Bio-Dis and the Paddle Dissolution Apparatuses Applied to the Release Characterization of Ketoprofen from Hypromellose Matrices

The purposes of this work were: (1) to comparatively evaluate the effects of hypromellose viscosity grade and content on ketoprofen release from matrix tablets, using Bio-Dis and the paddle apparatuses, (2) to investigate the influence of the pH of the dissolution medium on drug release. Furthermore, since direct compression had not shown to be appropriate to obtain the matrices under study, it was also an objective (3) to evaluate the impact of granulation on drug release process. Six formulations of ketoprofen matrix tablets were obtained by compression, with or without previous granulation, varying the content and viscosity grade of hypromellose. Dissolution tests were carried out at a fixed pH, in each experiment, with the paddle method (pH 4.5, 6.0, 6.8, or 7.2), while a pH gradient was used in Bio-Dis (pH 1.2 to 7.2). The higher the hypromellose viscosity grade and content were, the lower the amount of ketoprofen released was in both apparatuses, the content effect being more expressive. Drug dissolution enhanced with the increase of the pH of the medium due to its pH-dependent solubility. Granulation caused an increase in drug dissolution and modified the mechanism of the release process.

Gastro-resistant Pellets of Didanosine obtained by Extrusion and Spheronization: Assessing the Production Process

The aim this work was develop gastro-resistant pellets of didanosine as well as study the impact on the pellets properties, regarding the way as the binder was added and drying process used. The pellets formation was accompanied by analysis of morphological parameters and didanosine dissolution. In the most cases, pellets showed diameter around 1.0 mm and shape parameters acceptable. The variations of the process did not interfere significantly in pellets size. In turn, drying in fluid bed favored the dissolution of didanosine, in contrast to binder addition on powder form that impaired. In another hand, this last resulted in the best aspect factor (about 1.1). Gastro-resistant pellets showed adequate dissolution, compatible with this type of dosage form. The variables of process studied enabled obtain pellets with characteristics of shape and dissolution just slightly different, indicating flexibility of the formulation for production of gastro-resistant pellets of didanosine.

Development and In Vitro Evaluation of Propranolol Hydrochloride Controlled Release Tablets Using HPMC as Matrix Former

The purpose of this paper was to produce controlled-release matrices with 120 mg of propranolol hydrochloride (PHCl) employing hydroxypropyl methylcellulose (HPMC, Methocel (R) K100) as the gel forming barrier. Although this class of polymers has been commonly used for direct compression, with the intent of use reduced polymer concentrations to achieve controlled drug release, in this study tablets were produced by the wet granulation process. HPMC percentages ranged from 15-34 % and both soluble and non soluble diluents were tested in the 10 proposed tablet compositions. Dissolution testing of matrices was performed over a 12 h period in 1.2 pH medium (the first 2 h) and in pH 6.8 (10 h). Dissolution kinetic analysis was performed by applying Zero-order, First-order and Higuchi models with the aim of elucidating the drug release mechanism. All physical-chemical characteristics such as average weight, friability, hardness, diameter, height, and drug content were in accordance to the pharmacopeial specifications. Taking into account that PHCl is a very soluble drug, low concentrations (15 %) of HPMC were sufficient to reduce the drug release and to promote controlled release of PHCl, presenting good dissolution efficiencies, between 50 % and 63 %. The Higuchi model has presented the best fit to the 15 % HPMC formulations, indicating that the main release mechanism was diffusion. It could be concluded that the application of the wet granulation method reduced matrices erosion and promoted controlled release of the drug at low HPMC percentages.

Obtention and Evaluation of Inclusion Complexes of Furosemide with beta-ciclodextrin and hidroxipropil-beta-ciclodextrin: Effects on Drug`s Dissolution Properties

Obtention and Evaluation of Inclusion Complexes of Furosemide with beta-ciclodextrin and hidroxipropil-beta-ciclodextrin: Effects on Drug`s Dissolution Properties. The purpose of this study was to prepare, characterize and evaluate the dissolution behavior of inclusion complexes of furosemide with beta-cyclodextrin (beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD). Solid complexes of furosemide with P-CD and-HP-beta-CD were prepared by using a freeze-drying method. Physical mixtures were prepared for comparison. The inclusion complexes were characterized by differential scanning calorimetry (DSC), Infrared (IR) and dissolution test. ""In vitro"" dissolutions assays were performed at pH 1,2; pH 4,5 and pH 6,8 media for a 60 min period. Statistical analysis employing ANOVA and Tukey`s Test, for the dissolution efficiency values (ED%), showed that complexation of furosemide with both cyclodextrins improved significantly ED% of the drug in all tested media, suggesting a minor pH influence on dissolution properties of the drug.

Dissolution of a solid sphere in an unbounded, stagnant liquid

An exact analytical solution is obtained for the transient dissolution of solid spheres in a diffusion-controlled environment. This result provides a useful reference point for drug testing in humans. The dimensionless solution is expressed in terms of a single parameter, which accounts for solubility, bulk flow, and stagnant fluid composition. A simple, explicit and exact expression was found to predict time-to-complete dissolution (TCD). An approximate solution was also found which tracks the exact case for low solubility conditions.

