Influence of different viscosity grade cellulose-based polymers on the development of valsartan controlled release tablets

This work is based on formulating and optimizing controlled release (CR) valsartan (160 mg) tablets using different viscosity grades of the cellulosic polymer. The objective was to develop an effective once-daily drug delivery system of this cardiovascular agent. Central composite design was used for designing the formulations. Polymers used were Methocel® K4M, K15M and K100M. Compatibility of excipients with active was studied through FT-IR. Micromeritic properties were determined and formulations exhibiting appropriate flow characteristics were compressed. Swelling behavior and in vitro buoyancy effect were studied and response surface curves were constructed to optimize the formulation. Multi-point dissolution profiles of valsartan CR tablets at pH 1.2, 4.5 and 6.8 were obtained. Model-dependent and model-independent methods were performed including f2, stability test as per ICH guidelines and ANOVA. FT-IR studies revealed the compatibility of valsartan with all excipients. Formulation K4T9 (containing 25% K4M polymer) was selected to be the best optimized trial, based on physical properties and controlled release profile (23% at 4 h, 82% at 16 h and 100% at 24 h). Results of buoyancy and swelling behavior indicated that HPMC-K4M polymer exhibited excellent floating lag time and swelling indexes. In vitro drug release kinetics showed that formulation K4T9 displayed Korsmeyer–Peppas drug release pattern with r value > 0.99. The manufacturing process of K4T9 was also found to be reproducible with a shelf life period of 41 and 36 months at room temperature and accelerated conditions, respectively. Valsartan CR matrix-based formulation was successfully prepared with Methocel K4M retardant.     

Attenuation of cocaine-induced locomotor activity by butyrylcholinesterase.

A primary enzyme for the metabolism of cocaine is butyrylcholinesterase (BChE). To determine whether the systemic administration of BChE can increase the metabolism of cocaine sufficiently to alter a behavioral effect, rats were tested in a locomotor activity chamber after receiving 17 mg of cocaine per kg intraperitoneally. In rats pretreated intravenously with 5,000 IU of horse serum-derived BChE, the locomotor activity effect was significantly attenuated. BChE pretreatment increased plasma BChE levels approximately 400-fold. When added to rat plasma, this amount of BChE reduced the cocaine half-life from over 5 hr to less than 5 min. BChE altered the cocaine metabolic pattern such that the relatively nontoxic metabolite ecgonine methyl ester was produced, rather than benzoylecgonine. These results suggest that systemic administration of BChE can increase the metabolism of cocaine sufficiently to alter a behavioral effect of cocaine and thus should be investigated as a potential treatment for cocaine abuse. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Rice β-Glucosidase 4 (Os1βGlu4) Regulates the Hull Pigmentation via Accumulation of Salicylic Acid

Salicylic acid (SA) is a stress hormone synthesized in phenylalanine ammonia-lyase (PAL) and the branching acid pathway. SA has two interconvertible forms in plants: SAG (SA O-β-glucoside) and SA (free form). The molecular mechanism of conversion of SA to SAG had been reported previously. However, which genes regulate SAG to SA remained unknown. Here, we report a cytoplasmic β-glucosidase (β-Glu) which participates in the SA pathway and is involved in the brown hull pigmentation in rice grain. In the current study, an EMS-generated mutant brown hull 1 (bh1) displayed decreased contents of SA in hulls, a lower photosynthesis rate, and high-temperature sensitivity compared to the wild type (WT). A plaque-like phenotype (brown pigmentation) was present on the hulls of bh1, which causes a significant decrease in the seed setting rate. Genetic analysis revealed a mutation in LOC_Os01g67220, which encodes a cytoplasmic Os1βGlu4. The knock-out lines displayed the phenotype of brown pigmentation on hulls and decreased seed setting rate comparable with bh1. Overexpression and complementation lines of Os1βGlu4 restored the phenotype of hulls and normal seed setting rate comparable with WT. Subcellular localization revealed that the protein of Os1βGlu4 was localized in the cytoplasm. In contrast to WT, bh1 could not hydrolyze SAG into SA in vivo. Together, our results revealed the novel role of Os1βGlu4 in the accumulation of flavonoids in hulls by regulating the level of free SA in the cellular pool.     

