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  • 1
    ISSN: 1435-1536
    Keywords: Key words Surface pressure ; Phospholipid monolayers ; Dynamic and static conditions ; Emulsion stability ; Interfacial tension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Notes: Abstract The effect of the interaction between phospholipid monolayers and PEG-660-12-hydroxy stearate as a non-ionic surfactant on lipid emulsion stability in dynamic and static conditions was studied. The presence of PEG-660-12-hydroxy stearate molecules with phospholipid monolayers (static state) leads to a remarkable increase in the surface pressure (from 5 to 30 mN/m in the initial molecular area), whereas in the dynamic state, when the two emulsifiers are separated and each dissolved in one phase of the two emulsion phases, a sudden decrease in the surface pressures is observed. This indicates that PEG-660-12-hydroxy stearate molecules are intercalated between the phospholipid monolayers forming a molecular mixed film. At the same time, a part of the phospholipid monolayers interacts with the surfactant monomers to form a soluble or partially soluble association complex. This interpretation was also supported by interfacial tension measurements, where the interfacial tension in the dynamic state was lower than that in the static one. This indicates that in static conditions the phospholipids partially interact with PEG-660-12-hydroxy stearate resulting in a non-active association complex. Subsequently there is insufficient utilization of the available surfactants during the emulsification process. In contrast, in dynamic conditions both emulsifiers are available at the free surface from the beginning. This behaviour was substantiated by investigating the stability of emulsions which were prepared either by the static condition or the dynamic one during the autoclaving process.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 882-888 
    ISSN: 1573-904X
    Keywords: liposomes ; octanol ; partitioning ; solubility ; absorption ; phospholipids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Appropriate physicochemical parameters are desired for the prediction of passive intestinal drug absorption during lead compound selection and drug development. Methods. Liposome distribution coefficients measured titrimetrically and solubility data at pH 6.8 were used to characterize 21 structurally diverse ionizable drugs covering a range from 〈5% to almost complete absorption. Results. A sigmoidal relationship was found between the percentage of human passive intestinal absorption and a new absorption potential parameter calculated from liposome distribution data and the solubility dose ratio. In contrast, the human absorption data did not correlate with an octanol-based absorption potential or partitioning data alone. Poor correlations were found between liposome and octanol partitioning of ionic species or nonionic bases indicating the profound differences of the partitioning systems. Conclusions. Liposome distribution coefficients of ionizable drugs derived by a pH-metric titration were successfully used to calculate a parameter that correlates with the percentage of passive intestinal absorption in humans. Profound differences between liposome and octanol partitioning were found for a highly diverse set of species. This titration technique may serve to generate liposome partitioning data for the selection and optimization of lead compounds and in drug development.
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  • 3
    ISSN: 1435-1536
    Keywords: Amplitudengewichtete Phasenstrukturation ; Elektrophorese ; Laserstreulichtverfahren ; Teilchengrößenbestimmung ; Zetapotential
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Description / Table of Contents: Abstract With AWPS (Amplitude Weighted Phase Structuration), a new signal processing scheme is demonstrated for the simultaneous determination of zeta potentials and particle sizes. It allows the measurements of a small electrophoretic mobility in the presence of large particle diffusion and constant velocity, e. g. due to thermal convection. Laser light scattering techniques instead of the former methods determine electrophoretic velocity more objectively and precisely. The applicability of laser measurement techniques by analysis of the frequency spectrum is limited for particles ≪50 nm or very low potentials, because of the broadening of the spectral peak by Brownian motion. In contrast to AWPS a separation of the various kinds of collective motion is not possible. The presented results demonstrate that this separation is of considerable significance in the acquisition of reliable values. Additionally the novel signal processing scheme allows a significant increase in sensitivity and therefore the application of an oscillating field (50–100 Hz) with a very small field strength. The system is feasible for particle sizes in the range of a few nm up to several μm. Its high resolution allows experiments with low fields or with small zeta potentials, even in the critical particles size range of a few nanometers.