The anodic dissolution of magnesium in chloride and sulphate solutions

The electrochemical behaviour of magnesium was studied in representative chloride and sulphate solutions including NaCl, Na2SO4, NaOH and their mixed solutions, HCl, and H2SO4: (1) by measuring electrochemical polarisation curves, (2) by using electrochemical impedance spectroscopy (EIS), and (3) by simultaneous measurement of hydrogen gas evolution and measurement of magnesium dissolution rates using inductively coupled plasma atomic emission spectrophotometry (ICPEAS). These experiments showed that a partially protective surface film played an important role in the dissolution of magnesium in chloride and sulphate solutions. Furthermore, the experimental data were consistent with the involvement of the intermediate species Mg+ in magnesium dissolution at film imperfections or on a film-free surface. At such sites, magnesium first oxidised electrochemically to the intermediate species Mg+, and then the intermediate species chemically reacted with water to produce hydrogen and Mg2+. The presence of Cl- ions increased the film free area, and accelerated the electrochemical reaction rate from magnesium metal to Mg+. (C) 1997 Elsevier Science Ltd.

Production and properties of xylanases from Aspergillus terricola Marchal and Aspergillus ochraceus and their use in cellulose pulp bleaching

Aspergillus terricola and Aspergillus ochraceus, isolated from Brazilian soil, were cultivated in Vogel and Adams media supplemented with 20 different carbon sources, at 30 A degrees C, under static conditions, for 120 and 144 h, respectively. High levels of cellulase-free xylanase were produced in birchwood or oat spelt xylan-media. Wheat bran was the most favorable agricultural residue for xylanase production. Maximum activity was obtained at 60 A degrees C and pH 6.5 for A. terricola, and 65 A degrees C and pH 5.0 for A. ochraceus. A. terricola xylanase was stable for 1 h at 60 A degrees C and retained 50% activity after 80 min, while A. ochraceus xylanase presented a t (50) of 10 min. The xylanases were stable in an alkali pH range. Biobleaching of 10 U/g dry cellulose pulp resulted in 14.3% delignification (A. terricola) and 36.4% (A. ochraceus). The brightness was 2.4-3.4% ISO higher than the control. Analysis in SEM showed defibrillation of the microfibrils. Arabinase traces and beta-xylosidase were detected which might act synergistically with xylanase.

Xylanases from Aspergillus niger, Aspergillus niveus and Aspergillus ochraceus produced under solid-state fermentation and their application in cellulose pulp bleaching

This study describes the production of xylanases from Aspergillus niveus, A. niger, and A. ochraceus under solid-state fermentation using agro-industrial residues as substrates. Enzyme production was improved using a mixture of wheat bran and yeast extract or peptone. When a mixture of corncob and wheat bran was used, xylanase production from A. niger and A. ochraceus increased by 18%. All cultures were incubated at 30 A degrees C at 70-80% relative humidity for 96 h. For biobleaching assays, 10 or 35 U of xylanase/g dry cellulose pulp were incubated at pH 5.5 for 1 or 2 h, at 55 A degrees C. The delignification efficiency was 20%, the brightness (percentage of ISO) increased two to three points and the viscosity was maintained confirming the absence of cellulolytic activity. These results indicated that the use of xylanases could help to reduce the amount of chlorine compounds used in cellulose pulp treatment.

Production of xylanase by Aspergilli using alternative carbon sources: application of the crude extract on cellulose pulp biobleaching

The ability of xylanolytic enzymes produced by Aspergillus fumigatus RP04 and Aspergillus niveus RP05 to promote the biobleaching of cellulose pulp was investigated. Both fungi grew for 4-5 days in liquid medium at 40A degrees C, under static conditions. Xylanase production was tested using different carbon sources, including some types of xylans. A. fumigatus produced high levels of xylanase on agricultural residues (corncob or wheat bran), whereas A. niveus produced more xylanase on birchwood xylan. The optimum temperature of the xylanases from A. fumigatus and A. niveus was around 60-70A degrees C. The enzymes were stable for 30 min at 60A degrees C, maintaining 95-98% of the initial activity. After 1 h at this temperature, the xylanase from A. niveus still retained 85% of initial activity, while the xylanase from A. fumigatus was only 40% active. The pH optimum of the xylanases was acidic (4.5-5.5). The pH stability for the xylanase from A. fumigatus was higher at pH 6.0-8.0, while the enzyme from A. niveus was more stable at pH 4.5-6.5. Crude enzymatic extracts were used to clarify cellulose pulp and the best result was obtained with the A. niveus preparation, showing kappa efficiency around 39.6% as compared to only 11.7% for that of A. fumigatus.

