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排序方式: 共有157条查询结果,搜索用时 31 毫秒
1.
Objective: To compare the safety and efficacy of two compounds of dihydroartemisinin(DHA) -Artekin and Artekin (T) in the treatment of uncomplicated falciparum malaria. Methods:The regimen of 8-tablet for 2 days of Artekin and Artekin (T) were applied to 100 patients with uncomplicated falciparum malaria, who were randomly divided into two groups. Each group contained 50 cases. The cure rate, the mean parasites clearance time, the mean fever clearance and side-effects were observed to assess the safety and efficacy of the compounds used. Results: The mean parasites clearance time was 31. 7±9.0 hours in the Artekin group and 32. 8±8. 8 hours in Artekin (T) group respectively; the mean fever clearance time was 12. 7±7. 2 hours in Artekin group and 16. 5±7. 9 hours in Artekin (T) group; there were no recrudescence case in both groups within the 28 days of follow-up, the cure rates in Artekin group and Artekin (T) groups were 100%. It indicated that the tolerability of both compounds were very good, the 相似文献
2.
目的:为了弄清蒿甲醚合成母液中的衍生杂质结构及开发新的药源。方法:用色谱法从合成蒿甲醚的母液中分离其衍生物成分,并用化学波谱法鉴定其结构,结果:分离得到5个化合物分别鉴定为α-蒿甲醚(Ⅰ),二氢青蒿素(Ⅱ),青蒿素(Ⅲ),八氢-8-甲氧基-4,7-二甲基-呋喃[3,2-i]苯并吡喃-10-乙酸酯(Ⅳ)和12-脱氧-11-烯青蒿素(Ⅴ)。结论:化合物Ⅴ为一新化合物,命名为12-脱氧-11-烯青蒿素,并首次从合成蒿甲醚的母液中得到。 相似文献
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Frank Kloprogge Rose McGready Aung Pyae Phyo Marcus J Rijken Warunee Hanpithakpon Hla Hla Than Nathar Hlaing Naw Thida Zin Nicholas P J Day Nicholas J White Fran?ois Nosten Joel Tarning 《British journal of clinical pharmacology》2015,80(4):642-653
Aim
The aim was to compare the pharmacokinetic properties of artesunate and dihydroartemisinin in the same women: i) pregnant with acute uncomplicated malaria on day 1 and 2, ii) pregnant with convalescent malaria on day 7 and iii) in a healthy state 3 months post-partum on day 1, 2 and 7.Methods
Non-linear mixed-effects modelling was used to compare plasma concentration–time profiles of artesunate and dihydroartemisinin over 7 days of treatment following oral and intravenous artesunate administration to pregnant women with uncomplicated Plasmodium falciparum malaria during their second or third trimesters of pregnancy. The same women were restudied 3 months after delivery when fully recovered. Non-compartmental results of the same study have been published previously.Results
Twenty pregnant patients on the Thailand-Myanmar border were studied and 15 volunteered to be restudied 3 months post-partum. Malaria and pregnancy had no effect on the pharmacokinetic properties of artesunate or dihydroartemisinin after intravenous artesunate administration. However, malaria and pregnancy had opposite effects on the absorption of orally administered artesunate. Malaria increased the absolute oral bioavailability of artesunate by 87%, presumably by inhibiting first pass effect, whereas pregnancy decreased oral bioavailability by 23%.Conclusions
The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered artesunate. Lower drug exposures during the second and third trimesters of pregnancy may contribute to lower cure rates and thus the development of drug resistance. Dose optimization studies are required for artesunate containing artemisinin-based combination therapies (ACTs) in later pregnancy. 相似文献5.
