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31.
Characterization of the Solubility and Dissolution Properties of Several New Rifampicin Polymorphs, Solvates, and Hydrates 总被引:2,自引:0,他引:2
Stanley Q. Henwood Wilna Liebenberg Lourens R. Tiedt Antonie P. L tter Melgardt M. de Villiers 《Drug development and industrial pharmacy》2001,27(10):1017-1030
Based on reports that tuberculosis is on the increase, this investigation into the physicochemical properties of rifampicin when recrystallized from various solvent systems was undertaken. Rifampicin is an essential component of the currently recommended regimen for treating tuberculosis, although relatively little is known about its solubility and dissolution behavior in relation to its solid-state properties. A rifampicin monohydrate, a rifampicin dihydrate, two amorphous forms, a 1:1 rifampicin:acetone solvate, and a 1:2 rifampicin:2-pyrrolidone solvate were isolated and characterized using spectral, thermal, and solubility measurements. The crystal forms were relatively unstable because except for the 2-pyrrolidone solvate, all the hydrated or solvated materials changed to amorphous forms after desolvation. Fourier transform infrared (FTIR) analysis confirmed the favorable three-dimensional organization of the pharmacophore to ensure antibacterial activity in all the crystal forms except the 2-pyrrolidone solvate. In the 2-pyrrolidone solvate, the strong IR signals of 2-pyrrolidone interfered with the vibrations of the ansa group. The 2-pyrrolidone solvate was the most soluble in phosphate buffer at pH 7.4. This solvate also had the highest solubility (1.58 mg/ml) and the fastest dissolution in water. In 0.1 M HCl, the dihydrate dissolved the quickest. A X-ray amorphous form (amorph II) was the least soluble and had the slowest dissolution rate because the powder was poorly wettable and very electrostatic. 相似文献
32.
van Hoek AH de Jonge R van Overbeek WM Bouw E Pielaat A Smid JH Malorny B Junker E Löfström C Pedersen K Aarts HJ Heres L 《International journal of food microbiology》2012,153(1-2):45-52
Pork contributes significantly to the public health disease burden caused by Salmonella infections. During the slaughter process pig carcasses can become contaminated with Salmonella. Contamination at the slaughter-line is initiated by pigs carrying Salmonella on their skin or in their faeces. Another contamination route could be resident flora present on the slaughter equipment. To unravel the contribution of these two potential sources of Salmonella a quantitative study was conducted. Process equipment (belly openers and carcass splitters), faeces and carcasses (skin and cutting surfaces) along the slaughter-line were sampled at 11 sampling days spanning a period of 4 months. Most samples taken directly after killing were positive for Salmonella. On 96.6% of the skin samples Salmonella was identified, whereas a lower number of animals tested positive in their rectum (62.5%). The prevalence of Salmonella clearly declined on the carcasses at the re-work station, either on the cut section or on the skin of the carcass or both (35.9%). Throughout the sampling period of the slaughter-line the total number of Salmonella per animal was almost 2 log lower at the re-work station in comparison to directly after slaughter. Seven different serovars were identified during the study with S. Derby (41%) and S. Typhimurium (29%) as the most prominent types. A recurring S. Rissen contamination of one of the carcass splitters indicated the presence of an endemic 'house flora' in the slaughterhouse studied. On many instances several serotypes per individual sample were found. The enumeration of Salmonella and the genotyping data gave unique insight in the dynamics of transmission of this pathogen in a slaughter-line. The data of the presented study support the hypothesis that resident flora on slaughter equipment was a relevant source for contamination of pork. 相似文献
33.
J Schuurman GJ Perdok TE Lourens PW Parren MD Chapman RC Aalberse 《Canadian Metallurgical Quarterly》1997,99(4):545-550
1. We evaluated the antianginal effects of YM430 in several experimental models in vitro and in vivo. 2. In isolated dog coronary artery, YM430 (10(-8)-10(-6) M) inhibited 3,4-diaminopyridine-induced rhythmic contractions with an IC50 value of 59.2 nM. 3. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg PO. 4. In anesthetized dogs, YM430 (0.3 mg/kg IV) significantly inhibited ST-segment elevation induced by coronary artery occlusion. 5. These findings suggest that YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina. 相似文献
34.
We consider the problem of coloring a planar graph with the
minimum number of colors so that each color class avoids one or
more forbidden graphs as subgraphs. We perform a detailed study of
the computational complexity of this problem. We present a complete picture for the case with a single forbidden
connected (induced or noninduced) subgraph. The 2-coloring
problem is NP-hard if the forbidden subgraph is a tree with at
least two edges, and it is polynomially solvable in all other
cases. The 3-coloring problem is NP-hard if the forbidden
subgraph is a path with at least one edge, and it is polynomially solvable in all other
cases. We also derive results for several forbidden sets of
cycles. In particular, we prove that it is NP-complete to decide if a planar
graph can be 2-colored so that no cycle of length at most 5 is
monochromatic. 相似文献
35.
