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甲氧基红霉素对卡马西平药物动力学的影响 总被引:2,自引:0,他引:2
应用荧光偏振免疫法,测定6只家兔po卡马西平及连续多次po用搓甲氧基红霉素后po卡马西平的血清卡马西平浓度,用3p87程序包按二室模型对数据进行处理并进行统计学分析。 相似文献
3.
The in vivo effects of berberine (BBR), the widely used bioactive herbal ingredient from many traditional Chinese medicinal herbs, on the pharmacokinetics of carbamazepine (CBZ, a substrate of CYP3A) and its metabolite carbamazepine 10,11‐epoxide (ECBZ), digoxin (DIG, a substrate of P‐gp) and cyclosporine A (CsA, a dual substrate of CYP3A and P‐gp) were evaluated in rats. After a 2‐week pretreatment with BBR, the pharmacokinetic parameters of i.g. administered CBZ and ECBZ were not significantly altered. The pharmacokinetics of i.v. administered DIG was not modified by single and 2‐week pretreatments with BBR, but a dose‐dependent increase in AUC and Cmax was observed in the i.g. administered DIG parameters in rats. The AUCs of DIG with BBR (30 mg/kg, 100 mg/kg) were 133%, 170% (single) and 123%, 169% (2‐week) of control, respectively. The AUC and Cmax of i.g. administered CsA with a 2‐week pretreatment with BBR increased by 62% and 43% (BBR 30 mg/kg, p < 0.05), 96% and 60% (BBR 100 mg/kg, p < 0.01), compared with the control. In conclusion, berberine produced a dose‐dependent increased bioavailability of digoxin and cyclosporine A by inhibition of intestinal P‐gp. No significant changes in CYP3A activity by berberine were observed. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
4.
卡马西平片体外溶出度与体内吸收相关性 总被引:2,自引:0,他引:2
目的:考察卡马西平(CBZ)片溶出度与体内吸收的相关性。方法:应用ZRS-4溶出度仪测定卡马西平片的溶出度。4名男性健康志愿性po单剂量200mgCBZ用TDx分析仪测定血药浓度,并按照Wagner-Nelson公式计算药物吸收分数。结果:体外溶出度与体内药物吸收分数的相关系数r=0.9261,体外溶出度与体内药物吸收分数的相关系数r=0.9977。结论:CBZ片体外溶出度与体内吸收有较好的相关性 相似文献
5.
卡马西平多晶型的研究 总被引:4,自引:0,他引:4
红外吸收图谱与中国药典图谱不符合的卡马西平(A晶),可通过用较高浓度乙醇使其转为B晶而符合规定,经 ̄(13)CNMR、MS、X线衍射分拆,证实该两种晶体为同质异晶。 相似文献
6.
Samara U. Oliva Rhaiza R. Andretta Joana N. Simas Renato B. Tesser Camila C. Paccola Sandra M. Miraglia 《Andrologia》2021,53(3):e13969
Carbamazepine (CBZ) is used in the control of seizure and affective disorders, causing hypothyroidism. Thyroid hormones regulate the Sertoli cell proliferation and differentiation. Clinical aspects must be considered since epileptic fertile women need to continuously use CBZ during pregnancy and lactation. This study aimed to evaluate the effects of CBZ on testis development of rat offspring from dams treated during pregnancy/lactation. Rat dams received CBZ (20 mg kg−1 day−1) or vehicle by intra-peritoneal route during gestation and lactation. Progenies were euthanised at 4, 14, 41, 63 and 93-days post-partum (dpp) for the evaluation of T3, T4 and TSH plasma total levels. Testicular cross sections were submitted to anti-Ki67, anti-PCNA, anti-p27kip1 and anti-transferrin immunolabelling for the evaluation of Sertoli cells. There was a significant reduction in p27kip1-positive Sertoli cell numerical densities and an increase in TSH level at 14 dpp. CBZ exposure affected the volume density of transferrin-positive immunolabelling at 63 dpp. These results suggest that CBZ may cause a dysregulation of the controller system of thyroid hormones homeostasis leading to an increase in the proliferation rate at the neonatal phase and a differentiation delay of the Sertoli cell, culminating in an altered function at late puberty. The occurrence of hypothyroidism cannot be completely discarded. 相似文献
7.
