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排序方式: 共有164条查询结果,搜索用时 15 毫秒
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Angel J. Amante Herwig-Ulf Meier-Kriesche Linda Schoenberg B. D. Kahan 《Transplant international》1997,10(3):217-222
The initial poor absorption of the corn oil-based, gel capsule oral formulation of cyclosporin (CyA) greatly limits its use
for inception of immunosuppressive therapy. Insufficient drug concentrations during the early post-transplant period predispose
to renal allograft rejection. The present study served to compare the time required to achieve therapeutic CyA concentrations
after de novo administration of the corn oil-based gel capsule (CyA-GC; n = 11) versus the microemulsion (CyA-ME; n = 11) formulation of CyA. During the 1st month after renal transplantation, patients underwent serial pharmacokinetic profiling
from which we obtained observed and dose-corrected values of several parameters. Although patients in neither the CyA-GC nor
the CyA-ME group adequately absorbed the drug during days 0–2, from day 3 to 4 patients in the CyA-ME group showed significantly
greater absorption than those in the CyA-GC group (P = 0.041). Patients in the CyA-ME group reached the 1st month target average concentration (Cav) values ( ≥ 550 ng/ml) earlier than those in the CyA-GC group and required significantly lower daily CyA doses (P = 0.018). We conclude that therapeutic CyA levels can be achieved more rapidly and with lower doses of the drug after de
novo administration of CyA-ME than with CyA-GC.
Received: 13 September 1996 Accepted: 7 January 1997 相似文献
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微乳对难溶性药物增溶机理的研究 总被引:17,自引:1,他引:16
目的:初步探讨微乳对难溶性药物的增溶机理.方法:经处方筛选及相图研究确定(BL-9/正丁醇3∶1)/油/水比例为9∶1∶40的微乳处方;以二氢吡啶类药物为模型药物,测定其在微乳、胶束和油相中的溶解度及油/水分配系数;根据化学结构,采用计算机软件计算药物的特性参数,并结合模型药物的特性分析微乳增溶难溶性药物的机理.结果:微乳对药物的增溶效果远大于油相和胶束,并随药物的脂溶性和空间结构的改变而变化.结论:微乳可用于增溶难溶性药物,且脂溶性越大,空间位阻越小,增溶效果越明显. 相似文献
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十二烷基硫酸钠微乳体系的相行为及电导行为研究 总被引:1,自引:0,他引:1
目的 对十二烷基硫酸钠(SDS)/正庚烷/正丁醇/水体系微乳液的相行为和电导行为进行了研究.方法 用电化学方法测定了微乳体系的电导率.结果 体系在水滴定过程中均出现渗滤电导现象,温度升高,体系的电导率增大,表观活化能也增大,SDS微乳体系在pH2.5~11范围内具有良好的抗酸、碱性能.结论 通过电导率的测定可研究微乳体系的结构及结构转变. 相似文献
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Peptide drugs are increasingly becoming a very important class of therapeutic agents with the rapid advances in the field of biotechnology engineering. However, these drugs are generally not suitable for oral administration. In this review, the main physico-chemical and biopharmaceutical characteristics of peptides are summarized. The obstacles to peptide drug absorption and the different possibilities for solving these difficulties are listed. Results using this formulation approach for oral drug delivery of peptides are apparently promising with some specific peptides such as cyclosporin. Various mechanisms are only beginning to be understood and further investigations need to be performed in this area to explain the results obtained with some peptides. 相似文献
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Lingyun Xu Jinyuan Pan Qiyou Chen Qizhi Yu Huabing Chen Huibi Xu Yinsheng Qiu Xiangliang Yang 《Food and chemical toxicology》2008,46(12):3792-3799
Triptolide (TP) is a major active component of Tripterygium wilfordii Hook F (TWHF), which is used to treat rheumatoid arthritis (RA). TP has a narrow therapeutic window. To increase the therapeutic index of TP, a novel TP-loaded transdermal delivery system, named TP-loaded hydrogel-thickened microemulsion (TP-MTH), has been developed to treat RA. Our previous studies have demonstrated the good efficacy of TP-MTH in animals. This paper evaluated the safety of TP-MTH with several animals. Results demonstrated no obvious toxicities in a series of toxicity tests: acute toxicity study of TP-MTH (1.2 mg/kg) in rabbits, 6-month long-term toxicity study of TP-MTH (0.06, 0.18, 0.54 mg/kg) in rabbits, safety pharmacology study of TP-MTH (0.03, 0.09, 0.27 mg/kg, for 5 d) in mice and beagle dogs, skin irritation study in rabbits, and skin allergic reaction test in guinea pigs. Only mild reversible skin irritation signs were observed on the skin of animals. These studies suggest that topical TP-MTH is a promising drug formulation for the treatment of RA. 相似文献
10.
To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubility and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage. 相似文献