Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties

Objective: Aprepitant (APR) is a water insoluble drug approved for the treatment of chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV). The innovator Emend^® is a formulation incorporating drug nanoparticles with good bioavailability (~67%). The objective of the current work was to evaluate the feasibility of formulating a cyclodextrin complex of APR with enhanced solubility/dissolution rate and concomitantly bioavailability.

Methods: The complex was prepared using two approaches: kneading and slurry method. The formulated complex was evaluated using DSC, XRPD and FT-IR studies.

Results: DSC, XRPD and FT-IR studies confirmed the interaction of β-cyclodextrin with APR indicating formation of a true complex wherein the drug was encapsulated in the cyclodextrin cavity (inclusion phenomenon). In addition to inclusion complexation, non inclusion phenomenon viz., interaction among hydroxyl groups of cyclodextrin and APR was also observed. The saturation solubility and dissolution rate of drug complex was higher than that of aprepitant API. The rate (C_max) and extent of absorption (AUC) of APR from the complex were found to be comparable to that of Emend^® (Reference product).

Conclusion: These studies established that cyclodextrin complexation may provide another viable and cost effective option for enhancing solubility and bioavailability of APR.     

Preparation and study of light transmitting properties of sulfoaluminate cement-based materials

Polymethylmethacrylate (PMMA) optical fibers with two types of diameters were uniformly arranged in sulfoaluminate mortar by different methods. Light transmitting sulfoaluminate cement-based materials (LTSCM) were prepared. Optical and mechanical properties of LTSCM were studied. The compressive strength decreased linearly with increasing volume fraction of optical fiber in LTSCM. Compressive strength of specimen after 80 °C water bath was larger than that of specimen under standard curing conditions. According to CCD technology, brightness of optical fiber in different positions of LTSCM can be exhibited clearly. Light transmitting performance of LTSCM was tested by optical power method. Transmittance of specimen decreased with increasing spacing between the detector and specimen. Optical power increased with increasing number of fiber and with increasing diameter of fiber. Transmittance of fiber was weakened due to water bath at high temperature. Voids existed between the fiber and matrix.     

Molecular printboards on silicon oxide: lithographic patterning of cyclodextrin monolayers with multivalent, fluorescent guest molecules

Three compounds bearing multiple adamantyl guest moieties and a fluorescent dye have been synthesized for the supramolecular patterning of beta-cyclodextrin (CD) host monolayers on silicon oxide using microcontact printing and dip-pen nanolithography. Patterns created on monolayers on glass were viewed by laser scanning confocal microscopy. Semi-quantitative analysis of the patterns showed that with microcontact printing approximately a single monolayer of guest molecules is transferred. Exposure to different rinsing procedures showed the stability of the patterns to be governed by specific supramolecular multivalent interactions. Patterns of the guest molecules created at CD monolayers were stable towards thorough rinsing with water, whereas similar patterns created on poly(ethylene glycol) (PEG) reference monolayers were instantly removed. The patterns on CD monolayers displayed long-term stability when stored under N(2), whereas patterns at PEG monolayers faded within a few weeks due to the diffusion of fluorescent molecules across the surface. Assemblies at CD monolayers could be mostly removed by rinsing with a concentrated CD solution, demonstrating the reversibility of the methodology. Patterns consisting of different guest molecules were produced by microcontact printing of one guest molecule and specific adsorption of a second guest molecule from solution to non-contacted areas, giving well-defined alternating assemblies. Fluorescent features of sub-micrometer dimensions were written using supramolecular dip-pen nanolithography.     

Preparation of fluorescence ethosomes based on quantum dots and their skin scar penetration properties

In this study, the fluorescence ethosomes (ES-QDs) composed of hydrophilic CdTe fluorescent clusters (quantum dots, QDs) were prepared. The prepared ES-QDs with even particle size were obtained by extruding the vesicles through polycarbonate membrane filters and were characterized by TEM SEM HPPS and photoluminescence spectra. Their in vitro experiments to penetrate into human skin scar were performed by using the Franz diffusion cell. Results showed that the prepared ES-QDs not only have the properties of ethosome to penetrate the skin scar tissues but also have the fluorescence labeling properties of the quantum dots. The prepared ES-QDs have potential clinical application in therapy of skin scar.     