Grasman RP Huizenga HM Waldorp LJ Böcker KB Molenaar PC 《IEEE transactions on bio-medical engineering》2004,51(1):45-55
Interactions between cortical areas are crucial for cognitive functioning. Methods currently in use to assess such interactions are not well suited for this task because they lack timing precision, localization precision, or both. We present a method for simultaneous estimation of source location and orientation parameters and cross-spectral parameters to overcome these problems. Different estimators are evaluated for their performance. From a simulation study, we conclude that the estimators derived from the maximum-likelihood procedure have good statistical properties with moderate sample sizes, whereas those obtained from the generalized least squares procedure are biased and give poor-quality standard errors. The method is illustrated with visually evoked field data, with inconclusive results. 相似文献
36.
A simple algorithm is described that determines the focus quality of an image by measuring the maximum brightness gradient present in it. Measurements on actual television pictures are correlated with subjective focus evaluations on the CCIR five-point scale. The excellent correlation between measurement and subjective evaluation indicates the usefulness of the algorithm 相似文献
37.
This paper presents a parallel real time framework for emotions and mental states extraction and recognition from video fragments of human movements. In the experimental setup human hands are tracked by evaluation of moving skin-colored objects. The tracking analysis demonstrates that acceleration and frequency characteristics of the traced objects are relevant for classification of the emotional expressiveness of human movements. The outcomes of the emotional and mental states recognition are cross-validated with the analysis of two independent certified movement analysts (CMA’s) who use the Laban movement analysis (LMA) method. We argue that LMA based computer analysis can serve as a common language for expressing and interpreting emotional movements between robots and humans, and in that way it resembles the common coding principle between action and perception by humans and primates that is embodied by the mirror neuron system. The solution is part of a larger project on interaction between a human and a humanoid robot with the aim of training social behavioral skills to autistic children with robots acting in a natural environment. 相似文献
38.
The use of direct digital synthesis (DDS) to synthesize high-frequency analog signals has received much attention over the past decade. This technique allows modulation schemes such as FM and PM to be implemented with high fidelity using digital components. This paper investigates an improvement on the typical DDS approach of synthesizing the desired signal at an intermediate frequency. Instead, two quadrature baseband signals are generated, which are then mixed directly to the output center frequency. This method can be used to synthesize FM signals of arbitrarily high output frequency, using digital circuitry with considerably lower clock speeds 相似文献
39.
Results are presented of a study into how drivers say they behave and how they actually behave in traffic situations in which children are involved. An analysis was made of the most important types of encounters in which drivers become involved in accidents with children. On the basis of accident surveys and psychological theories on information processing, it was assessed by means of a questionnaire what knowledge drivers have concerning their own behavior in these situations, as well as their expectations about typical child behavior. Actual behavior of drivers in these situations was investigated by assessing video recordings of their behavior in driving a one hour standard track through residential areas. From the questionnaire it appeared that younger drivers reported more frequently dangerous behavior than older drivers. The recordings showed that younger drivers also behaved more dangerously during child encounters. This result could not be explained by differences in speed, but could by the fact that younger drivers detected the children less frequently than older drivers. Implications for the contents of mass media campaigns and their evaluation are discussed. 相似文献
40.
Josef D.V. van Wyngaard Robin Meeske Lourens J. Erasmus 《Journal of dairy science》2018,101(11):9954-9966
The effect of concentrate feeding level on enteric CH4 emissions from cows grazing medium quality summer pasture is yet to be investigated. Sixty multiparous Jersey cows (9 rumen-cannulated) were used in a randomized complete block design study (with the cannulated cows in a 3 × 3 Latin square design) to investigate the effect of concentrate feeding level (0, 4, and 8 kg/cow per day; as-fed basis) on enteric CH4 emissions, production performance, and rumen fermentation of dairy cows grazing summer pasture (17 cows plus 3 cannulated cows per treatment). Enteric CH4 emissions were measured from 11 cows per treatment group during one 7-d measurement period using the sulfur hexafluoride tracer gas technique. Pasture dry matter intake (DMI) was determined parallel with the CH4 measurement period using TiO2 as an external marker, and milk yield, milk composition, cow condition, and pasture pre- and postgrazing measurements were also recorded. Daily total DMI (11.2 to 15.6 kg/cow), milk yield (9.1 to 18.2 kg/cow), energy-corrected milk (ECM; 11.2 to 21.6 kg/cow), and milk lactose content (44.1 to 46.7 g/kg) increased linearly, whereas pasture DMI (11.2 to 8.4 kg/cow) decreased linearly with increasing concentrate feeding level. Daily CH4 production (323 to 378 g/d) increased linearly due to the increase in total DMI, whereas CH4 yield (29.1 to 25.1 g/kg of DMI) and CH4 intensity (35.5 to 21.1 g/kg of milk yield; and 28.8 to 17.6 g/kg of ECM) decreased linearly with increasing concentrate feeding level. Diurnal ruminal pH (6.45 to 6.32) and in sacco DM and neutral detergent fiber disappearance decreased linearly. Acetic and propionic acid were unaffected by treatment, whereas butyric acid (5.21 to 6.14 mM) increased linearly and quadratically with increasing concentrate feeding level. It was concluded that a high concentrate feeding level not only increases animal efficiency but is moreover a viable CH4 mitigation option for dairy cows grazing kikuyu-dominant pasture in late summer when pasture is inherently fibrous. 相似文献