Ahmet Tektemur Ebru Etem Önalan Nalan Kaya Tektemur Serap Dayan Cinkara Ayten Kılınçlı Çetin İbrahim Tekedereli Tuncay Kuloğlu Gaffari Türk 《Andrologia》2021,53(2):e13954
Male infertility is a global health problem, and the underlying molecular mechanisms are not clearly known. Ion channels and microRNAs (miRNAs), known to function in many vital functions in cells, have been shown to play a significant role in male infertility through changes in their expressions. The study aimed to evaluate the alterations of testicular and/or spermatozoal potassium voltage-gated channel subfamily J member 11 (KCNJ11), Cystic fibrosis transmembrane conductance regulator (CFTR), miR-let-7a and miR-27a expressions in carbamazepine-related male infertility. Here, we showed that carbamazepine reduced sperm motility, increased abnormal sperm morphology, and impaired hormonal balance as well as increased relative testis weight and decreased relative seminal vesicle weight. On the other hand, downregulated KCNJ11 and upregulated miR-let-7a expressions were determined in testis (p < .05). Also, downregulated KCNJ11 and upregulated CFTR and miR-27a expressions were found in spermatozoa (p < .05). Interestingly, altered testicular KCNJ11 and miR-let-7a expressions were correlated with decreased sperm motility and elevated sperm tail defect. Besides, spermatozoal CFTR and miR-27a expressions positively correlated with sperm tail defects. The results indicated a significant relationship between ion channel and/or miRNA expression alterations and impaired sperm parameters due to carbamazepine usage. 相似文献
8.
RF—HFLC法测定人血浆中苯巴比妥、苯妥英和卡马西平浓度 总被引:2,自引:3,他引:2
目的 建立血浆中苯巴比妥 (phenobarbital,PB)、苯妥英 (phenytion ,PT)和卡马西平 (carbamazepine ,CBZ)三种抗癫痫药的HPLC检测方法。方法 采用日本分光JASCO 15 0 0系列高效液相色谱仪 ,ODSHypersil柱 (15 0mm× 4 6mm ,5 μm) ,以艾司唑仑(estazolam ,EZ)为内标 ,流动相组成为甲醇 -乙腈 -水 -四甲基乙二胺 -冰醋酸 (5 0∶5 0∶10 0∶2∶1 5 ) ,流速为 0 8ml·min-1,紫外检测波长 2 5 4nm ,灵敏度AuFs=0 0 2。结果 血浆中 3种组分和内标均能很好地分离 ,无明显的干扰峰。PB线性范围为 2~ 5 0mg·L-1,r=0 9997;PT线性范围为 2~ 5 0mg·L-1,r=0 9998;CBZ线性范围为 0 5~ 2 0mg·L-1,r=0 9998,日内、日间RSD <5 %。结论 本法操作简便、结果可靠 ,适用于药物监测和中毒分析 相似文献
9.
卡马西平对吗啡依赖大鼠戒断症状及ACTH的影响 总被引:2,自引:1,他引:2
目的 :观察卡马西平 (Carb)对吗啡依赖大鼠纳洛酮催促戒断症状的抑制作用及血清促肾上腺皮质激素(ACTH)水平的影响。方法 :剂量递增法皮下注射 (sc)盐酸吗啡 (Mor) ,建立大鼠吗啡依赖模型 ,腹腔注射 (ip)盐酸纳洛酮 1mg·kg- 1 催促 ,观察戒断反应并评分 ;免疫发光法测定血清ACTH水平。结果 :Carb 10 0mg·kg- 1 及 2 0 0mg·kg- 1 均可明显减轻大鼠戒断症状 (P <0 0 5 )。 10 0mg·kg- 1 剂量组的ACTH水平接近正常 ,低于Carb 2 0 0mg·kg- 1 组(P <0 0 5 )。结论 :适当剂量的卡马西平可有效控制吗啡依赖大鼠的戒断症状 相似文献
10.
HPLC法同时测定血清中苯巴比妥、苯妥英和卡马西平的浓度 总被引:7,自引:1,他引:7
目的 :建立快速测定血清中苯巴比妥、苯妥英和卡马西平浓度的方法。方法 :色谱柱DiamonsilC18(4 .6mm× 2 5 0mm ,5 μm) ,流动相甲醇∶水∶乙腈 (4 0∶4 5∶15 ) ,流速1.2ml·min-1,检测波长 2 4 0nm ,内标硝西泮 ,柱温 4 0℃。结果 :提取回收率为 84 .4~ 89.2 % ,日内和日间RSD均 <7.9% ;标准曲线相关性良好。对 10 4例患者作血清浓度监测 ,临床效果满意。结论 :本方法可作为苯巴比妥、苯妥英和卡马西平的血药浓度监测的常规方法。 相似文献