Development,In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity

Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken as independent variables and their effects were evaluated on vesicle size (nm), entrapment efficiency (%, EE) and drug release (%, DR). Furthermore, optimized EZL-PNs (EZL-PNs-opt) formulation was evaluated for ex vivo permeation, pharmacokinetic and ulcer protection activity. Result: The EZL-PNs-opt formulation showed 616 ± 13.21 nm of vesicle size, and 81.21 ± 2.35% of EE. EZL-PNs-opt exhibited negative zeta potential and spherical confirmed scanning electron microscopy. EZL-PNs-opt showed sustained release of EZL (95.07 ± 2.10% in 12 h) than pure EZL dispersion. The ex-vivo gut permeation result exhibited a significantly (p < 0.05) enhanced flux than pure EZL. The in vivo results revealed 4.02-fold enhancement in bioavailability and 61.65% protection in ulcer than pure EZL dispersion (43.82%). Conclusion: Our findings revealed that EZL-PNs formulation could be an alternative delivery system of EZL to enhance oral bioavailability and antiulcer activity.     

Isolation and HPLC Quantitative Determination of 5α-Reductase Inhibitors from Tectona grandis L.f. Leaf Extract

Steroid 5α-reductase plays a crucial role in catalyzing the conversion of testosterone to dihydrotestosterone, which is involved in many androgen-dependent disorders. Leaf-hexane extract from Tectona grandis L.f. has shown promise as a 5α-reductase inhibitor. The objectives of this current study were to isolate and identify 5α-reductase inhibitors from T. grandis leaves and to use them as the bioactive markers for standardization of the extract. Three terpenoid compounds, (+)-eperua-8,13-dien-15-oic acid (1), (+)-eperua-7,13-dien-15-oic acid (2), and lupeol (3), were isolated and evaluated for 5α-reductase inhibitory activity. Compounds 1 and 2 exhibited potent 5α-reductase inhibitory activity, while 3 showed weak inhibitory activity. An HPLC method for the quantitative determination of the two potent inhibitors (1 and 2), applicable for quality control of T. grandis leaf extracts, was also developed. The ethanolic extract showed a significantly higher content of 1 and 2 than found in the hexane extract, suggesting that ethanol is a preferable extraction solvent. This study is the first reported isolation of 5α-reductase inhibitors (1 and 2) from T. grandis leaves. The extraction and quality control methods that are safe and useful for further development of T. grandis leaf extract as an active ingredient for hair loss treatment products are also reported.     

继电器动态过程中动态参数的测试方法

本文介绍了一种测试继电器在动态过程中动态参数测试的方法。采用此方法能直接测量和观察继电器动态过程中的线圈电压、电流 ,同时可测出继电器的动作时间 ,还可了解其接点在接触过程是否有振动现象存在。所以 ,此方法是一种多用途的继电器动态参数测量方法     

Stationary states of crystal growth in three dimensions

A new Markov process describing crystal growth in three dimensions is introduced. States of the process are configurations of the crystal surface, which has a terrace-edge-kink structure. The states are continuous along edges but discrete across edges, in accordance with the very different rates for the two types of captures of particles. Stationary distributions, describing steady crystal growth, are found in general. To our knowledge, these are the first examples of stationary distributions for layered crystal growth in three dimensions. The steady growth rate and other quantities are obtained explicitly for two interacting edges. For many interacting edges, growth behavior is determined (a) in various asymptotic regimes including thermodynamic limits, (b) via simulations, and (c) using series (cluster) expansions in the slope of the surface, the first three coefficients being computed. The theoretical growth rates show a marked dependence on surface dimensions. This may contribute to the size dependence and dispersion in the observed growth rate of small crystals.     