橡胶相尺度对亚微米或纳米橡胶颗粒填充环氧复合材料性能的影响

对比研究了由液体橡胶在环氧树脂中原位形成的亚微米橡胶/环氧复合材料和在环氧树脂中直接添加纳米橡胶颗粒形成的纳米橡胶/环氧复合材料的性能。研究表明：未固化混合物的黏度随着纳米橡胶相的加入逐渐增加,但随着亚微米橡胶相含量的增加而降低;橡胶/环氧复合材料的玻璃化转变温度随着纳米橡胶颗粒的加入逐渐增加,但随着亚微米橡胶相含量的增加而降低;两种橡胶相的添加均使复合材料的弹性模量降低,断裂延伸率增加;在较低含量时,纳米橡胶颗粒可以提高环氧的拉伸强度;两种橡胶填充的橡胶/环氧复合材料均显示出明显的增韧效果。微观形貌分析表明,两种橡胶均可以在应力作用下脱粘并促进裂纹尖端的塑性变形。     

含碳纳米管的新型抗静电纤维的制备和性能

将多壁碳纳米管分散在自制的抗静电载体PR-86中制备出新型、高效和耐久的抗静电母粒．抗静电母粒的添加量仅为0．5％就可以制备出性能优良的“基体-微纤”型抗静电PP纤维．该纤维的抗静电机理为异极性大分子放电机理．多壁碳纳米管的存在增强了微纤相的极化程度和抗静电母粒的抗静电效果．抗静电纤维的抗静电性具有耐久性．抗静电母粒对纤维的性能基本上没有影响．     

Study on preparation and characterization of MOF based lanthanide doped luminescent coordination polymers

Coordination polymers (metal–organic frameworks or MOFs) offer the opportunity for fine-tuning the luminescence behavior because of the possibility to entrap in the network pores molecules that can influence the lanthanide (Ln) emission. In this study, Zn (II) and polycarboxylate based MOFs were first pre-formed by solvothermal method, then considered as host-matrix for in situ doping of low-input concentration of Eu³⁺ and Tb³⁺ (two most commonly used lanthanides in life science assays), and afterwards lanthanide doped luminescent materials were synthesized. Different characterizations (X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM), Energy-Dispersive Spectroscopy (EDS)) were carried out to confirm accordingly MOF's crystallinity, the structure and chemical composition. The study on luminescent properties of the material has revealed an efficient energy transfer from the ligand excited states to the Eu³⁺ and Tb³⁺ f-excited states. With quite low input concentrations (8–15%) of doped rare earth ions, these complexes displayed intense emissions at room temperature and proved to be good candidates for red and green emitter luminescent materials. Generally, this design concept can be extended for the preparation of other rare earth coordination polymers.     

Mn掺杂TiO_2负载竹质活性炭纤维的制备及可见光光催化性能研究

采用溶胶-凝胶法和浸渍法制备Mn掺杂TiO2负载竹质活性炭纤维(Mn/Ti-BACF)光催化复合材料,利用扫面电镜(SEM)、X射线衍射仪(XRD)、傅立叶变换红外光谱(FT-IR)、紫外-可见光分光光度计(UV-Vis)等考察了Mn掺杂量对Mn/Ti-BACF复合材料结构和可见光光催化性能的影响。结果发现,Mn掺杂改善了TiO2在竹质活性炭纤维表面的负载;Mn离子的掺杂并没有改变样品基材的碳网结构,也未出现新的Mn—O的特征吸收峰。随着Mn掺杂浓度的增加,Mn/Ti-BACF样品中TiO2粒径逐渐减小,可见光下的吸光度先增加后减少。当n(Mn)∶n(Ti)=1∶200时,样品在可见光下对亚甲基蓝的降解率达到了97.7%。     

冠脉支架表面载药涂层的制备和性能

采用溶液聚合法制备了改性的聚甲基丙烯酸树脂,作为支架表面载药涂层的药物载体聚合物.采用浸涂法制备了不锈钢基体表面聚合物及聚合物载药涂层,并利用红外光谱及核磁共振波谱分析了所制备共聚物的成分,并评价了物理性能、生物稳定性能以及药物的释放性能.结果表明,所制备的涂层具有较好的生物稳定性,甲基丙烯酸和甲基丙烯酸丁酯的加入提高了聚合物的物理性能,尤其是涂层与金属基体的结合力所制备的药物释放涂层具有缓释紫杉醇的功能,其释放周期超过15 d.聚甲基丙烯酸树脂携带紫杉醇的载药涂层在生物稳定性、物理性能及药物释放性能方面满足冠脉支架的表面涂层的使用要求.     

