环糊精包合物在医药方面的研究简介

本文介绍了环糊精,环糊精的包合作用,环糊精包合物的特征、意义以及其应用前景。同时,着重对环糊精包合物在医药研究方面的具体实例进行了介绍,如:阿莫西林、丁吡吗啉、利福平、阿魏酸等药物制备的环糊精包合物。     

β-环糊精包合物的研究进展

β-环糊精(β-CD)是一类环状低聚糖,价格低廉且易得,因有独特的空腔结构而常被当作宿主分子,与其他物质形成包合物。β-环糊精包合物常被作为一种药物制剂的中间体,可大量用于增加药物溶解度、提高稳定性、液体药物固体化、降低刺激性等。β-环糊精包合物也在食品和化妆品领域应用广泛。综述了β-环糊精包合物包合条件、影响因数及应用,并在β-环糊精包合物应用前景进行了展望。     

β-环糊精包合技术及应用的研究进展

β-环糊精包合物的制备、结构、性质和应用研究日益广泛.本文对环糊精包合物的制备方法、环糊精包合物的应用进行了综述.     

几种抗结核杆菌包合物的制备与活性研究

以β-环糊精为药物载体,采用饱和水溶液法制备了吡嗪酰胺-β-环糊精包合物、异烟肼-β-环糊精包合物、异烟肼利福霉素腙-β-环糊精包合物,采用冷冻干燥法制备了胸腺五肽-β-环糊精包合物。吡嗪酰胺与β-环糊精的最佳包合工艺条件为:吡嗪酰胺与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.03 h,此条件下的综合评价为96.18%。异烟肼与β-环糊精的最佳包合工艺条件为:异烟肼与β-环糊精物质的量比1.5∶1、包合温度30℃、包合时间0.5 h,此条件下的综合评价为87.80%。异烟肼利福霉素腙与β-环糊精的最佳包合工艺条件为:异烟肼利福霉素腙与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.08 h,此条件下的综合评价为90.83%。胸腺五肽与β-环糊精的最佳包合工艺条件为:胸腺五肽与β-环糊精物质的量比1.5∶1、包合温度70℃、包合时间1.15 h,此条件下的综合评价为90.03%。包合后药物的水溶解性和热稳定性得到明显改善,具有较好的抗结核杆菌活性。     

环糊精包合物的研究进展

20世纪70年代初到现在,环糊精化学的研究进入了鼎盛时期,随着经济的不断发展,环糊精包合物的研究越来越广泛,在许多方面都表明出其具有独特的作用。环糊精包合物的制备、表征和应用研究一直是环糊精化学的重要内容。文章主要介绍了环糊精包合物在制备时常采用的三种方法,以及对其表征时常采用的方法进行一定的阐述,详细概括了环糊精包合物的形成因素,并对于环糊精的包合物在今后的应用以及展望进行了讨论。     

沙喹那韦环糊精包合物的制备研究

目的:制备沙喹那韦β-环糊精包合物并考察其溶解度。方法:用相溶解度法判断沙喹那韦与β-环糊精形成包合物的摩尔比,通过有机溶剂蒸发法制备沙喹那韦β-环糊精包合物,用红外光谱(IR)对包合物进行鉴定。结果:沙喹那韦与β-环糊精形成包合物的摩尔比为1∶1,采用有机溶剂挥发法得到白色疏松固体。经IR鉴定,包合物已经形成,包合物能显著提高沙喹那韦的溶解度。结论:β-环糊精能够与沙喹那韦形成包合物,提高后者的溶解度。     

氯菊酯-β-环糊精包合物的制备及表征

为了开发具有药物缓释性能的新型防蚊试剂,用饱和水溶液法制备了氯菊酯与β-环糊精的超分子包合物(包合比为1∶1),并通过物相分析、红外光谱、紫外光谱及荧光光谱等分析方法对其进行了表征。结果表明,包合物与反应前物质及物理混合物相比,呈现出了新的物相性质,均匀的水包油结构及在多种溶剂中的溶解度明显降低证明了包合物的形成;氯菊酯-β-环糊精包合物是一种靠疏水作用和分子间力结合的超分子结构,包合过程没有新的化学键产生;包合对氯菊酯的结构没有产生影响,但其紫外吸收与荧光强度明显增强。     

硫酸亚铁-β-环糊精包合作用的研究

采用饱和水溶液法制备硫酸亚铁-β-环糊精包合物,紫外分光光度法表征了包合物的形成,并用循环伏安法进一步证实β-环糊精和硫酸亚铁的主客体包合作用。最后采用紫外分光光度法确定了硫酸亚铁-β-环糊精包合物的包合比,并测定了包合物的包合常数,结果表明,β-环糊精与硫酸亚铁可形成包合物,包合比为1：1,包合常数为57．74L/mol。     

