Liquid chromatography–tandem mass spectrometry method for simultaneous quantification of urapidil and aripiprazole in human plasma and its application to human pharmacokinetic study

A sensitive and selective liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed and validated for simultaneous determination of urapidil and aripiprazole in human plasma. A simple liquid–liquid extraction with ethyl acetate was used for the sample preparation. Chromatographic separation was achieved on a Phenomenex C₁₈ (4.6 × 50 mm, 5 µm) column with 0.1% formic acid–acetonitrile (10:90, v/v) as the mobile phase with flow rate of 0.6 mL/min. The quantitation of the target compounds was determined in a positive ion multiple reaction monitoring mode. Calibration plots were linear over the range of 2.0–2503.95 ng/mL for urapidil and 1.0–500.19 ng/mL for aripiprazole. The lower limit of quantitation for urapidil and aripiprazole was 2.0 and 1.0 ng/mL, respectively. Mean recovery was in the range of 69.94–75.62% for both analytes and internal standards. Intra‐day and inter‐day precisions of the assay at three concentrations were 2.56–5.89% with accuracy of 92.31–97.83% for urapidil, and 3.14–6.84% with accuracy of 91.38–94.42% for aripiprazole. The method was successfully applied to human pharmacokinetic study of urapidil and aripiprazole in healthy human male volunteers. Copyright © 2013 John Wiley & Sons, Ltd.     

Studies on defect formation in femtosecond laser-irradiated PMMA and PDMS

We report here our results on the spectroscopic and elemental analysis of femtosecond (fs) laser-modified regions in polymers of polymethylmethacrylate (PMMA) and polydimethylsiloxane (PDMS) in the context of defect formation and emission in the visible region. Different physical and chemical models are used to explain the changes in modified regions. We found that the emission intensity, recorded from the fs-modified regions of polymers, decreased over time to a constant value. We also demonstrate that these materials are suitable for the preparation of the microstructures en route for light guiding applications. The fs laser-irradiated regions exhibited paramagnetic behavior as was confirmed from electron spin resonance studies through the formation of peroxide-type free radicals. Raman mapping was performed in the modified regions which consisted of defects and found that the modulations in intensity are predominant in the central portion of the structure compared to edges. Elemental analysis has been performed in the modified regions using field emission scanning electron microscope instrument and energy-dispersive X-ray absorption spectroscopy to estimate the percentage contents of individual elements which resulted in defect formation such as paramagnetic and optical centers.     

A New Route to the Synthesis of N-Formyl Lactams Using Vilsmeier Reagent

A convenient synthesis of N-formyl lactams from the corresponding tetralone and flavanone oximes using Vilsmeier reagent is described.     

STUDY OF SH-WAVE PROPAGATION IN AN INITIALLY STRESSED TRICLINIC LAYER SANDWICHED BETWEEN TRANSVERSELY ISOTROPIC ELASTIC AND HETEROGENEOUS POROELASTIC HALF-SPACES

Journal of Applied Mechanics and Technical Physics - In this paper, SH-wave propagation in an initially stressed triclinic layer welded between two half-spaces is investigated. The upper half-space...     

Ultrafast Excited State Relaxation Dynamics of New Fuchsine- a Triphenylmethane Derivative Dye

An all-inclusive investigation of the ultrafast excited state relaxation dynamics of a triphenylmethane derivative molecule, New Fuchsine (NF), using a combined approach of density functional theory (DFT), femtosecond transient absorption spectroscopy (fs-TAS), and photoluminescence spectroscopy is presented in this work. The DFT calculations confirmed the formation of twisted molecular structure in the excited state of NF in ethanol solution with bond rotation of ≈86°. TAS measurements of NF solution exhibited ultrafast ground state-recovery pathway via a conical intersection confirming an ultrafast structural reorientation. On the contrary, TAS measurements of NF thin-film exhibited a longer excited-state lifetime suggesting a hindered molecular twisted state formed as an intermediate step. Photophysical kinetic models are proposed to globally fit the fs-TAS data establishing the twisted intramolecular charge transfer (TICT) state mediated ground state recovery for NF in solution and thin film, respectively. Temperature-dependent photoluminescence study of NF film provided a clear insight into the effect of rotational motion of phenyl rings in NF molecules over the TICT mediated emission.     

Design,synthesis and characterization of peptidyl boronate analogues as effective antimicrobial agents

Research on Chemical Intermediates - Antibiotic-resistant penicillin binding protein (PBPs) production is one of the reasons why bacteria develop resistance to β-lactam antibiotics, and this...     

Synthesis,antioxidant, and antimicrobial activity of 3-(1H-indole-3-carbonyl)-2H-chromen-2-ones

A simple and convenient method for the one-pot synthesis of 3-(1H-indole-3-carbonyl)-2H-chromen-2-one derivatives from the reaction of 3-cyanoacetyl indole and salicylaldehyde in the presence of Na₂CO₃ in water: methanol (1:1) is described. Wider substrate scope, high yields, operational simplicity, and simple purification process make the protocol highly applicable in the synthesis of 3-(1H-indole-3-carbonyl)-2H-chromen-2-ones. For the first time, in vitro antioxidant and antimicrobial activity was studied. Compounds 5e , 7a , and 7b exhibits good radical scavenging ability against DPPH free radical. Compounds 7b , 5f , and 5g possess lower EC₅₀ values than the Standards AA and BHA and thus proving their high reducing power. Compounds 5d and 5f show good antibacterial activity against gram-positive bacteria (MRSA) while compounds 5c , 7a , and 7b exhibits good antibacterial activity against Bacillus sp. Compounds 5b and 5e show good antibacterial activity against gram negative bacterial strains (Escherichia coli, Klebsiella pneumoniae) and compounds 5g and 5h exhibits good antifungal activity against Candida albicans.     

Instantaneous work hardening behaviour of two-phase tungsten heavy alloys: a phenomenological approach

ABSTRACT

The present work describes a phenomenological approach to explain the instantaneous behaviour of tungsten heavy alloys (WHAs) in heat-treated and swaged conditions. The strengths and elongation values of heat-treated materials are lower and higher than those of the swaged samples respectively. The heat-treated materials exhibit two slopes in true stress–true plastic strain curves and follow the Ludwigson constitutive equation. On the other hand, swaged materials display a single slope and adhere to typical Swift constitutive equation. The latter reflect the presence of pre-strain in the materials due to swaging deformation. The fracture surfaces in heat-treated materials consist of W-W decohesion along with matrix rupture and W-cleavage, while swaged samples consist of mainly W-cleavage. Both the materials display three typical stages (I, II and III) of work hardening. The second derivatives of true stress–true plastic strain curves of these alloys exhibit a perfect parabola although the nature of true stress–true strain as well as true stress–true plastic strain curves is quite different in heat-treated and swaged materials. This has been observed for the first time in WHAs consisting of matrix and W-grains. The shape of the parabola is simple and easy to fit. The fitting parameters of parabolas have been successfully employed to explain the flow behaviour of a large number of tungsten heavy alloys having two-phase microstructure in different processing conditions.