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白菊玲 《合成材料老化与应用》2020,49(2):116-119
葫芦脲又名瓜环,属大环家族中的重要成员,是第四代新型超分子大环主体化合物。葫芦脲化合物是具有外亲水、内疏水的高度对称的葫芦状结构,具有选择性络合金属离子、中性分子的能力,故用途广泛。该文简要介绍了葫芦脲化学的产生、发展、应用及结构特征。详细综述了:(1)新型葫芦脲衍生物的合成及应用;(2)新型瓜环衍生物的合成及应用。并对葫芦脲化学的发展进行了展望。 相似文献
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《化学推进剂与高分子材料》2017,(3):62-67
综述了以葫芦脲为主体的超分子水凝胶的最新研究进展,包括不同客体分子的设计及合成,不同新型超分子水凝胶的自组装,简述了其在材料学、环境学及药物释放等方面的应用。 相似文献
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有序孔结构功能与应用广泛,但长期以来对有序孔结构研究局限于固态。总结了水溶性的有序自组装孔结构-超分子有机框架(Supramolecular Organic Frameworks,SOFs)的研究进展,内容包括相关超分子化学和分子自组装研究的发展背景、有孔超分子聚合物的构建及有序性控制研究背景、不同拓扑结构的超分子有机框架的组装及其催化和药物输送功能探索(主要通过疏水作用驱动的葫芦脲[8]对两个同体或异体芳香二聚体的包结作用。展望了水溶性有序超分子孔结构的研究前景。 相似文献
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分别综述了以葫芦[7]脲与盐酸黄连素、盐酸巴马汀、黄连碱包结配合物为荧光探针的药物分析原理、方法及研究进展。 相似文献
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空心多孔纳米载体负载药物的药量分布研究 总被引:3,自引:0,他引:3
药物活性成分负载于空心多孔纳米载体材料上时,既可分布在载体的孔道和空腔内部,即内部载药(DI,Drug Inside),也可存在于载体的外部表面区域,即外部载药(DO,Drug Outside).了解DI与DO的分布情况,对于进一步改善载药技术,研究和控制药物剂型的缓释性能,提高药物的利用率等都具有很重要的意义.今提出采用热重分析和溶出实验相结合的方法,先由热重分析测出载体的整体载药量,再根据内部载药(DI)和外部载药(DO)不同的溶出特性,即外部载药可全部快速释放而内部载药是在外部载药溶解后才缓慢溶出,来确定外部载药(DO)量,并最终确定DI/DO值.此外还探讨了载药分子和载药方式对DI/DO的影响,结果表明:小分子药物能更快进入纳米空心载体的内腔,具有更高的DI/DO值,因此根据载体选择药物或根据药物设计载体是制备药物控释剂的一个要素;与直接浸渍工艺相比,超临界包埋法可得到较大的整体载药量,且DI/DO值更大,缓释性能好,但操作成本也比较大,因此权衡性能指标和经济因素来选择载药方法也是制备控释剂所需要考虑的因素之一. 相似文献
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综述了近年来生物降解聚合物药物微球的制备方法。随着药剂学的不断发展,传统的载药体系已经不能满足其需求。因此出现了许多新型的具有不同功能特性的药物载体。生物降解聚合物微球由于其结构组成可设计,并具有良好的安全性、生物相容性和生物降解性,可用作药物控释载体、表面改性、支架材料等,在生物医学领域获得了广泛的重视和应用。 相似文献
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Deng‐Guang Yu Xiao‐Fei Zhang Xia‐Xia Shen Chris Brandford‐White Li‐Min Zhu 《Polymer International》2009,58(9):1010-1013
BACKGROUND: Drug‐loaded electrospun ultrafine fibers have the advantages of both nanoscale drug delivery systems and conventional solid dosage forms. To improve the control of drug release, the combined use of electrospinning and pharmaceutical polymers has attracted increasing interest recently. RESULTS: Ultrafine drug‐loaded polyvinylpyrrolidone fibers were successfully prepared using an electrospinning process with ibuprofen as the active pharmaceutical ingredient and polyvinylpyrrolidone K30 as the filament‐forming polymer. The analytical results from scanning electron microscopy, differential scanning calorimetry and Fourier transform infrared spectroscopy indicated that the drug had good compatibility with the polymer and that the drug was well distributed in the ultrafine fibers as an amorphous physical form. In vitro dissolution tests showed that the fiber mats were able to dissolve within 10 s through a polymer‐controlled mechanism. CONCLUSION: The fast dissolution of drug‐loaded fibers may lead to applications that improve dissolution rates of poorly water‐soluble drugs, or that involve the preparation of oral fast‐dissolving drug delivery systems. Copyright © 2009 Society of Chemical Industry 相似文献