格列吡嗪-β-环糊精包合物的制备及其理化性质考察

研究了格列吡嗪 β 环糊精包合物的制备方法,考察了包合物的理化性质。通过实验优化了格列吡嗪 β 环糊精包合物的制备工艺,确定n(格列吡嗪)∶n(β 环糊精)=1∶2,包合时间为8h;制得产物的包合率为91 73%。HPLC图谱显示,格列吡嗪被β 环糊精包合前后的主成分没有发生变化,包合物的DSC图谱和X射线粉末衍射图谱与格列吡嗪、格列吡嗪 β 环糊精混合物的图谱具有显著性差异。格列吡嗪包合物的溶解度是格列吡嗪的10倍,体外溶出速率有显著提高。实验表明,格列吡嗪被β 环糊精包合后呈现出新的物相特征,与格列吡嗪相比其理化性质有显著的改变。     

抗肿瘤天然产物与环糊精包合物的研究进展

随着生物制药、食品工业的不断发展,抗肿瘤天然产物与环糊精包合物的研究成为超分子化学的研究热点。本文对抗肿瘤天然产物与环糊精包合物的应用进行综述,发现抗肿瘤天然产物与环糊精形成包合物后,其水溶性差这个缺点都得到了解决。因而,扩大了其在临床上的应用范围。同时希望通过制备抗肿瘤天然产物/环糊超分子体系,可制得水溶性高、药物活性高和毒性低的抗肿瘤天然产物药物制剂,为其今后在医药方面的应用提供参考。     

环糊精包合手性分子的新进展

介绍了环糊精的结构特征及包合性能,环糊精包合手性分子的新进展。重点综述了近几年各类环糊精的包合作用在医药、生命科学及材料科学等领域的新应用,展望了其广阔的前景,期望能在医药学、生命科学及材料科学的应用上更有意义。     

环糊精及其包合物的研究与应用

介绍了环糊精及其包合物的合成、结构、包合物形成的热力学与动力学等的研究概况，着重叙述了环糊精的包合作用与环糊精的修饰，描绘了环糊精化学的应用与发展前景。     

侧链含有环糊精的聚合物的研究进展

聚合物侧链可通过化学键及分子间力与环糊精相互作用。当聚合物侧链通过化学键与环糊精作用时,环糊精空腔一般为空,可与小分子包合,对不同立体结构的分子具有选择性,在分析化学方面具有潜在的应用。当聚合物侧链与环糊精包合时,环糊精空腔与一定结构的侧链包合,形成侧链型多聚(准)轮烷。侧链型环糊精基多聚(准)轮烷的结构、性能独特,在许多领域具有潜在的应用。本文介绍了国内外文献中关于侧链含有环糊精的聚合物的研究进展,包括合成方法以及在各领域的应用等。     

Equalizing effect of β‐cyclodextrin on dyeing of polyamide 6,6 woven fabrics with acid dyes

Cyclodextrins (CD) are produced from starch by the action of cyclodextrin glycosyltransferase (CGTase) enzyme. Structurally, cyclodextrins consist of 6, 7, or 8 (α, β, and γ cyclodextrins, respectively) D‐glucopyranosyl units connected by α‐(1,4) glycosidic linkages. Having polar and hydrophilic outer sides and hydrophobic cavitation gives cyclodextrins a chance to form inclusion complexes with dyes in hydrophilic mediums. In this research, the equalizing effect of β‐cyclodextrins in dyeing of polyamide 6,6 woven fabrics with 6 different acid dyes were investigated. From the experimental results, it was determined that the β‐cyclodextrin shows a retarding and equalizing effect in dyeings carried out with the dyes that show interaction with β‐CD. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 103: 2660–2668, 2007     

表面张力法测定环糊精与表面活性剂包结常数的几种数值处理方法

表面张力法是研究环精精与表面活性剂相互作用的有力工具,用表面张力--表面活性剂浓度（γ－Ｃ）曲线来计算包结化合物的形成常数是可行的。本介绍了六种用表面张力法计算环糊精－表面活性剂包结化合和形成常数的数值处理方法。     

High‐Pressure 31P{1H} NMR Studies of RhH(CO)(TPPTS)3 in the Presence of Methylated Cyclodextrins: New Light on Rhodium‐Catalyzed Hydroformylation Reaction Assisted by Cyclodextrins

The effect of methylated cyclodextrins on the RhH(CO)(TPPTS)₃ complex in hydroformylation conditions [50 atm of CO/H₂ (1/1) and 80 °C] has been investigated by high‐pressure ³¹P{¹H} NMR spectroscopy. In the presence of methylated β‐cyclodextrin, the equilibria between the rhodium species lie in favor of phosphine low‐coordinated rhodium species. The formation of a stable inclusion complex between this cyclodextrin and the trisulfonated triphenylphosphine ligand (TPPTS) was found to be the key to understanding the displacement of the equilibria. Indeed, the methylated α‐cyclodextrin which does not interact with the TPPTS and the methylated γ‐cyclodextrin which can weakly bind to the TPPTS have no and a very low effect on the equilibria, respectively. These results explain for the first time why a decrease in the normal to branched aldehydes ratio is always observed when cyclodextrins are used as mass‐transfer agents in aqueous biphasic hydroformylation processes.     