新型咔唑-吲哚并咔唑共轭聚合物材料的合成与性能研究

通过Suzuki偶联聚合方式合成了两种基于咔唑和吲哚并咔唑的新型共轭聚合物材料.目标聚合物具有较高的分子量,良好的热性能和电化学氧化还原性能.通过对材料的光物理性能分析,所制备的共轭聚合物材料是一类具有潜在应用价值的纯正蓝色电致发光材料.     

可降解镁合金表面载药涂层的制备和性能

在可降解AZ31B镁合金心血管支架表面成功制备了携带雷帕霉素的聚乳酸-聚三亚甲基碳酸酯(PLA-PTMC)共聚物涂层,评价了涂层的表面形貌、降解性能、血液相容性和药物释放性能.结果表明,PLA-PTMC共聚物作为载药涂层具有良好的柔韧性,表面均匀、光滑,降解周期超过1个月,血液相容性良好.涂层具有缓释雷帕霉素的功能,释药周期超过1个月,可在内膜增生期内有效抑制支架植入后再狭窄的发生,满足冠脉支架表面载药层的使用要求.     

Mn、N共掺杂TiO_2负载竹质活性炭纤维的制备及可见光光催化性能

为研究Mn、N共掺杂TiO_2负载竹质活性炭纤维(Mn-N/TiO_2-BACF)的可见光光催化性能,首先,以MnSO_4·H_2O为锰源,尿素为氮源,采用溶胶-凝胶法制备了光催化复合材料Mn-N/TiO_2-BACF;然后,利用SEM、XRD及XPS等考察了煅烧温度对Mn-N/TiO_2-BACF结构和可见光光催化性能的影响。结果表明:Mn、N共掺杂使光催化复合材料的光响应范围由紫外光区域拓宽至可见光区域;随煅烧温度的提高,光催化复合材料表面的晶格氧含量逐渐降低,吸附氧含量先降低后增加,而羟基氧含量有所增加;光照400min后,350℃锻烧制备的Mn-N/TiO_2-BACF在可见光下对亚甲基蓝的光降解率达99.7%。同时,还发现Mn-N/TiO_2-BACF在可见光下的光降解率与煅烧温度没有相关性。     

碳毡电路模拟吸波复合材料的研究

分别研究了含矩形碳毡电路屏和“十”字形碳毡电路屏吸波复合材料的微波吸收特性，并对碳毡电路屏的吸波机理做了初步的探讨。结果表明，碳毡电路模拟吸波材料的吸波性能与电路屏阵列单元的结构和尺寸密切相关。矩形电路屏阵列单元中矩形缝隙的长或宽增大，材料的吸波性能提高；矩形缝隙之间的距离增加，材料的吸波性能降低。本实验条件下当矩形缝隙的长、宽和间距分别为24、12和6mm时，材料可获得8．56GHz的有效带宽和-25dB的最大反射衰减。“十”字形电路屏阵列单元中“十”字形缝隙的臂长或臂宽增大，材料的吸波性能提高；“十”字形缝隙之间的距离增加，材料的吸波性能降低。“十”字形缝隙的臂长、臂宽和“十”字形缝隙之间的距离分别为16、8和6mm时，材料的有效带宽7．2GHz，最大反射衰减-26．2dB。     

Preparation and performance of intermediate-temperature fuel cells based on Gd-doped ceria electrolytes with different compositions

In this work, the effect of two frequently used Gd_xCe_1−xO_2−x/2 electrolytes (x = 0.1 and x = 0.2) on the performance of fuel cells operated at intermediate temperature was studied. The microstructures of ceria electrolytes responsible for the performance were discussed. Electrochemical measurements of as-prepared cells showed that the cell with Gd_0.2Ce_0.8O_1.9 electrolyte had a better performance than that of Gd_0.1Ce_0.9O_1.95. It can be concluded that the increase of grain boundary conductivity of Gd_0.2Ce_0.8O_1.9 electrolyte contributes to its better cell performance.     

