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This study was performed to investigate which human organic cation transporter, hOCT1, hOCT2 or hOCT3, participates with regard to cation specificity and membrane localization in the intestinal absorption of orally available cationic drugs. Inhibition of N-[methyl-3H]4-phenylpyridinium ([3H]MPP+) uptake by various compounds into Caco-2 cells and into cells(More)
Microemulsions are modern colloidal drug carrier systems. They form spontaneously combining appropriate amounts of a lipophilic and a hydrophilic ingredient, as well as a surfactant and a co-surfactant. Due to their special features, microemulsions offer several advantages for pharmaceutical use, such as ease of preparation, long-term stability, high(More)
The separation of the major stratum corneum lipids, i.e., ceramides, fatty acids, cholesterol and its esters by means of high-performance thin-layer chromatography is hereby presented. The used automated multiple development technique allows the reproducible development of a 17-step solvent gradient also capable of separating seven ceramide classes in the(More)
In this work, amorphous atorvastatin calcium nanoparticles were successfully prepared using the supercritical antisolvent (SAS) process. The effect of process variables on particle size and distribution of atorvastatin calcium during particle formation was investigated. Solid state characterization, solubility, intrinsic dissolution, powder dissolution(More)
Purpose. This study on the intestinal transport of β-lactam antibiotics was undertaken to investigate the correlation between cellular transport parameters and the bioavailability. Methods. Transport of 23 β-lactam antibiotics was characterized by measuring their ability to inhibit the uptake of glycylsarcosine into Caco-2 cells, their uptake into the cells(More)
Vehicle dependent effects on the penetration behavior of drugs following topical application are well known from the literature. In this context, many reports concerning the enhancing activities for hydrophilic as well as lipophilic substances by colloidal drug carrier systems, particularly microemulsions, are available. However, there is little knowledge(More)
The influence of the chain length of the free fatty acid (FFA) in a stratum corneum (SC) lipid model membrane composed of N-(α-hydroxyoctadecanoyl)-phytosphingosine (CER [AP]), cholesterol (Ch), FFA and cholesterol sulphate (ChS) was investigated by neutron diffraction. The internal nanostructure of the SC lipid membrane in addition to the water(More)
Angiotensin-converting enzyme (ACE) inhibitors are often regarded as substrates for the H+/peptide transporters (PEPT)1 and PEPT2. Even though the conclusions drawn from published data are quite inconsistent, in most review articles PEPT1 is claimed to mediate the intestinal absorption of ACE inhibitors and thus to determine their oral availability. We(More)
The structure and hydration of a stratum corneum (SC) lipid model membrane composed of N-(α-hydroxyoctadecanoyl)-phytosphingosine (CER6)/cholesterol (Ch)/palmitic acid (PA)/cholesterol sulfate (ChS) were characterized by neutron diffraction. The neutron scattering length density across the SC lipid model membrane was calculated from measured diffraction(More)
The thermotropic and lyotropic phase behaviour of mixtures of ceramides type IV and cholesterol was investigated using Fourier transform (FT) Raman spectroscopy and differential scanning calorimetry (DSC). In the dry and in the fully hydrated state of these mixtures the DSC-curves exhibit an eutectic melting followed by the melting of the residual solid(More)