888 resultados para Sustained release system


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The activation of pre-kininogenin to kininogenin (pre-kallikrein to kallikrein) is one of the steps in the series of reactions of a complex system, linked also to fibrinolysis and coagulation, that leads to kinin release in plasma (See Cochrane et al., 1976; Wuepper, 1976; Kaplan et al., 1976; Kaplan et al., 1976). For human plasma, a test using kaolin as activator and measuring kallikrein activity with the chromogenic substrate Chromozym PK (Nα-benzoyl-prolyl-phenylalanyl-arginyl-nitroanilide, Pentapharm, Basle) is routinely employed. The purpose of this paper is to further study the mechanism of this activation, by means of different activators and using as inhibitor hexadimethrine bromide (Polybrene). Besides kaolin, sulfated polysaccharides, such as heparin and cellulose sulfate are able to activate pre-kininogenin to kininogenin. Hexadimethrine as expected, inhibited the activation by heparin and also that by cellulose sulfate. The activation by kaolin however followed a different pattern suggesting, at least partially, a different mode of action of this activator. © 1979.

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Fibrinolysis is a basic defense mechanism of the organism designed to control the deposition of fibrin in the vascular system and elsewhere. Fibrinolytic activity was measured by the fibrin plate method for three groups of rats (N = 6) that were maintained at room temperature, 20-25 degrees C, 3 degrees C or 38 degrees C for 4 h before testing. Based on measurement of fibrinolytic activity, the level of plasminogen activator released from isolated aortic segments of rats maintained at room temperature (24-28 degrees C) differed significantly from that of the 38 degrees C group. The animals maintained at 3 degrees C did not release plasminogen activator, suggesting that the fibrinolytic response was impaired at low temperature.

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The effect of thiopentone/halothane anaesthesia on the release of endogenous opioid, adrenocorticotrophin, arginine vasopressin, cortisol and catecholamine was investigated in ponies. The contribution made by halothane itself was studied by maintaining six ponies with a constant 12 per cent end tidal halothane concentration and five with a concentration ranging between 0.8 and 12 per cent. Cardiorespiratory depression was more prolonged in the ponies receiving a constant 1-2 per cent end tidal halothane concentration than in those which received less halothane. Plasma lactate concentration increased and haematocrit decreased during halothane anaesthesia. The concentrations of met-enkephalin, dynorphin and catecholamines did not change and those of β-endorphin, adrenocorticotrophin, arginine vasopressin and cortisol increased during halothane anaesthesia. Halothane appeared to be a major stimulus to pituitary adrenocortical activation because the adrenocortical secretion was proportional to the amount of halothane inhaled. β-endorphin increased proportionally more than adrenocorticotrophin and their plasma concentrations were not correlated, suggesting that they have independent secretion mechanisms.

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Fencamfamine (FCF) is a central stimulant that facilitates central dopaminergic transmission through inhibition of dopamine uptake and enhanced release of the transmitter. We evaluated the changes in the inhibition of uptake and the release of striatal [ 3H]-dopamine at 9:00 and 21:00 h, times corresponding to maximal and minimal behavioral responses to FCF, respectively. Adult male Wistar rats (200-250 g) maintained on a 12-h light/12-h dark cycle (lights on at 7:00 h) were used. In the behavioral experiments the rats (N = 8 for each group) received FCF (3.5 mg/kg, ip) or saline at 9:00 or 21:00 h. Fifteen minutes after treatment the duration of activity (sniffing, rearing and locomotion) was recorded for 120 min. The basal motor activity was higher (28.6 ± 4.2 vs 8.4 ± 3.5 s) after saline administration at 21:00 h than at 9:00 h. FCF at a single dose significantly enhanced the basal motor activity (38.3 ± 4.5 vs 8.4 ± 3.5 s) and increased the duration of exploratory activity (38.3 ± 4.5 vs 32.1 ± 4.6 s) during the light, but not the dark phase. Two other groups of rats (N = 6 for each group) were decapitated at 9:00 and 21:00 h and striata were dissected for dopamine uptake and relase assays. The inhibition of uptake and release of [ 3H]-dopamine were higher at 9:00 than at 21:00 h, suggesting that uptake inhibition and the release properties of FCF undergo daily variation. These data suggest that the circadian time-dependent effects of FCF might be related to a higher susceptibility of dopamine presynaptic terminals to the action of FCF during the light phase which corresponds to the rats' resting period.

