PubMed · 14131556
The source did not provide an abstract. Follow the original record for more information.
Explore connections, maps & timelines
I PERSSON. 1964-04-16. [PHENFORMIN].. https://pubmed.ncbi.nlm.nih.gov/14131556/
Cite the original work for its findings. Save a collection to share your selection of sources.
KEEP EXPLORING
The preparation of colloidal particles of different morphologies, including spheres, of two drugs, loratadine and danazol, is described. In principle these particles were obtained by precipitation when nonsolvents (water or aqueous surfactant solutions) were added to ethanol solutions of the drug. In addition, procedures were developed that made it possible to use the drug particles thus obtained as cores to be then coated with either silica or aluminum (hydrous) oxide layers. The presence of these inorganic shells was confirmed by electron microscopy, energy dispersive spectroscopy, and electrophoresis.
The successful practice of medicinal chemistry is crucially dependent on the principles of molecular recognition: the first and "fundamental" requirement for a drug is to bind to its target; specificity, or at least selectivity, of binding is also a must. Subsequent optimization steps to develop a lead compound into a drug are a complex mixture of processes that are not yet fully understood or predictable. Fortunately, criteria exist to discard leads that would be intractable for optimization. The concepts of non-lead-likeness and lead-likeness, in respect to drug-likeness and non-drug-likeness, have prompted a rich discussion in the recent medicinal chemistry literature. The fragment approach is an emerging philosophy in the process of lead compound discovery. The basic interactions responsible for binding affinity are defined from the "protein interactions world" and key structural fragments are combined according to the criteria of three-dimensional diversity to find new leads. New techniques in screening are used for the detection of the weaker interactions of fragments with their targets that might be undetectable in classical biological assays.
The concepts of high-throughput (HT) screening and combinatorial synthesis have been integrated into the pharmaceutical discovery process, but are not yet commonplace in the pharmaceutical development arena. Emerging strategies to speed pharmaceutical development and capture solid form diversity of pharmaceutical substances have resulted in the emergence of HT crystallization technologies. The primary type of diversity often refers to polymorphs, which are different crystal forms of the same chemical composition. However, diverse salt forms, co-crystals, hydrates and solvates are also amenable to study in HT crystallization systems. The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control. This review highlights the opportunities and challenges of HT crystallization technologies as they apply to pharmaceutical research and development.