Synthesis and Spectral Characterization of Related Substances of Vardenafil,an Erectile Dysfunction Drug

Abstract

Vardenafil hydrochloride trihydrate (Levitra) is used to treat erectile dysfunction (ED) and is an inhibitor of phosphodiesterase type 5 (PDE-5) enzyme. It maintains higher levels of cyclic guanosine monophosphate (cGMP), relaxes smooth muscles, promotes penile blood flow, and enhances erectile function. During the bulk drug synthesis of vardenafil hydrochloride trihydrate, six related substances (impurities), vardenafil dimer, vardenafil N-oxide, vardenafil glycene, vardenafil oxopiperazine, vardenafil oxoacetic acid, and phenyl vardenafil were identified, and these are reported herein for the first time. The present work describes the synthesis and characterization of these impurities.     

心脏外科手术后脑梗死患者的影像学特点及相关因素分析

本文对心脏外科手术后脑梗死患者的影像学特点及发生脑梗死的相关因素进行探讨。选取本院心脏外科手术患者286例作为研究对象,术后34例发生脑梗死,按照手术方式的不同将脑梗死患者分为体外循环组(11例)和非体外循环组(23例),比较两组术后脑梗死的影像学特点,并对心脏外科手术后脑梗死的影响因素进行分析。研究发现,两组穿支梗死、分水岭梗死、多发梗死、陈旧梗死的发生率比较,差异无统计学意义(P>0.05);体外循环组皮层梗死的发生率明显低于非体外循环组,体外循环组大面积梗死、双侧梗死的发生率明显高于非体外循环组,差异有统计学意义(P<0.05)。经单因素分析,性别、空腹血糖、TC、TG、LDL-C、Hcy、吸烟、饮酒不是心脏外科手术后脑梗死的影响因素(P>0.05),年龄、文化程度、高血压病史、糖尿病为心脏外科手术后脑梗死的影响因素(P<0.05),经多因素二元Logistic回归分析,年龄高、文化程度低、高血压病史≥10、有糖尿病,是心脏外科手术后脑梗死的独立影响因素(P<0.05)。结果显示,体外循环手术常为大面积梗死、双侧梗死,症状较重,而非体外循环手术常为皮层梗死,且两者分水岭梗死较多,均与栓塞和低灌注有关。心脏外科手术后脑梗死与年龄高、文化程度低、高血压病史≥10、有糖尿病密切相关,早期给予针对性预防干预可能降低脑梗死的发生。     

Measurements of RF heating during 3.0-T MRI of a pig implanted with deep brain stimulator

Purpose

To present preliminary, in vivo temperature measurements during MRI of a pig implanted with a deep brain stimulation (DBS) system.

Materials and Methods

DBS system (Medtronic Inc., Minneapolis, MN) was implanted in the brain of an anesthetized pig. 3.0-T MRI was performed with a T/R head coil using the low-SAR GRE EPI and IR-prepped GRE sequences (SAR: 0.42 and 0.39 W/kg, respectively), and the high-SAR 4-echo RF spin echo (SAR: 2.9 W/kg). Fluoroptic thermometry was used to directly measure RF-related heating at the DBS electrodes, and at the implantable pulse generator (IPG). For reference the measurements were repeated in the same pig at 1.5 T and, at both field strengths, in a phantom.

Results

At 3.0 T, the maximal temperature elevations at DBS electrodes were 0.46 °C and 2.3 °C, for the low- and high-SAR sequences, respectively. No heating was observed on the implanted IPG during any of the measurements. Measurements of in vivo heating differed from those obtained in the phantom.

Conclusion

The 3.0-T MRI using GRE EPI and IR-prepped GRE sequences resulted in local temperature elevations at DBS electrodes of no more than 0.46 °C. Although no extrapolation should be made to human exams and much further study will be needed, these preliminary data are encouraging for the future use 3.0-T MRI in patients with DBS.     

Calorimetric and computational study of 2H-1, 4-benzoxazin-3(4H)-one and of related species

The standard molar enthalpy of formation in the gas phase of 2H-1,4-benzoxazin-3(4H)-one was derived from the standard energy of combustion determined by static bomb combustion calorimetry in oxygen atmosphere and from the standard sublimation enthalpy determined by Calvet microcalorimetry. In addition, we report the results of a systematic theoretical study of the keto and enol tautomers in benzoxazinones and diones using density functional theory. The keto tautomers are computed to be more stable than the enols. Tautomerization energies are reported.     