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Dihydroartemisinin suppresses ovalbumin-induced airway inflammation in a mouse allergic asthma model
《Immunopharmacology and immunotoxicology》2013,35(3):382-389
AbstractAsthma is a complex disease characterized by reversible airway obstruction, airway hyper-responsiveness (AHR) and chronic inflammation of the airways. Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin isolated from the traditional Chinese herb Artemisia annua, has been shown to possess antimalarial and antitumor activities, but whether it can be used in asthma treatment has not been investigated. In this study, we attempted to determine whether DHA regulates inflammatory mediators in the ovalbumin (OVA)-induced mouse asthma model. BALB/c mice were sensitized and challenged by OVA to induce chronic airway inflammation. The intragastrical administration of DHA at 30?mg/kg significantly decreased the number of infiltrating inflammatory cells, T-helper type 2 (Th2) cytokines, OVA-specific immunoglobulin E (IgE) and AHR. Treatment with DHA also attenuated OVA-induced mRNA expression of Muc5ac and chitinase 3-like protein 4 (Ym2) in lung tissues. In addition, lung histopathological studies revealed that DHA inhibited inflammatory cell infiltration and mucus hypersecretion. Then signal transduction studies showed that DHA significantly inhibited extracellular signal-regulated protein kinase (ERK), p38 mitogen-activated protein kinase phosphorylation. DHA also inhibited nuclear factor-κB (NF-κB) activation via the inhibition of phosphorylation of IκBα. These findings provide new insight into the immunopharmacological role of DHA in terms of its effects in a mouse model of asthma. 相似文献
7.
目的:观察注射用青蒿琥酯和复方双氢青蒿素片序贯治疗对南苏丹恶性疟疾病人的疗效。方法:回顾性分析2011年7月-2013年11月在南苏丹瓦乌中国二级医院住院的55例恶性疟疾病历。结果:肌注或静脉注射青蒿琥酯注射液(首剂120mg,后60mg/d)1~5d[(3.2±0.9)d],最后一次静脉注射或肌注后24、30、48、72h口服复方双氢青蒿素片2片,共8片。55例疟疾病人的总治愈率为100%,其中3d治愈52例(94.5%),3~7d治愈3例(5.5%)。4例(7.3%)病人发生恶心、呕吐、腹泻或头晕等轻度不良反应。结论:注射用青蒿琥酯和复方双氢青蒿素片序贯治疗,对南苏丹恶性疟疾病人具有非常好的临床疗效,适合多种人群,耐受性好。 相似文献
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目的阐明双氢青蒿素(DHA)诱导肿瘤细胞铁死亡的作用及其机制。方法利用3,3′,5,5′-四甲基联苯胺(TMB)检测DHA与FeSO_4体外芬顿样(Fenton)反应生成氧自由基(·OH)的能力;MTT法检测DHA对人肝癌HepG2细胞的毒性(包括FeSO_4与去铁胺预处理组)。MTT法考察谷胱甘肽(GSH)与铁死亡抑制剂(Fer-1)对DHA细胞毒性的影响;采用DCFH-DA染料考察DHA(包括FeSO_4预处理组)诱导的细胞内活性氧的生成能力;采用C11-BODIPY581/591与DiO分别考察DHA(包括FeSO_4预处理组)对细胞内脂质过氧化物生成能力以及细胞膜结构的影响;利用谷胱甘肽过氧化物酶4(GPX-4)试剂盒测定DHA(包括FeSO_4预处理组)对HepG2细胞内GPX-4活性的影响。结果 Fe~(2+)能够催化DHA发生芬顿样反应并生成·OH;DHA的半数抑制浓度(IC_(50))为(39.96±8.78)μmol/L,FeSO_4与去铁胺分别能够增加或者降低DHA的细胞毒性;DHA处理后细胞内活性氧含量与脂质过氧化物含量升高,细胞形态变大,细胞膜呈散点状分布并呈现解离状态。FeSO_4预处理组与DHA组相比较进一步增加细胞内活性氧含量与脂质过氧化物含量,并且细胞膜形态完全破坏。FeSO_4能够增强DHA对GPX-4活性的抑制作用。结论 DHA通过芬顿样反应升高细胞内活性氧而最终诱导肿瘤细胞铁死亡。另外,外源性铁可以加速DHA发生芬顿样反应进而加速肿瘤细胞铁死亡的发生与发展。 相似文献
10.
Efficacy of artesunate + sulphadoxine/pyrimethamine and artemether + lumefantrine and dhfr and dhps mutations in Somalia: evidence for updating the malaria treatment policy
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