Mathematical modeling of drug delivery from cylindrical implantable devices

A mechanistic mathematical model applicable to the controlled dispersed‐drug release from cylindrical device such as implantable drug delivery system was derived. Analytical solutions based on the pseudosteady state approximation are derived taken account an exact external medium volume. The model prediction is accurate when the initial drug load is higher than the drug solubility in the polymer. The results obtained are compared with the analytical solutions available in the literature. The equations are corroborated by comparison with experimental profiles reported in the literature for sink conditions and non sink conditions. The evolution of concentration distribution profiles is compared for different volume of external medium. A reduction in the volume of the external solution leads to an increase in the concentration on the surface of the device, which determines decreases in the release of drug. One criterion for determining whether the volume of external solution should be considered for the prediction of drug release from cylindrical devices is established. This criterion is based on establishing a maximum percentage error allowed in the values of amount of drug released. The usefulness of the model is focused in the design of implant for controlled release of drug into a small volume of external medium of release. Copyright © 2014 John Wiley & Sons, Ltd.     

Adsorption of naphthalene and pyrene from isooctane solutions on commercial activated carbons

The adsorption of naphthalene and pyrene on two different types of commercial activated carbons was studied by batch and column experiments. Adsorption equilibrium was measured at three different temperatures. Heats of adsorption were estimated from the equilibrium results and compared to other previous reports. From the column experiments, using parameters obtained from the batch experiments and literature correlations, effective surface diffusivities were estimated for naphthalene and pyrene on both adsorbents in different feed concentrations. The corrected diffusivities, using Darken equation, appear to be almost constant for naphthalene (ca. 1.3⋅10⁻⁸ cm²/min), and for pyrene (ca. 2.3⋅10⁻¹⁰ cm²/min), in both activated carbons.     

Efficient synthesis and free-radical scavenging capacity of new 2,4-substituted tetrahydroquinolines prepared via BiCl<Subscript>3</Subscript>-catalyzed three-component Povarov reaction,using <Emphasis Type="Italic">N</Emphasis>-vinylamides

Efficient synthesis of new structurally different 2-(het)aryl-4-amidyl-substituted tetrahydroquinolines 8–29 is reported. The synthesis based on BiCl₃-catalyzed three-component Povarov reaction between anilines, (het)aryl aldehydes and enamides offers a fast, safe, and cheap way for efficient tetrahydroquinoline libraries construction. Using N-vinylamides (N-vinylpyrrolidin-2-one and N-vinylacetamide) in this reaction, it was possible to obtain two series of different cis tetrahydroquinolines with antioxidant properties. Among 14 tested compounds, 7 tetrahydroquinolines revealed a prominent anti-radical capacity, equal or higher than that of the commercial antioxidants. Being the most active molecule, the N-[2-(α-furanyl)-6-methoxy-1,2,3,4-tetrahydroquinolin-4-yl] acetamide 21 was ca. 2.2-fold more potent than the well-known antioxidant, vitamin E (α-tocopherol).     

Dominant vertices in regulatory networks dynamics

Discrete-time regulatory networks are dynamical systems on directed graphs with a structure that is inspired on natural systems of interacting units. Using a notion of determination between vertices, we define sets of dominant vertices, and we prove that in the asymptotic regime, the projection of the dynamics on a dominant set allows us to determine the state of the whole system at all times. We provide an algorithm to find sets of dominant vertices, and we test its accuracy on several examples. We also explore the possibility of using the dominant set characteristics as a measure of the structural complexity of networks.     

Application of sulfobutylether-beta-cyclodextrin with specific degrees of substitution for the enantioseparation of pharmaceutical mixtures by capillary electrophoresis.

In this research the separation of the enantiomers of the basic drug bidisomide (SC-40230) from five closely related known process impurities was investigated using several neutral and anionic sulfobutylether beta-cyclodextrins (SBE-beta-CDs) as isomer selectors. Several novel sulfobutylether derivative mixtures and purified charge types having a specific degree of substitution were used to study the effect of selector charge on the efficiency and selectivity of both chiral and achiral separations. The effects of run buffer pH, selector type, and selector concentration on the chiral separation of bidisomide and the achiral separation of the related process impurities was also investigated. The related process impurity, SC-47500, displayed significant peak tailing with SBE-beta-CD mixtures which contained mono- to deca-substituted cyclodextrins. This problem was explored using isolated SBE-beta-CD charge types having degrees of substitution from one to seven. Peak tailing increased as the charge on the selector increased, suggesting that the distortion was due to electrodispersion and the large countercurrent mobility of the negatively charged complexes. Pure charge types having a lower degree of substitution provided adequate chiral and achiral selectivity, while eliminating the severe peak distortion caused by electrodispersion. The complete analysis of the bidisomide enantiomers and the related impurities was achieved with a pH 2.5 running buffer containing 5-10 mM of the isolated sulfobutylether charge types SBE[2]ds(1)sr-beta-CD or SBE[3]ds(1)sr-beta-CD. These conditions gave baseline resolution of bidisomide enantiomers and all five impurities, thus allowing both chiral and achiral purity to be determined in a single run.     

Chemical CdS Thin-Film Deposition Influenced by External Electric and Magnetic Fields

Cadmium sulfide polycrystalline thin films were grown on glass substrates by the chemical-bath deposition technique (CBD) under application of both a pulsating direct electric and a dc magnetic field acting on the Cd- and S-ions during growth in an aqueous solution which contains CdCl₂ and thiourea as source material for the cadmium and sulfur components, respectively. The field orientation in each case of deposition was chosen perpendicular as well as parallel to the growing CdS-film interface. Two different values of the magnetic field strength were applied. Various properties of the films were studied, such as optical transmission and reflection, surface morphology, X-ray diffraction, and dark electrical resistivity, as a function of the applied field configurations, which reveal a clear effect of the field presence during growth.     

Poly(N‐acetyl‐α‐acrylic acid): Synthesis,Characterization and Chelation Properties through Liquid Phase Polymer‐Based Retention Technique

The synthesis and characterization of the water‐soluble poly(N‐acetyl‐α‐acrylic acid) by radical polymerization were carried out. The polymer was characterized by Fourier Transform Infrared (FT‐IR), ¹H NMR and ¹³C NMR spectroscopies, and thermogravimetric analysis (TGA). The metal ion binding properties for the metals Cu(II), Co(II), Ni(II), Cd(II), Zn(II), Pb(II), Hg(II), Cr(III) in the aqueous phase were studied using the liquid‐phase polymer‐based retention technique. The metal ion interactions with the hydrophilic polymer were determined as a function of pH and of the filtration factor. The polychelatogen showed a high affinity for metal ions and higher selectivity for Cr(III) at pH = 3.     

Chelating properties of poly(N‐acryloyl piperazine) by liquid‐phase polymer‐based retention (LPR) technique

The synthesis of poly(N‐acryloylpiperazine) was carried out by radical polymerization giving a yield of 90%. The polymer was soluble in water and was characterized by FTIR, ¹H NMR, ¹³C NMR spectroscopy, and TGA. The metal ability binding properties for the Ag(I), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Pb(II), and Cr(III) metal ions in the aqueous phase were investigated using the liquid‐phase polymer‐based retention (LPR) method. The metal ion interactions with the hydrophilic polymers were determined as a function of pH and filtration factor.