Surface treatments on Tencel fabric: Grafting with β‐cyclodextrin

Tencel is a cellulosic fabric obtained from wood pulp that is very similar to natural cotton. For its potential performances to be expanded, Tencel needs to be processed in different ways. The ability of cyclodextrins to include hydrophobic molecules, such as fragrances, antimicrobial agents, and other chemicals, can be exploited to produce new grafted textiles with peculiar performances. We report studies on the grafting of acrylamidomethylated β‐cyclodextrin and monochlorotriazinyl‐β‐cyclodextrin to Tencel and on the inclusion of different molecules in the free cavities of cyclodextrins. The physicochemical properties and performances of the untreated and treated fabric have been determined with differential scanning calorimetry, ultraviolet–visible spectra, X‐ray diffractometry, and breaking load loss, aroma, and antimicrobial finishing tests. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 88: 706–715, 2003     

Extraction of toluene,o-xylene from heptane and benzyl alcohol from toluene with aqueous cyclodextrins

The separation of aromatic compounds (toluene and o-xylene) from heptane and of benzyl alcohol from toluene with aqueous solutions of cyclodextrins has been experimentally investigated, because cyclodextrins and its derivatives can selectively incorporate several organic compounds, whereas the separation of the aqueous solution of complexed cyclodextrins from the organic feed is simple. Cyclodextrins are not soluble in organic liquids, but cyclodextrin derivatives are highly soluble in water. Hydroxypropyl-β-cyclodextrins with different degrees of substitution and methylated β-cyclodextrin were selected for the extraction of toluene and o-xylene from heptane. Hydroxypropyl-β-cyclodextrin (two different substitution degrees) and hydroxypropyl-α-cyclodextrin were selected for the extraction of benzyl alcohol from toluene. The liquid–liquid distribution experiments were carried out at room temperature. Toluene and o-xylene form 1:1 complexes with different cyclodextrins and heptane can form 1:1 to 1:3 complexes. Benzyl alcohol forms 1:3 complexes with hydroxypropylated cyclodextrins. The models developed describe the experimental data reasonably well, considering the large deviations in the analyses.Aqueous cyclodextrin solutions are not feasible for the separation of aromatic components from aliphatic hydrocarbons, due to low distribution ratios of toluene (0.05) and o-xylene (0.023) between the aqueous and organic phase. With high distribution ratios of benzyl alcohol, between 0.3 and 2.2 depending on the CD concentration (at a solvent-to-feed ratio of 1) and a benzyl alcohol/toluene selectivity of at least 100, aqueous hydroxypropylated cyclodextrin solutions have sufficient potential for extracting benzyl alcohol from toluene.     

Synthetic membranes containing schardinger cyclodextrin additives

The permeation characteristics of the isomers of such aromatics as dichlorobenzenes, nitrochlorobenzenes, xylenes, etc., through a Methocel HG membrane containing various amounts of Schardinger α-cyclodextrin and β-cyclodextrin additives were measured in liquid/liquid dialysis and pervaporation experiments. The results showed that the cyclodextrins are able to selectively mediate molecular transport through the Methocel HG membranes. In general, increased membrane selectivity and a decrease in permeation rates were observed. Permeation rates for some aromatic compounds were decreased several hundred times with only 25% amounts of additive cyclodextrins in the Methocel HG membranes. Concentration electrical potential and bi-ionic electrical potential in membranes containing the Schardinger cyclodextrin have been measured and also show that the cyclodextrins are able to induce ion transport selectively through nonionic membranes. Dynamic mechanical properties of Methocel HG membranes containing cyclodextrins suggest these additives to be antiplasticizing agents. A mechanism for the modification of the intrinsic membrane permeation properties by cyclodextrin additive involving antiplasticizing action by the additives plus induced tortuous diffusion, where the latter is a result of specific interactions between the cyclodextrin additive and the permeating molecules, is proposed.     

环糊精包合作用组装大分子网络

利用环糊精的包合作用可以组装构筑大分子网络体系.这种独特的组装方法交联模式简单、交联度易于调控,得到的网络体系既能为聚合物的缔合理论提供理想的实验模型,又能广泛用于黏度调节和药物控释.环糊精的独特结构及对多种客体分子的包合作用使其近年来成为分子组装研究的热点.本文综述了以环糊精包合作用构筑大分子网络的研究进展,分别介绍了链状大分子组装交联和环糊精分子管道结晶缔合这两种方法.