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The photo-Fenton process using potassium ferrioxalate as a mediator in the photodegradation reaction of organochloride compounds in an aqueous medium was investigated. The influence of parameters such as hydrogen peroxide and ferrioxalate concentrations and initial pH, was evaluated using dichloroacetic acid (DCA) as a model compound under black-light lamp irradiation. An upflow annular photoreactor, operating in a single pass or recirculating mode was used during photodegradation experiments with artificial light. The extent of the release of chloride ions was used to evaluate the photodegradation reaction. The optimum pH range observed was 2.5-2.8. The efficiency of DCA dechlorination increased with increasing concentrations of H2O2 and potassium ferrioxalate, reaching a plateau after the addition of 6 and 1.5 mmol/L of those reagents, respectively. The total organic carbon (TOC) content in DCA and 2,4-dichlorophenol (DCP) solutions was compared with the chloride released after photodegradation. The influence of natural solar light intensity, measured at 365 nm, was evaluated for the dechlorination of DCA on typical summer's days showing a linear dependency. The photodegradation of DCA using black-light lamp and solar irradiation was compared.

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The present study investigated the central role of angiotensin II and nitric oxide on arterial blood pressure (MAP) in rats. Losartan and PD123349 AT 1 and AT 2 (selective no peptides antagonists angiotensin receptors), as well as FK 409 (a nitric oxide donor), N W-nitro-L-arginine methyl ester (L-NAME) a constituve nitric oxide synthase inhibitor endothelial (eNOSI) and 7-nitroindazol (7NI) a specific neuronal nitric oxide synthase inhibitor (nNOSI) were used. Holtzman strain, (Rattus norvergicus) weighting 200-250 g were anesthetized with zoletil 50 mg kg -1 (tiletamine chloridrate 125 mg and zolazepan chloridrate 125 mg) into quadriceps muscle anda stainless steel cannula was stereotaxically implanted into their Lateral Ventricle (LV). Controls were injected with a 0.5 μl volume of 0.15 M NaCl. Angiotensin II injected into LV increased MAP (19±3 vs. control 3±1 mm Hg), which is potentiated by prior injection of L-NAME in the same site 26±2 mm Hg. 7NI injected prior to ANG II into LV also potentiated the pressor effect of ANG II but with a higher intensity than L-NAME 32±3 mm Hg. FK 409 inhibited the pressor effect of ANG II (6±1 mm Hg). Losartan injected into LV before ANG II influences the pressor effect of ANG II (8±1 mm Hg). The PD 123319 decreased the pressor effects of ANG II (16±1 mm Hg). Losartan injected simultaneously with FK 409 blocked the pressor effect of ANG II (3±1 mm Hg). L-NAME produced an increase in the pressor effect of ANG II, may be due to local vasoconstriction and all at once by neuronal NOS inhibition but the main effect is of the 7-NIT an specific nNOS inhibitor. The AT 1 antagonist receptors improve basal nitric oxide (NO) production and release. These data suggest the involvement of constitutive and neuronal NOS in the control of arterial blood pressure induced by ANG II centrally, evolving AT 1 receptor-mediated vasoconstriction and AT 2 receptor-mediated vasodilatation. These results were confirmed by the experiment using FK 409. © 2006 Asian Network for Scientific Information.

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Under biotic/abiotic stresses, the red alga Kappaphycus alvarezii reportedly releases massive amounts of H2O2 into the surrounding seawater. As an essential redox signal, the role of chloroplast-originated H2O2 in the orchestration of overall antioxidant responses in algal species has thus been questioned. This work purported to study the kinetic decay profiles of the redox-sensitive plastoquinone pool correlated to H2O2 release in seawater, parameters of oxidative lesions and antioxidant enzyme activities in the red alga Kappaphycus alvarezii under the single or combined effects of high light, low temperature, and sub-lethal doses of 3-(3,4-dichlorophenyl)-1,1-dimethylurea (DCMU) and 2,5-dibromo-3-methyl-6-isopropyl-p-benzoquinone (DBMIB), which are inhibitors of the thylakoid electron transport system. Within 24 h, high light and chilling stresses distinctly affected the availability of the PQ pool for photosynthesis, following Gaussian and exponential kinetic profiles, respectively, whereas combined stimuli were mostly reflected in exponential decays. No significant correlation was found in a comparison of the PQ pool levels after 24 h with either catalase (CAT) or ascorbate peroxidase (APX) activities, although the H2O2 concentration in seawater (R = 0.673), total superoxide dismutase activity (R = 0.689), and particularly indexes of protein (R = 0.869) and lipid oxidation (R = 0.864), were moderately correlated. These data suggest that the release of H2O2 from plastids into seawater possibly impaired efficient and immediate responses of pivotal H2O2-scavenging activities of CAT and APX in the red alga K. alvarezii, culminating in short-term exacerbated levels of protein and lipid oxidation. These facts provided a molecular basis for the recognized limited resistance of the red alga K. alvarezii under unfavorable conditions, especially under chilling stress. © 2006 Elsevier B.V. All rights reserved.

