and offer an attractive starting point for future drug development.
University of Dundee
ORCID: 0000-0002-9035-4608Publishes on Crystallization and Solubility Studies, X-ray Diffraction in Crystallography, Crystallography and molecular interactions. 19 papers and 406 citations.
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and offer an attractive starting point for future drug development.
OBJECTIVES: In a short approach, we want to present the improvements that have recently been done in the world of new solid forms of known active pharmaceutical ingredients (APIs). The different strategies will be addressed, and successful examples will be given. KEY FINDINGS: This overview presents a possible step to overcome the 10-15 years of hard work involved in launching a new drug in the market: the use of new forms of well-known APIs, and improve their efficiency by enhancing their bioavailability and pharmacokinetics. It discusses some of the latest progresses. SUMMARY: We want to present, in a brief overview, what recently has been done to improve the discovery of innovative methods of using well-known APIs, and improve their efficiency. Multicomponent crystal forms have shown to be the most promising achievements to accomplish these aims, by altering API physico-chemical properties, such as solubility, thermal stability, shelf life, dissolution rate and compressibility. API-ionic liquids (ILs) and their advantages will be briefly referred. An outline of what has recently been achieved in metal drug coordination and in drug storage and delivery using bio-inspired metal-organic frameworks (BioMOFs) will also be addressed.
In recent years, scientific research has neglected the importance of personality and trait emotions in explaining fear of crime. Through a survey administered to 205 individuals, this study explored the relationship between individual variables and abstract fear of crime, perception of victimization risk (cognitive dimension), and behavioral expressions. A positive correlation between neuroticism (a personality dimension) and the abstract fear of crime was observed but not with the cognitive and behavioral dimensions. It was also found that trait fear emotion correlated only with the abstract fear of crime. Contrary to what was hypothesized, social desirability was positively correlated with abstract fear of crime, cognitive dimensions and behavioral dimensions in both men and women. Lastly, regression models revealed that distinct variables explaining each of the fear of crime dimensions exist. The implications of the findings are discussed herein.
Sulfadimethoxine (SDM) cocrystal formation was screened using coformers with cyclic amines, amide, carboxylic acid, and sulfonamide based moieties. Eight new multicomponent crystal forms were obtained by solution crystallization and liquid-assisted grinding techniques, showing a preference for the amine derivatives. Cocrystals were obtained with isonicotinamide (SDM:ISO) and 4,4′-bipyridine (SDM:BIP:ACE; SDM:BIP:H2O), and molecular salts were synthesized with piperazine (SDM:PIP), 4,4′-trimethylenedipiperidine (SDM:TRI), and 1,4-diazabicyclo[2.2.2]octane (two anhydrous polymorphic forms (SDM:DABCO) and one hydrate (SDM:DABCO:H2O)). The new forms were fully characterized by X-ray diffraction. Structural characterization shows the disruption of the typical R22(8) sulfonamide synthon, while the supramolecular arrangement is achieved through several new synthons. In cocrystals, the amide nitrogen Nsulfonamide behaves as the best donor and bonds to the Oacetamide of ISO, while with BIP the interaction is established with the NBIP atom. In salts, charge assisted hydrogen bonds are established, predominantly with the amide nitrogen, the best acceptor, or the sulfonyl O atom, but there is a strong competition with the N atom of the pyrazine ring (Npyrazine). Thermal behavior and physicochemical properties were assessed by thermogravimetric analysis, differential scanning calorimetry, variable temperature powder X-ray diffraction, and hot-stage microscopy techniques. As expected, the molecular salts reveal higher solubility in water than the cocrystals, an important aspect for the improvement of SDM performance.