Fast Melt Cocoa Butter Tablet: Effect of Waxes,Starch, and PEG 6000 on Physical Properties of the Preparation

A fast melt tablet (FMT) is well regarded as an alternative delivery system that might help resolve a patient’s non-compliance issue. The main objective of this study was to develop a cocoa butter-based FMT. Additives, namely 5–15% of PEG 6000, beeswax, paraffin wax, and corn starch, were incorporated into the cocoa butter-based FMT to study the effects of these additives with the physical characteristic of a cocoa butter FMT. An optimum-based formulation was chosen according to the desired hardness and disintegration time and the taste masking property achieved with the model drug—dapoxetine. The analysis demonstrated that incorporating beeswax (15%) and paraffin wax (15%) could prolong the disintegration time by at least two-fold. On the contrary, the presence of corn starch was found to cause an increase in the hardness and reduction of the disintegration time. The disintegration mechanism might be presumed due to the synergistic effect of starch swelling and cocoa butter melting. The hardness value and in vitro disintegration time of the optimum formulation were recorded at 2.93 ± 0.22 kg and 151.67 ± 6.98 s. In terms of dissolution, 80% of dapoxetine was released within 30 min and the dissolution profile was comparable to the innovator product. The formulation was palatable and stable for at least 1 year. The exposure of the FMT formulation at 30 °C for 12 months was reported to be stable. Along with the sound palatability profile and high drug load capacity, the current formulation possesses the desired characteristics to be scaled up and marketed.     

双联齿轮断裂分析

机床传动系统双联直齿轮投入运行不久即发生齿面断裂事故,造成较大经济损失.传动系统所用双联齿轮未达到设计使用寿命,属于早期断裂失效.对现场收集到的断裂齿轮残块进行化学成分分析和硬度测试,对齿廓工作面及断裂形成的断口用扫描电镜进行微观观察,对齿轮残块上出现的裂纹用光学金相显微镜观察其形貌和微观特征,依据检测实验数据和结果,...     

Rational Exploration of N‐Heterocyclic Carbene (NHC) Palladacycle Diversity: A Highly Active and Versatile Precatalyst for Suzuki–Miyaura Coupling Reactions of Deactivated Aryl and Alkyl Substrates

As less attention has been focussed on the design of highly efficient palladium precatalysts to ensure the smooth formation of the active catalyst for metal‐mediated cross coupling reactions, we herein demonstrate that combining the bulky N‐heterocyclic carbene (NHC) 1,3‐bis(2,6‐diisopropylphenyl)imidazol‐2‐ylidene (IPr) with cyclopalladated acetanilide as the optimal palladium precatalyst leads to superior catalytic activity compared with the state‐of‐the‐art NHC–Pd catalysts. The complex was discovered through the evaluation of a small, rationally designed library of NHC–palladacycles prepared by a novel, practical and atom‐economic method, the direct reaction of IPr?HCl with palladacycle acetate dimers.     

Effect of La2O3 on a Precipitated Iron Catalyst for Fischer-Tropsch Synthesis

A series of La₂O₃-promoted precipitated iron catalysts (100Fe/2.8Si/nLa, n = 0, 0.5, 1, 2, and 4, atomic ratio) were prepared and characterized by in situ X-ray diffraction, CO temperature-programmed reduction, and N₂ adsorption-desorption. The catalytic performance for Fischer-Tropsch synthesis was studied in a fixed-bed reactor. It was found that the addition of a small amount of La₂O₃ (La/Fe ≤ 0.01) gave a large decrease in the particle size of Fe₂O₃, which increased the specific surface area and dispersion of the catalysts. This also favored the formation of iron carbides, which gave a high catalytic activity in Fischer-Tropsch synthesis. With increasing La₂O₃ content (La/Fe ≥ 0.02), a high La₂O₃ coverage and the formation of a LaFeO₃ compound decreased the formation of iron carbides, and the reaction activity decreased. The optimum La₂O₃ content was La/Fe = 0.01. The addition of La₂O₃ increased the selectivity for methane and suppressed the formation of C₅₊ hydrocarbons.     

Fast and Sensitive HPLC-ESI-MS/MS Method for Etoricoxib Quantification in Human Plasma and Application to Bioequivalence Study

Etoricoxib is a non-steroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation. The objective of the current study was to develop a sensitive, fast and high-throughput HPLC-ESI-MS/MS method to measure etoricoxib levels in human plasma using a one-step methanol protein precipitation technique. A tandem mass spectrometer equipped with an electrospray ionization (ESI) source operated in a positive mode and multiple reaction monitoring (MRM) were used for data collection. The quantitative MRM transition ions were m/z 359.15 > 279.10 and m/z 363.10 > 282.10 for etoricoxib and IS. The linear range was from 10.00 to 4000.39 ng/mL and the validation parameters were within the acceptance limits of the European Medicine Agency (EMA) and Food and Drug Analysis (FDA) guidelines. The present method was sensitive (10.00 ng/mL with S/N > 40), simple, selective (K prime > 2), and fast (short run time of 2 min), with negligible matrix effect and consistent recovery, suitable for high throughput analysis. The method was used to quantitate etoricoxib plasma concentrations in a bioequivalence study of two 120 mg etoricoxib formulations. Incurred sample reanalysis results further supported that the method was robust and reproducible.     

对镶在圆柱障板上单块有限复合板散射近场的研究

本文提出了预测镶在圆柱障板上一块具有三层加筋结构的复合材料有限板的振动特性和近场散射特性的理论模型。研究了在密介质中振动系统和入射声场的互作用以及不同振动之间由于辐射场引起的互耦合作用,数值计算了简支镶嵌在圆柱障板上的单块有限复合板的各种振动模式自耦合和互耦合系数,计算分析了有限复合板的振动再辐射近场特性。设计进行了测定有限复合板系统的近场实验。实验结果与理论计算结果符合较好。     

采用PID算法实现EMBCCD的精确制冷控制

EMBCCD(Electron Multiplying Back Illuminated CCD)在较稳定的低温环境中工作时可以有效地提高其图像信噪比。针对这个问题设计了相应的PID控制算法,包括PID参数的计算和处理策略、PID算法的实现过程和对EMBC-CD进行精确制冷控制的调试方法。实验结果表明,PID算法可以将温度控制在-10.5℃,精度为±0.5℃,达到了控制目的。     

Self‐Assembly of Highly Stable Zirconium(IV) Coordination Cages with Aggregation Induced Emission Molecular Rotors for Live‐Cell Imaging

The self‐assembly of highly stable zirconium(IV)‐based coordination cages with aggregation induced emission (AIE) molecular rotors for in vitro bio‐imaging is reported. The two coordination cages, NUS‐100 and NUS‐101, are assembled from the highly stable trinuclear zirconium vertices and two flexible carboxyl‐decorated tetraphenylethylene (TPE) spacers. Extensive experimental and theoretical results show that the emissive intensity of the coordination cages can be controlled by restricting the dynamics of AIE‐active molecular rotors though multiple external stimuli. Because the two coordination cages have excellent chemical stability in aqueous solutions (pH stability: 2–10) and impressive AIE characteristics contributed by the molecular rotors, they can be employed as novel biological fluorescent probes for in vitro live‐cell imaging.     

对碘酚对鲁米诺化学发光增强的试验研究

本文报道了由过氧化物酶催化鲁米诺与过氧化氢发光反应的增强发光研究。合成了增强剂对碘酚,并用对碘酚对鲁米诺与过氧化氢发光反应的光增强作用进行了试验,已经证实增强发光反应可将过氧化物酶的最低检测浓度降低到10-12～10-13mol/L水平。