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Sustained attention and vigilance are processeses that characterize attention, and are essential for the development of certain abilities Aim: a prospective study to propose a simple, easy and quick behavioral tool to support the assessment of sustained auditory attention. Material and methods: volunteer children aged between 6 and 11 years (139 female and 141 male) were selected. The test was named Sustained Auditory Attention Ability Test, and is based on the Continuous Performance Test. It consist of a binaural and diotic presentation of a list of 100 monosyllabic words in which a target monosyllable is included 20 times. This list was presented six times with no breaks. The test was carried out in a soundproofed room, using a CD player attached to a two-channel audiometer at 50 dBSL during 9 minutes. The test resulted in a total score and a vigilance decrement. Results: There was no statistically significant difference between genders, but a significant difference was found between ages. Conclusion: The proposed test had no discomfort for the participants, and was shown to be extremely promising to assess the sustained auditory attention ability in children. © Revista Brasileira de Otorrinolaringologia. All Rights reserved.

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Upland rice (Oryza sativa L.) cultivation has been increasing in importance in Asia while water availability for irrigation has been decreasing because of rapid growth in industry and urban centers. Therefore, the development of technologies that increase upland rice yields under aerobic conditions, thereby saving water, would be an effective strategy to avoid a decrease in global rice grain production. The use of the no-tillage system (NTS) and cover crops that maintain soil moisture would prove advantageous in the move toward sustainable agriculture. However, upland rice develops better in plowed soil, and it has been reported that this crop does not perform well under the NTS. Therefore, the aim of this study was to investigate the effect of cover crops on upland rice grain yield and yield components sowed in a NTS. A field experiment was conducted during two growing seasons (2008-2009 and 2009-2010), and treatments consisted of growing rice under five cover crops in a NTS and two control treatments under the conventional tillage system (plowing once and disking twice). Treatments were carried out in a randomized block design with three replications. Our findings are as follows: On average, Brachiaria brizantha (12.32Mgha-1), Brachiaria ruziziensis (11.08Mgha-1) and Panicum maximum (11.62Mgha-1) had outstanding biomass production; however, these grasses provided the worst upland rice yields (2.30, 2.04, and 2.67Mgha-1, respectively) and are not recommended as cover crops before upland rice. Millet and fallow exhibited the fastest straw degradation (half-lives of 52 and 54 days, respectively), and millet exhibited the fastest nitrogen release (N half-life of 28 days). The use of a NTS was promising when millet was used as a cover crop; this allowed the highest upland rice yield (3.94Mgha-1) and did not statistically differ from plowed fallow (3.52Mgha-1). © 2012 Elsevier B.V.

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Dynamic exercise evokes sustained cardiovascular responses, which are characterized by arterial pressure and heart rate increases. Although it is well accepted that there is central nervous system mediation of cardiovascular adjustments during exercise, information on the role of neural pathways and signaling mechanisms is limited. It has been reported that glutamate, by acting on NMDA receptors, evokes the release of nitric oxide through activation of neuronal nitric oxide synthase (nNOS) in the brain. In the present study, we tested the hypothesis that NMDA receptors and nNOS are involved in cardiovascular responses evoked by an acute bout of exercise on a rodent treadmill. Moreover, we investigated possible central sites mediating control of responses to exercise through the NMDA receptor-nitric oxide pathway. Intraperitoneal administration of the selective NMDA glutamate receptor antagonist dizocilpine maleate (MK-801) reduced both the arterial pressure and heart rate increase evoked by dynamic exercise. Intraperitoneal treatment with the preferential nNOS inhibitor 7-nitroindazole reduced exercise-evoked tachycardiac response without affecting the pressor response. Moreover, treadmill running increased NO formation in the medial prefrontal cortex (MPFC), bed nucleus of the stria teminalis (BNST) and periaqueductal gray (PAG), and this effect was inhibited by systemic pretreatment with MK-801. Our findings demonstrate that NMDA receptors and nNOS mediate the tachycardiac response to dynamic exercise, possibly through an NMDA receptor-NO signaling mechanism. However, NMDA receptors, but not nNOS, mediate the exercise-evoked pressor response. The present results also provide evidence that MPFC, BNST and PAG may modulate physiological adjustments during dynamic exercise through NMDA receptor-NO signaling. © 2013 Elsevier B.V.