功能磁共振成像的基本尺度熵分析

人体大脑活动的复杂度随年龄变化而变化, 并且和性别有一定的联系, 通过对功能磁共振成像复杂度的分析有助于发现人脑活动和性别年龄之间关系的规律. 本文提出需要根据年龄段的变化对基本尺度熵的参数做适当的调整, 以便获得良好的信号区分效果. 本文研究了人脑活动和性别年龄之间存在的关系. 结果证明, 同龄男女的基本尺度熵值存在一定的差异, 并且随年龄段的不同发生相应的变化, 另外基本尺度熵中的参数在数据分析中也随年龄变化存在一定规律的变化. 通过对fMRI数据的分析表明, 基本尺度熵能够有效地区分不同人群fMRI数据特征, 为进一步信号复杂度分析提供方便. 关键词： 功能磁共振成像 基本尺度熵 复杂度     

Plasma nanoscience: from nano-solids in plasmas to nano-plasmas in solids

The unique plasma-specific features and physical phenomena in the organization of nanoscale soild-state systems in a broad range of elemental composition, structure, and dimensionality are critically reviewed. These effects lead to the possibility to localize and control energy and matter at nanoscales and to produce self-organized nano-solids with highly unusual and superior properties. A unifying conceptual framework based on the control of production, transport, and self-organization of precursor species is introduced and a variety of plasma-specific non-equilibrium and kinetics-driven phenomena across the many temporal and spatial scales is explained. When the plasma is localized to micrometer and nanometer dimensions, new emergent phenomena arise. The examples range from semiconducting quantum dots and nanowires, chirality control of single-walled carbon nanotubes, ultra-fine manipulation of graphenes, nano-diamond, and organic matter to nano-plasma effects and nano-plasmas of different states of matter.     

The bilingual brain: Flexibility and control in the human cortex

The goal of the present review is to discuss recent cognitive neuroscientific findings concerning bilingualism. Three interrelated questions about the bilingual brain are addressed: How are multiple languages represented in the brain? how are languages controlled in the brain? and what are the real-world implications of experience with multiple languages? The review is based on neuroimaging research findings about the nature of bilingual processing, namely, how the brain adapts to accommodate multiple languages in the bilingual brain and to control which language should be used, and when. We also address how this adaptation results in differences observed in the general cognition of bilingual individuals. General implications for models of human learning, plasticity, and cognitive control are discussed.     

基于时间序列的飞机运动扰动建模

飞机的运动常常受到各种扰动因素的影响,这使得对其运动状态的刻画较为困难.由于确定飞机状态的三个量航速、航向、高度三者具有强相关性,采用了时间序列中的多维自回归方法对飞机扰动进行统计建模,以实例验证了所提方法是可行和有效的.     

磁共振成象新进展

磁共振成象(MRI)已经成为生命科学研究和医疗诊断的有力手段，因此荣获2003年诺贝尔生理学或医学奖．文章概述了磁共振成象的新近进展，包括医疗成象、脑功能成象、显微成象、活体磁共振波谱等方面．     

Single-walled carbon nanotube formation with double laser vaporization technique

Single-walled carbon nanotubes (SWNTs) were prepared with double laser vaporization of a graphite target and a metal/alloy target inside an electric furnace at 1200 ^°C ambient temperature with 500 torr Ar gas atmosphere. Each target was vaporized simultaneously with a different Nd:YAG laser. Several kinds of metal/alloy target (Ni, Co, Fe, and permalloy) were tested in order to see the difference in the resulting SWNT yield and the diameter distribution of them. The Raman spectra of SWNT-containing soot prepared by use of this technique with permalloy/carbon system indicated that permalloy gives almost the same yield as compared with Ni/Co carbon composite rod with single laser vaporization technique, though the diameter distribution of them is slightly different. Also, time-resolved images of the plume by carbon and permalloy nanoparticles after laser vaporization were collected using a high-speed video camera. These images suggest that the hot plumes due to carbon and permalloy nanoparticles do not mix together so extensively, at least in a few hundred microseconds after laser vaporization. The effect of time delay between two laser pulses on the yield and the diameter distribution of SWNTs was also presented and discussed.