Biofilm Dissolution and Cleaning Ability of Different Irrigant Solutions on Intraorally Infected Dentin

Introduction: The aim of this study was to evaluate the biofilm dissolution and cleaning ability of different irrigant solutions on intraorally infected dentin. Methods: One hundred twenty bovine dentin specimens were infected intraorally by using a removable orthodontic device. Thirty samples were used for each irrigant solution: 2% chlorhexidine and 1%, 2.5%, and 5.25% sodium hypochlorite (NaOCl). The solutions were used for 5, 15, and 30 minutes and at 2 experimental volumes, 500 mu L and 1 mL. The samples were stained by using acridine orange dye before and after the experiments and evaluated by using a confocal microscope. The percentage of biofilm, isolated cells, and noncolonized dentin was measured by using a grid system. Differences in the reduction or increase of the studied parameters were assessed by using nonparametric methods (P < .05). Results: The higher values of biofilm dissolution and noncolonized dentin were found in the 30-minute NaOCl group and in the 5-minute and 15-minute groups of 5.25% NaOCL. The use of 2% chlorhexidine solution did not improve the biofilm dissolution or increase the cleaning of the dentin in comparison with the NaOCl solutions (P < .05). Conclusions: Two percent chlorhexidine does not dissolve the biofilms. Thirty minutes of NaOCl are necessary to have higher values of biofilm dissolution and to increase the cleaning of the dentin independently of the concentration in comparison with the 5-minute and 15-minute contact times. (J Endod 2011;37:1134-1138)

Dissolution of sucrose crystals in the anhydrous sorbitol melt

The dissolution of a sugar (sucrose as a model) with higher melting point was studied in a molten food polyol (sorbitol as a model) with lower melting point, both in anhydrous state. A DSC and optical examination revealed the dissolution of anhydrous sucrose crystals (mp 192 degreesC) in anhydrous sorbitol (mp 99 degreesC) liquid melt. The sucrose-sorbitol crystal mixtures at the proportions of 10, 30, 60, 100 and 150 g of sucrose per 100 g of sorbitol were heat scanned in a DSC to above melting endotherm of sorbitol but well below the onset temperature of melting of sucrose at three different temperatures 110, 130 and 150 degreesC. The heat scanning modes used were with or without isothermal holding. The dissolution of sucrose in the sorbitol liquid melt was manifested by an increase in the glass transition temperature of the melt and corresponding decrease in endothermic melting enthalpy of sucrose. At given experimental conditions, as high as 25 and 85% of sucrose dissolved in the sorbitol melt during 1 h of isothermal holding at 110 and 150 degreesC, respectively. Optical microscopic observation also clearly showed the reduction in the size of sucrose crystals in sorbitol melt during the isothermal holding at those temperatures. (C) 2003 Elsevier Science Ltd. All rights reserved.

Perspectives on the electrically induced properties of electrospun cellulose/liquid crystal devices

A mat of electrospun cellulose fibers are deposed on transparent conductive oxide covered glass, and two such plates enclose a nematic liquid crystal. Thus two new types of Cellulose based Polymer Dispersed Liquid Crystal devices, based on hydroxypropylcellulose and Cellulose Acetate and the nematic liquid crystal E7 have been obtained. The current-voltage characteristics indicates ionic type conduction. Heating-cooling cycles have been applied on the samples and the activation energies have been determined. Simultaneously with the thermo-stimulated currents, the optical transmission dependence on the d.c. electric field and temperature was registered. ON-OFF switching times have been determined for different control voltages. (C) 2011 Elsevier B.V. All rights reserved.

Liquid crystal necklaces: cholesteric drops threaded by thin cellulose fibres

Liquid crystals in confined geometries exhibit numerous complex structures often including topological defects that are controlled by the nematic elasticity, chirality and surface anchoring. In this work, we study the structures of cholesteric droplets pierced by cellulose fibres with planar anchoring at droplet and fibre surfaces. By varying the temperature we demonstrate the role of twisting power and droplet diameter on the equilibrium structures. The observed structures are complemented by detailed numerical simulations of possible director fields decorated by defects. Three distinct structures, a bipolar and two ring configurations, are identified experimentally and numerically. Designing cholesteric liquid crystal microdroplets on thin long threads opens new routes to produce fibre waveguides decorated with complex microresonators.

A cellulose liquid crystal motor: a steam engine of the second kind

The salient feature of liquid crystal elastomers and networks is strong coupling between orientational order and mechanical strain. Orientational order can be changed by a wide variety of stimuli, including the presence of moisture. Changes in the orientation of constituents give rise to stresses and strains, which result in changes in sample shape. We have utilized this effect to build soft cellulose-based motor driven by humidity. The motor consists of a circular loop of cellulose film, which passes over two wheels. When humid air is present near one of the wheels on one side of the film, with drier air elsewhere, rotation of the wheels results. As the wheels rotate, the humid film dries. The motor runs so long as the difference in humidity is maintained. Our cellulose liquid crystal motor thus extracts mechanical work from a difference in humidity.

Light shutters from nanocrystalline cellulose rods in a nematic liquid crystal

This work reports a recently developed electro-optical (EO) device that can potentially be used as a light shutter or a privacy window. By using nanocrystalline cellulose rods, we were able to improve some of the most relevant parameters characterising the EO behaviour. A brief description of the proposed working mechanism for these devices is presented, and numerical simulations based on this mechanism of both the optical transmission and the cells' electrical capacitance are compared with the obtained results, validating the underlying working model considered.