral matrix system formulation for budesonide to deliver the major part of the drug to the colon for treatment of ulcerative colitis that has not been reported before. Directly compressed matrix tablets were prepared using different molecular weights of dextran and three ratios of drug-to-polymer. The physical properties of the tablets including weight variation, hardness, content uniformity, and release profile in HCl 0.1 N, phosphate buffer pH 7.4 and 6.8 containing 4% rat caecal and colonic contents were studied. The efficacy of the desired formulation was also evaluated against acetic acid-induced colitis in rats. Physical properties of the tablets were in the ranges recommended by official references. More than 10% of the drug was released in HCl 0.1 N and pH 7.4, while a very drastic increase was observed after exposure to pH 6.8 containing rat caecal contents. The efficacy of the selected formulation against rat-induced colitis was also increased in comparison to the non-targeted formulation of budesonide. In conclusion, matrix tablets with a 1:10 drug-to-dextran ratio with high molecular weight could deliver the drug specifically to the colon and are promising for treatment of ulcerative colitis. 相似文献
992.
993.
目的:探讨极低频率电磁场(extremely low—frequency electromagnetic field,ELF—EMF)对小鼠生育力和着床前期子宫与输卵管上皮细胞高度的影响。方法:80只雌性NMRI小鼠随机分为对照组和EMF组。对照组小鼠不接受EMF,EMF组小鼠接受50Hz、0.5mTEMF,每次4h,每周6次,连续2周。雌小鼠注射孕马血清促性腺激素和人绒毛膜促性腺激素促其排卵,与雄鼠交配。通过观察阴道栓形成确定小鼠妊娠后,冲洗子宫腔获得胚泡,取子宫角和输卵管组织用于光学显微镜检查。结果:EMF组小鼠平均胚泡数比对照组明显减少(P〈0.03)。光学显微镜下观察发现。EMF组小鼠输卵管上皮细胞高度较对照组明显增加,而子宫内膜上皮细胞高度与对照组比较差异无统计学意义。结论:ELF—EMF可能通过减少胚泡数目,增加输卵管上皮细胞高度而损伤雌性小鼠生育能力。 相似文献
994.
Ebrahimnejad P Dinarvand R Jafari MR Tabasi SA Atyabi F 《International journal of pharmaceutics》2011,406(1-2):122-127
SN-38, the active metabolite of irinotecan, poses a challenge in terms of drug delivery due to its low solubility and labile lactone ring. The aim of this study was to develop a SN-38 nanoparticulate delivery system to evaluate the in vivo blood profile and biodistribution properties of nanoparticles (NPs). Poly lactide-co-glycolide (PLGA) NPs that were covalently bound to polyethylene glycol-folate (PEG-FOL) were prepared, and their in vivo biodistribution in rats was investigated. Either the SN-38 solution or SN-38 NP suspension was administered intravenously into the tail vein at a dose of 2mg SN-38 eq./kg. As expected, SN-38 NPs showed a higher plasma concentration in vivo when compared with free SN-38 during a 24h period. Compared with the SN-38 solution, both folate targeted and non-targeted NPs exhibited superior drug concentration in body organs such as the liver, spleen, and lung at 1 and 8h post-administration. 相似文献
995.
Hanafi-Bojd MY Iranshahi M Mosaffa F Tehrani SO Kalalinia F Behravan J 《Planta medica》2011,77(14):1590-1593
In multidrug resistance (MDR), cancer cells exposed to anticancer agents develop resistance to a wide variety of chemicals and chemotherapeutic agents. Sesquiterpene coumarins are reported to inhibit P-glycoprotein and/or increase cytotoxicity of anticancer drugs in P-gp-overexpressing cell lines. In the current study, we investigated the effects of galbanic acid (from the roots of Ferula szowitsiana) and farnesiferol A (from the roots of Ferula persica) on functionality of the drug transporter P-glycoprotein (P-gp) using a rhodamine 123 efflux assay in a doxorubicin resistant breast cancer cell line (MCF7/Adr). Compared to verapamil, the well-known inhibitor of P-gp, galbanic acid (5, 10, and 25 μg/mL), significantly inhibited the P-gp activity. In inhibition of the P-gp transporter, farnesiferol A (0.5?μg/mL) was more potent than verapamil at 15 min exposure. Our results indicate that the plant derived sesquiterpene coumarins, farnesiferol A and galbanic acid, may be promising candidates to be considered for further studies on the reversal of multidrug resistance phenotype in chemotherapy of cancer patients. 相似文献
996.
Sodium is an essential micronutrient and, via salt taste, appetitive. High consumption of sodium is, however, related to negative health effects such as hypertension, cardiovascular diseases and stroke. In industrialized countries, about 75% of sodium in the diet comes from manufactured foods and foods eaten away from home. Reducing sodium in processed foods will be, however, challenging due to sodium's specific functionality in terms of flavor and associated palatability of foods (i.e., increase of saltiness, reduction of bitterness, enhancement of sweetness and other congruent flavors). The current review discusses the sensory role of sodium in food, determinants of salt taste perception and a variety of strategies, such as sodium replacers (i.e., potassium salts) and gradual reduction of sodium, to decrease sodium in processed foods while maintaining palatability. 相似文献
997.
Fatemeh Mosaffa Hermann Lage Jalil Tavakol Afshari Javad Behravan 《Inflammation research》2009,58(10):669-676
Objective
In this study, we aimed to evaluate the influence of proinflammatory cytokines on ABCG2 expression and function in human MCF-7 breast cancer cell line and its mitoxantrone-resistant derivative MCF-7/MX. 相似文献998.
Alizadeh BH Foroumadi A Emami S Khoobi M Panah F Ardestani SK Shafiee A 《European journal of medicinal chemistry》2010,45(12):5979-5984
A series of dibenzyl-γ-butyrolactones bearing a hydroxyl group at the benzylic position of 3-benzyl group were synthesized as hydrated analogue of isochaihulactone and evaluated against breast cancer human cell lines (MDA-M231, MCF-7 and T47D). The target compounds were synthesized in 7 steps from known lactone; (S)-(+)-γ-benzyloxymethyl-γ-butyrolactone. The key step was the aldol condensation between (+)-(R)-β-(benzo[d][1,3]dioxol-5-ylmethyl)-γ-butyrolactone and substituted benzaldehydes which afforded corresponding α-hydroxybenzyl butyrolactone analogues. The cytotoxic study of the synthesized compounds against breast cancer human cell lines showed that some of them inhibit breast cancer human cell proliferation with percentage inhibitions over 50% at concentrations less than 50?μg/mL. 相似文献
999.
1000.
Ulrike Nitz Oleg Gluz Matthias Christgen Ronald E. Kates Michael Clemens Wolfram Malter Benno Nuding Bahriye Aktas Sherko Kuemmel Toralf Reimer Andrea Stefek Fatemeh Lorenz-Salehi Petra Krabisch Marianne Just Doris Augustin Cornelia Liedtke Calvin Chao Steven Shak Rachel Wuerstlein Hans H. Kreipe Nadia Harbeck 《Breast cancer research and treatment》2017,163(3):573-586