钛金属薄膜上两种短链自组装分子膜的制备与摩擦特性

采用自组装技术在钛金属薄膜上制备了两种分子链长相同、官能团不同的自组装分子膜,并对其进行了不同时间的紫外照射,对钛金属薄膜和自组装分子膜进行了表征和摩擦特性测试,研究了紫外照射、官能团、滑动速度和载荷对自组装分子膜摩擦特性的影响,结果表明:通过紫外照射钛金属薄膜表面羟基化、自组装分子水解及自组装分子缩合可在钛金属薄膜上制备结构致密的自组装分子膜,制备的两种短链自组装分子膜可降低钛金属薄膜的摩擦特性,APS自组装分子膜的摩擦特性优于MPS自组装分子膜的摩擦特性,紫外照射5 min的自组装分子膜表面吸附的有机杂质被蒸发掉,对针尖的黏着力减小,从而导致针尖的变形减小,摩擦力最低,而紫外照射15 min的自组装分子膜致密的网状结构被破坏,减弱了自组装分子膜的润滑效应,两种自组装分子膜的摩擦力随着滑动速度的增加略呈上升趋势,随着载荷的增加略呈下降趋势,但是变化不大.     

Preparation and mechanical properties of C/SiC composites with carbon fiber woven preform

C/SiC composites reinforced with multilayer carbon fiber woven preforms were fabricated by isothermal chemical vapor infiltration (ICVI) process. To characterize the mechanical properties of the composites, mechanical testing was carried out under various loading conditions, including tension, bending and shear loads. The results indicated that the composites, with superior intrinsic through-the-thickness properties, exhibited high in-plane mechanical properties. Therefore, the composites developed can well meet the demands of the reusable nose cap, i.e. the easiness of near-net shaping and the capability of withstanding multidirectional mechanical and thermal stresses.     

含C、Ge的Fe-Si-Mn基热电材料的电学性能

对掺C和Ge的Fe—Si—Mn基热电材料的电学性能研究表明，相对于未掺的Fe—Si—Mn基热电材料，掺C样品的电阻率降低，但热电动势率增加。掺Ge样品的电阻率有所升高，但热电动势率增加更快，因此掺C、Ge样品有较高的功率因子，比未掺样品提高近1倍。     

Benzene-induced hydro(solvo)thermal synthesis of Cu and Zn coordination polymers based on 1,3-benzenedicarboxylate

Hydro(solvo)thermal reactions of Cu(NO₃)₂·2.5H₂O or Zn(NO₃)₂·6H₂O with 1,3-H₂bdc provided two structurally different coordination polymers; a 2D network “metallacalixarene” based on the paddlewheel-type cluster with the formula [Cu(1,3-bdc)·H₂O]·H₂O (1) and a 3D framework [Zn(1,3-bdc)] (2), respectively. The use of a base was unnecessary in this synthesis; however, the presence of benzene played a crucial role in the crystallization of the desired products and could act as a template molecule in the synthesis of polymer (1). The unsaturated apical sites in the Cu₂ cluster of polymer (1) were occupied by water molecules, what consequently led to the structural decomposition of the framework after exposing the sample in air, which was not the case of the Zn-coordination polymer (2).     

Dramatic effect of dispersed carbon nanotubes on the mechanical and electroconductive properties of polymers derived from ionic liquids

Free-radical polymerization of an imidazolium ion-based ionic liquid bearing a methacrylate group, gelling with single-walled carbon nanotubes (SWNTs), allows fabrication of a mechanically reinforced, electroconductive soft material (bucky plastic). A film sample of this material displays an excellent conductivity of 1 S cm(-1) and a 120-fold enhancement of the Young's modulus at a 7 wt % content of SWNTs. The conductivity is temperature-dependent in the range 5-300 K, suggesting that the conductive process involves carrier hopping. Scanning electron and atomic force micrographs of a bucky plastic film display the presence of crosslinked networks consisting of finely dispersed SWNTs. Such nanotube networks, developed in the polymer matrix, likely suppress slipping of entrapped polymer molecules via a strong interfacial interaction and also facilitate intertubular carrier transport. Although a bucky plastic derived from a vinylimidazolium ion-based ionic liquid monomer shows a comparable conductivity to that of the methacrylate version, the film is brittle irrespective of the presence or absence of SWNTs.     

彩色双层复合镀膜玻璃的在线制备与性能

分别采用电化学方法和化学气相沉积法对生产线锡槽和退火窑内的浮法玻璃两次镀膜,制备出具有阳光控制功能的双层彩色浮法玻璃,采用分光光度计、扫描电镜、能谱仪、透射电镜、原子力显微镜和二次离子质谱等方法分析了复合镀膜样品的形貌．结构,研究了不同深度的膜层成分和性能．结果表明,可见光透射比与硅烷浓度和电流强度之间有强烈依赖性;上层的硅膜表面均匀平整,表面粗糙度约9．66nm,团粒尺寸约100nm,其厚度约70-78nm,且沿厚度方向呈梯度化氧化;底层膜中铜和铋的扩散深度约10μm．