Synthesis and characterization of caprolactone based polyurethane with degradable and antifouling performance

In this work,a degradable polyurethane composed of caprolactone(CL)and L-Lactide(LLA)as soft seg-ments,and 4,4'-methylenebis(cyclohexyl isocyanate)(H12MDI)and polytetramethylene ether glycol(PTMEG)as hard segments,was prepared.Hydrolytic degradation experiment revealed that the degrad-able polyurethane(PU)could be degraded in artificial seawater.It also showed that caprolactone-co-polyurethane(CL-PU)copolymer with higher crystallinity degraded much slower in artificial seawater.However,the introduction of LLA resulted in an increase in the hydrophilicity and reduction in the crys-tallinity of degradable PU,as demonstrated by the contact angle analysis.The result of the scanning elec-tron microscope showed that the surface of degradable PU renewed under static condition.Moreover,degradable PU was able to be used as a carrier,and it controlled the release rate of 4,5-dichloro-2-octyl-isothiazolone(DCOIT).The anti-diatom(Navicula incerta)test demonstrated that the(caprolactone-co-L-lactide)-co-polyurethane 4(CL/LAx-PU4)with DCOIT contents prevented the adhe-sion of diatom Navicula incerta(88.37％reduction)due to their self-polishing and the release of antifou-lants.Therefore,the degradable PU consisted of CL,LLA,and DCOIT could be a durable resin with good antifouling activity for the application in the marine anti-biofouling field.     

VPR-Bench: An Open-Source Visual Place Recognition Evaluation Framework with Quantifiable Viewpoint and Appearance Change

International Journal of Computer Vision - Visual place recognition (VPR) is the process of recognising a previously visited place using visual information, often under varying appearance...     

A wireless Web for creating and sharing personal content through handsets

Mobile handsets have evolved from voice transmission devices to sophisticated digital assistants permanently connected to the Internet. These handsets now include hardware attachments that let users capture images and video and accurately track handsets' positions. These new features combined with the terminals' data transmission capabilities support a rich multimedia interaction model that enables users to share digital assets directly from their mobile devices. We call this model the Personalized Group Wide Web. PGWW aims to provide a flexible, simple, and efficient mechanism to enable next-generation cell phone users to share their digital assets. Increasingly sophisticated handheld devices provide an appropriate infrastructure to host a highly dynamic wireless WWW variant. This variant uses a flexible middleware infrastructure to overcome handset heterogeneity and resource limitations.     

Non‐Newtonian squashed flow simulation across Darcy‐Forchheimer sensor

The current mathematical formulation is dedicated to investigate the Darcy‐Forchheimer boundary layer–squeezed hydromagnetic flow of a Casson fluid passing through a sensor surface. The flow phenomenon is occurring in a locally free stream under the combined sway of heat generation and thermic radiation. The energy equation is deliberated with the assistance of Cattaneo‐Christov theory rather than using Fourier's law for conduction of heat. Here, the thermic conductivity is being presumed as a function of temperature. The governing mathematical structure consists of highly nonlinear terms, so a set of regulatory parameters is being accomplished to attain the unpretentious dimensionless equations. This nondimensional structure is then treated numerically to attain the nearly converging results. The significance of substantial parameters such as magnetic factor, radiation parameter, Casson fluid parameter, heat origination, and thermal relaxation time on the flow phenomenon is estimated and presented graphically. Besides this, the factors of engineering interest like the Prandtl number and squeezed flow index with vacillating thermic conductivity have strong effects on the flow behavior of the fluid. It is observed that the magnetic effect causes an expansion in the velocity curve while a reduction is found for squeezed flow index parameter.