Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 10 of 10 for “"kinetic solubility"”.
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Investigation of Amorphous Solid Dispersions of Poorly Water-soluble Drugs in Poly (2-hydroxyethyl Methacrylate) Hydrogels for Enhanced Solubility and Controlled Release
… supersaturation generation rate on the resulting kinetic solubility profiles of amorphous pharmaceuticals and delineates the interplay between dissolution and precipitation processes from a mechanistic viewpoint. In the absence of any dissolved polymer to inhibit drug precipitation from the …
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Solid Dispersions in Medium-Insoluble Hydrogels for Enhancing the Solubility and Bioavailability of Poorly Soluble Drugs
… emerging approach showing promise for tackling solubility related oral bioavailability problems. However, critical parameters important to the design of these ASDs have not been fully elucidated. Thus, the first part of the present study examines design factors for ASDs based on …
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The precipitation of candidate drugs on mixing DMSO stock solutions with aqueous buffers
… analyses, such as bioassay screening and some solubility screens. Precipitation from these mixtures, whilst a recognised issue, has little in the way of published work. This thesis explores in detail the precipitation of three poorly water soluble, commercially available drug molecules, namely …
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Preformulation solid-state supramolecular beneficiation of selected active pharmaceutical ingredients and a novel drug candidate
… of crystal structures and thermal behaviour. The solubility and thermodynamic stability ranking of the three forms was established and schematic energy-temperature diagrams were constructed through the use of the thermal methods listed above, solvent-mediated transition experiments and by kinetic …
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Synthesis and evaluation of D-cycloserine analogues against mycobacterium tuberculosis
… in rat, mouse and human liver microsomes. The kinetic solubility of the target compounds was determined using a HPLC-based method. The solubility data obtained was then correlated with melting point, tPSA and cLogP in order to establish structuresolubility relationships across the two compounds …
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Synthesis and profiling of antimalarial side-chain modified pyrido[1,2-a]benzimidazoles
… in vivo mouse P. berghei model. However, pharmacokinetic (PK) studies showed oral-limited absorption attributed to poor dissolution or solubility. Thus a series of derivatives was synthesized by making structural modifications to the parent PBI scaffold by distorting the symmetry through …
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Non-Neuroleptic Antitubercular and Anticancer Therapeutics through Rational Drug Remodelling of Phenothiazines and Related Antipsychotics
… chemical synthesis, drug metabolism and pharmacokinetic related properties were predicted in silico to assess drug-likeness of the new chemical entities derived from phenothiazines and related antipsychotics. The in silico profiling also included prediction of blood/brain partition coefficients …
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Synthesis, pharmacological and solubility evaluation of antiplasmodial pyrido[1,2-a]benzimidazoles with cyclic and functionalized amine side chain substituents
… oral bioavailability arising from low aqueous solubility. The mechanism of action of PBI antimalarials remains unknown. In an attempt to address these initial limitations associated with PBIs, and shed light on potential contributing mechanisms of action, PBI analogues containing aliphatic …
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Synthesis, biological activity and physicochemical properties evaluation of antiplasmodial pyrimido[1,2-a]benzimidazoles
… these compounds are beset by poor aqueous solubility and suboptimal in vivo pharmacokinetics (PK), which present barriers to in vivo efficacy improvement. Towards addressing these issues through improved physicochemical properties, in particular solubility, the related …
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Isolation and characterization of African marine natural products and repositioning of the natural product antibiotic fusidic acid and privileged benzimidazole scaffold for tuberculosis and malaria
… at 1 µM. Although it showed poor aqueous kinetic solubility as a free base at pH 7.4, it conformed to Lipinski and Veber rules for oral absorption and bioavailability, while it shared a similar chemical space with the clinically used 4-aminoquinoline drug naphthoquine. The results …