Christoph Saal

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The Orange Book database published by the U.S. Drug and Food Administration (FDA) was analyzed for the frequency of occurrence of different counterions used for the formation of pharmaceutical salts. The data obtained from the present analysis of the Orange Book are compared to reviews of the Cambridge Structural Database (CSD) and of the Martindale "The(More)
High-throughput screening (HTS) is an important method in the pharmaceutical industry for discovering hits that will be further developed into leads, clinical candidates, and eventually into medicines. After an HTS campaign, solubility studies of the discovered hits are an important means to judge the validity of the pharmacological result and to prioritize(More)
A novel analytical method to detect and characterize active pharmaceutical ingredient (API) trace crystallinity in an amorphous system using Raman microscopy and chemometric methods, namely band-target entropy minimization (BTEM) and target transformation factor analysis (TTFA) is developed. The method starts with Raman mapping measurements performed on(More)
Enhanced dissolution of poorly soluble active pharmaceutical ingredients (APIs) in amorphous solid dispersions often diminishes during storage due to moisture-induced re-crystallization. This study aims to investigate the influence of moisture protection on solid-state stability and dissolution profiles of melt-extruded fenofibrate (FF) and ketoconazole(More)
The aim of this study was to assess the usefulness of kinetic and thermodynamic solubility data in guiding medicinal chemistry during lead optimization. The solubility of 465 research compounds was measured using a kinetic and a thermodynamic solubility assay. In the thermodynamic assay, polarized-light microscopy was used to investigate whether the result(More)
In preclinical development, salt forms are often screened to assess their ability to improve drug candidate properties. In this study albendazole was used as a model for poorly soluble, weak basic compounds typical of current drug discovery programs. Four salts, the hydrochloride, mesylate, sulfate und tosylate, were prepared and characterized with respect(More)
Over half of the active pharmaceutical ingredients currently approved within the US are pharmaceutical salts. Selection of suitable pharmaceutical salts is carried out during late research or early development phase. Therefore several properties of different pharmaceutical salts of a new chemical entity are assessed during salt screening and salt selection.(More)