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In this work, we synthesized a novel series of hydrogels composed of polyacrylamide (PAAm), methylcellulose (MC), and calcic montmorillonite (MMt) appropriate for the controlled release of fertilizers, where the components presented a synergistic effect, giving very high fertilizer loading in their structure. The synthesized hydrogel was characterized in relation to morphological, hydrophilic, spectroscopic, structural, thermal, and kinetic properties. After those characterizations, the application potential was verified through sorption and desorption studies of a nitrogenated fertilizer, urea (CO(NH2)2). The swelling degree results showed that the clay loading considerably reduces the water absorption capability; however, the hydrolysis process favored the urea adsorption in the hydrogel nanocomposites, increasing the load content according to the increase of the clay mass. The FTIR spectra indicated that there was incorporation of the clay with the polymeric matrix of the hydrogel and that incorporation increased the water absorption speed (indicated by the kinetic constant k). By an X-ray diffraction technique, good nanodispersion (intercalation) and exfoliation of the clay platelets in the hydrogel matrix were observed. Furthermore, the presence of the montmorillonite in the hydrogel caused the system to liberate the nutrient in a more controlled manner than that with the neat hydrogel in different pH ranges. In conclusion, excellent results were obtained for the controlled desorption of urea, highlighting the hydrolyzed hydrogels containing 50% calcic montmorillonite. This system presented the best desorption results, releasing larger amounts of nutrient and almost 200 times slower than pure urea, i.e., without hydrogel. The total values of nutrients present in the system show that this material is potentially viable for application in agriculture as a nutrient carrier vehicle. © 2013 American Chemical Society.

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This study describes the histology and histochemistry of the male reproductive system in Callinectes ornatus, comparing juvenile and adult developmental stages. We also analyzed changes in the gonadosomatic (GSI) and hepatosomatic (HSI) indices, and the weights of the testis and vas deferens during the development. The results showed that all stages, beginning with the juvenile (JUV), through developing (DEV) and mature (MAT) adult males of C. ornatus produce sperm and spermatophores. During development, testicular lobes showed the same characteristics of production and release of sperm into the seminiferous duct. The vas deferens showed little histological and histochemical change in the epithelium in juvenile and adult males. The differences consisted of the larger amount of secretion in MAT males compared to JUV and DEV ones. The chemical composition of the seminal fluid was similar, but MAT males produced a more homogeneous secretion. Morphological and physiological maturation are not synchronized in C. ornatus, since JUV males produced spermatophores similar to those in DEV and MAT males. However, these JUV are not yet able to reproduce, since they still have the abdomen attached to the cephalothoracic sternum. The increase of the GSI during development was significant for MAT males, and is related to the production of sufficient volume of seminal fluid to form the sperm plug in the female seminal receptacle. The HSI decreased from DEV to MAT adult stages, indicating that reserves from the hepatopancreas are used to develop the reproductive system after the pubertal molt.

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In order to investigate the effect on the aqueous solubility and release rate of sulfamerazine (SMR) as model drug, inclusion complexes with beta-cyclodextrin (beta CD), methyl-beta-cyclodextrin (M beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD) and a binary system with meglumine (MEG) were developed. The formation of 1: 1 inclusion complexes of SMR with the CDs and a SMR: MEG binary system in solution and in solid state was revealed by phase solubility studies (PSS), nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), thermal analysis and X-Ray diffractometry (XRD) studies. The CDs solubilization of SMR could be improved by ionization of the drug molecule through pH adjustments. The higher apparent stability constants of SMR:CDs complexes were obtained in pH 2.00, demonstrating that CDs present more affinity for the unionized drug. The best approach for SMR solubility enhancement results from the combination of MEG and pH adjustment, with a 34-fold increment and a S-max of 54.8 mg/ml. The permeability of the drug was reduced due to the presence of beta CD, M beta CD, HP beta CD and MEG when used as solubilizers. The study then suggests interesting applications of CD or MEG complexes for modulating the release rate of SMR through semipermeable membranes.