    Notes: Zusammenfassung Mit AWPS (Amplitudengewichteter Phasenstrukturation) wird ein neues Signalverarbeitungssystem zur gleichzeitigen Bestimmung von Zetapotential und Partikelgröße vorgestellt. Es erlaubt die Messung geringer elektrophoretischer Beweglichkeiten in Gegenwart einer starken Diffusion der Partikel sowie einer überlagerten konstanten Geschwindigkeit, z. B. aufgrund eines Konvektionssthermes. Laserstreulichtverfahren anstatt der bisherigen Methoden bestimmen die elektrophoretische Geschwindigkeit objektiver und präziser. Die Anwendbarkeit der Lasertechniken, die über die Analyse des Frequenzspektrums arbeiten, ist begrenzt für Partikel ≪s50 nm oder sehr niedrige Potentiale, aufgrund der Verbreiterung des spektralen Peaks durch die Diffusionsbewegung. Im Gegensatz zu AWPS ist eine Auftrennung in die verschiedenen Komponenten der kollektiven Bewegung nicht möglich. Die vorgelegten Ergebnisse belegen, daß diese Auftrennung von beträchtlicher Bedeutung ist, um verläßliche Werte zu erhalten. Das neue Signalverarbeitungssystem ermöglicht zusätzlich einen bedeutenden Zuwachs an Empfindlichkeit und daher die Anwendung eines oszillierenden Feldes (50–100 Hz) mit sehr geringer Feldstärke. Das System ist anwendbar für Partikelgrößen im Bereich von wenigen nm bis zu einigen μm. Seine hohe Auflösung ermöglicht Experimente mit kleinen Feldern oder mit niedrigen Zetapotentialen, besonders im kritischen Teilchengrößenbereich von einigen Nanometern.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1435-1536
    Keywords: Nanoparticles ; acrylic acid copolymer ; ethoxylated surfactants ; hydrophobic interaction chromatography (HIC) ; poloxamer ; poloxamine ; antarox
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Notes: Abstract Copolymer nanoparticles of acrylic acid, acrylic amide, acrylic butylester, and methacrylic methylester with increasing content of acrylic acid were produced and surface-modified by adsorption of nonionic (Poloxamer 407, Poloxamine 908, Antarox CO 990) and ionic (Gafac RE 960) surfactants. The coated particles were characterized with regard to parameters relevant for the in vivo organ distribution: coating layer thickness, charge-reducing effect of the coating layer and surface hydrophobicity. Gafac was found to form highly charged surface layers leading to recognition by the reticuloendothelial system (RES). The hydrophobicity of the coating layers decreased with increasing thickness. The thickest coating layers were found on the most hydrophobic particles possessing least content of acrylic acid (1.9%). These particles coated with the nonionics were regarded as sufficiently hydrophilic to potentially reduce the uptake by the RES in vivo. The properties of coating layers can therefore be optimized by variation of the monomer ratios in copolymers.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1435-1536
    Keywords: Key words Powdered cellulose ; Microcrystalline cellulose ; Physicochemical properties ; Homogenisation process
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Notes: Abstract  The physicochemical properties of different types of powdered cellulose (PC) and microcrystalline cellulose (MCC) were studied by examining the changes in particle size, viscosity and specific surface area after a homogenisation process. An additional characterisation was carried out using X-ray diffractometry. A preliminary investigation using a type of MCC showed that increasing the homogenisation pressure and the number of passage cycles led to a significant decrease in the particle size and simultaneously to a remarkable increase in the specific surface area and viscosity. Most MCC types showed the same pattern during the homogenisation process. “Colloidal” MCC displayed a higher viscosity than the others but without significant change in the viscosity after different homogenisation cycles. In contrast to this behaviour of the MCCs, the PCs showed no remarkable change in the particle size but did show a marked change in their viscosity. Furthermore, only MCC suspensions, with the exception of “colloidal” MCC, agglomerated after the homogenisation process, whereas this was not seen in the PC suspensions. Hence, since the MCC types as well as the PC types originally had the same chemical structure, this different behaviour among these types can only be attributed to their different physical properties.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Pharmacy world & science 1 (1979), S. 449-456 
    ISSN: 1573-739X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Two polymorphic forms of acetohexamide have been characterised using differential scanning calorimetry, scanning electron microscopy and X-ray diffraction. For both polymorphic forms the dissolution rates and solubilities have been investigated. The phosphate buffer (pH 7.6) prescribed in the usp xix as the medium for the dissolution test of acetohexamide tablets cannot be used, because a less soluble potassium salt crystallises during the dissolution process.
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  • 7
    Publication Date: 1979-01-01
    Print ISSN: 0021-8820
    Electronic ISSN: 1881-1469
    Topics: Chemistry and Pharmacology , Medicine
    Published by Springer Nature
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  • 8
    Publication Date: 1983-01-01
    Print ISSN: 0021-8820
    Electronic ISSN: 1881-1469
    Topics: Chemistry and Pharmacology , Medicine
    Published by Springer Nature
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  • 9
    Publication Date: 1999-04-07
    Print ISSN: 0372-820X
    Electronic ISSN: 1435-1536
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Published by Springer
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  • 10
    Publication Date: 1999-12-01
    Print ISSN: 0024-4201
    Electronic ISSN: 1558-9307
    Topics: Biology , Chemistry and Pharmacology
    Published by Springer
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