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Temperature-sensitive hydrogels are attracting increasing attention for controlled drug delivery. However, achieving high drug loadings and sustained drug release remains challenging. Herein, we describe the successful synthesis of a series of novel temperature-sensitive poly(N-isopropylacrylamide) (PNIPA)/mesoporous silica nanoparticles (MSN) hydrogels by physical crosslinking of NIPA with MSN. The external and internal structures, temperature sensitivity, drug-loading capacity, and blood compatibility of the PNIPA/MSN composite hydrogels are studied. Results show that MSN addition improved the network structure and adjusted the size of the hole, MSN could also act as drug carrier, thereby enhancing the drug loading capacity. The composite hydrogels underwent a phase transition at 33.7 °C (at the lower critical solution temperature). The hemolysis rate of the composite hydrogels was less than 1%, thus they can be classified as a nonhemolytic materials with good biocompatibility. The composite hydrogels reported here thus have great potential in drug transport and temperature-activated drug release. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48391. 相似文献
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药物晶型可显著影响药品质量、安全性和有效性,国家"医药工业十二五发展规划"将药物晶型研究列为提升药物质量安全的主要任务和重点技术。本文介绍了药物多晶型的溶解度行为以及晶型转化的液相和固相介导机理,溶剂、添加剂/模板剂对药物晶型的控制有着重要的作用,而物理场效应(超声波、微波、超重力场等)对晶型转化过程起强化效应;过程分析技术的快速发展为晶型转化机理的研究以及过程优化、控制提供了先进手段。未来药物晶型转化与控制的研究将聚焦分子的组装与调控行为、过程分析以及药物的构效关系等方面。 相似文献
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Design,Synthesis, and in vitro Evaluation of Multivalent Drug Linkers for High‐Drug‐Load Antibody–Drug Conjugates 下载免费PDF全文
Dr. Bo Chen Dr. Diego A. Gianolio Dr. James E. Stefano Charlene M. Manning Dr. Richard C. Gregory Michelle M. Busch Dr. William H. Brondyk Dr. Robert J. Miller Dr. Pradeep K. Dhal 《ChemMedChem》2018,13(8):790-794
A series of novel multivalent drug linkers (MDLs) containing cytotoxic agents were synthesized and conjugated to antibodies to yield highly potent antibody–drug conjugates (ADCs) with drug/antibody ratios (DARs) higher than those typically reported in the literature (10 vs. ≈4). These MDLs contain two copies of a cytotoxic agent attached to biocompatible scaffolds composed of a branched peptide core and discrete polyethylene glycol (PEG) chains to enhance solubility and decrease aggregation. These drug linkers produced well‐defined ADCs, whose DARs could be accurately determined by LC–MS. Using this approach, ADCs with significantly lower aggregation and higher DAR than those of conventional drug linker design were obtained with highly hydrophobic cytotoxic agents such as monomethyldolastatin 10 (MMAD). The in vitro potencies of the MDL‐derived conjugates matched that of ADCs of similar DAR with conventional linkers, and the potency increased proportionally with drug loading. This approach may provide a means to prepare highly potent ADCs from a broader range of drugs, including those with lower cytotoxicity or poor solubility, which otherwise limits their use for antibody–drug conjugates. This may also provide a means to further improve the potency achievable with cytotoxins currently used in ADCs. 相似文献
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可降解高分子药物控释系统通过对药物剂量的有效控制,能够降低药物的毒副作用,提高药物的稳定性和利用率。近年来,静电纺丝纳米纤维因其具有比表面积大等特点,作为新型药物控制释放载体受到研究者的广泛关注。本文综述了可降解高分子纳米纤维药物控释系统的研究进展,对可降解高分子纳米纤维的制备及其在药物控释方面的研究进行介绍,并讨论了影响可降解高分子纳米纤维药物释放的因素。 相似文献