辐射在CH泡沫中传输的数值模拟

利用一维多群辐射输运程序对辐射在CH泡沫中的传输过程进行了数值模拟,给出一些细致的物理图像和定量结果。在一定的入射辐射流条件下,密度变化对辐射传输特征、辐射加热介质的热力学平衡弛豫过程有重要影响。随着密度下降,辐射由亚声速传输转变为超声速传输,辐射在传输过程中的能谱形状也不同。     

屯田余绪中的近世边疆社会嬗变—以1719至1949年间甘肃省金塔县水利事务为中心的研究

以公元1719至1949年间甘肃金塔县水利事务为主线,可以分析这一因屯田而兴起的边疆社会在两百余年间的演化特征。清代屯田时期,金塔县水利事务完全由政府控制,屯田结束后逐渐转向民间自行管理;但政府却出于对边疆地区民众领袖易引发社会不稳定的成见,刻意将士绅集团排斥于水利管理事务之外。民国时期随着外源性水利危机的爆发,向外部“争水”成为决定区域社会生死存亡的头等大事,政府转而支持士绅阶层积极“争水”,士绅由此控制了全县水利事务。“争水”成功的士绅阶层很快涣散并劣化,致使金塔内部水利逐渐废弛、社会矛盾重重,并非迫切的“对外争水”成为凝聚区域社会的唯一共识。从屯田到争水,金塔社会在近世大多数时间中始终为单一维度社会管制目标所牵引,并未走上繁荣、有序、富于活力的发展之路。这其中涉及政治、环境等复杂因素的交相作用,但自屯田时代所遗留的制度化要素扮演了重要角色。短时期的屯田活动,造就了长时期存在于边疆区域的“屯田社会”,其流风余绪影响至今。     

Inter-cell spectrum efficiency improvement technology

Improvement in inter-cell spectrum efficiency is a valuable research topic in mobile communication system, which affects cell edge user experience especially. According to current research results, there are three methods to deal with inter-cell interference to improve inter-cell spectrum efficiency, including inter-cell interference randomization, inter-cell interference cancellation and inter-cell interference coordination. This paper analyzes three important inter-cell spectrum efficiency improvement technologies, soft frequency reuse (SFR), uplink power control, and downlink coordinated multi-point transmission/reception (CoMP), and relative research progress.     

UPLC-MS-Based Metabolomic Study of Streptomyces Strain HCCB10043 Under Different pH Conditions Reveals Important Pathways Affecting the Biosynthesis of A21978C Compounds

The A21978C family of compounds includes precursors of daptomycin, an important antibiotic for the treatment of diseases infected by Gram-positive resistant bacteria. Focusing on these valuable compounds, the differences in metabolites obtained with or without pH control in their producing strain Streptomyces parvus HCCB10043 were investigated by comparative metabolomics analysis based on UPLC-TOF-MS technology. According to principal component analysis, there were fourteen biomarker compounds selected under the two pH culture conditions. The ten known compounds were divided into two types: a glycoside family participating in the primary metabolism (daidzein, glycitein, genistein, and soyasaponin Bb) and a peptide family of secondary metabolites (valistatin, bestatin, 3-amino-2-hydroxy-4-phenylbutanoylvalylisoleucine, and arylomycins A2, A4, and A5). Through orthogonal partial least squares-discriminant analysis, three compounds, soyasaponin Bb and arylomycins A2 and A4 were identified as the most relevant compounds to A21978C1-3 production, the glycolytic pathway, and the NRPS synthesis pathway. The competitive relationship between arylomycin and A21978C was verified. These results have demonstrated the usefulness of the metabolomic strategy based on UPLC-MS in studying significant metabolic changes in actinomycetes. Moreover, this metabolomic strategy can provide new ideas and guidance for the regulation and improvement of secondary metabolites production.     

Broadband excitation pulses for high‐field solid‐state nuclear magnetic resonance spectroscopy

In nuclear magnetic resonance spectroscopy, experimental limits due to the radiofrequency transmitter and/or coil means that conventional radiofrequency pulses (“hard pulses”) are sometimes not sufficiently powerful to excite magnetization uniformly over a desired range of frequencies. Effects due to nonuniform excitation are most frequently encountered at high magnetic fields for nuclei with a large range of chemical shifts. Using optimal control theory, we have designed broadband excitation pulses that are suitable for solid‐state samples under magic‐angle‐spinning conditions. These pulses are easy to implement, robust to spinning frequency variations, and radiofrequency inhomogeneities, and only four times as long as a corresponding hard pulse. The utility of these pulses for uniformly exciting ¹³C nuclei is demonstrated on a 900 MHz (21.1 T) spectrometer. Copyright © 2012 John Wiley & Sons, Ltd.