Conformational restriction strategies to increase the activity and selectivity of the STAT5b inhibitor Stafib‐2 are presented. The best conformationally restricted inhibitor Stafib‐2‐CR has threefold higher activity against STAT5b than Stafib‐2. A cell‐permeable prodrug of Stafib‐2‐CR inhibits phosphorylation of STAT5b in cultured human leukemia cells ...
Theresa Münzel +5 more
wiley +1 more source
Engineering Cocrystals of Poorly Water-Soluble Drugs to Enhance Dissolution in Aqueous Medium
Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aqueous ...
Indumathi Sathisaran +1 more
doaj +1 more source
Application of Twin Screw Extrusion in the Manufacture of Cocrystals, Part I: Four Case Studies
The application of twin screw extrusion (TSE) as a scalable and green process for the manufacture of cocrystals was investigated. Four model cocrystal forming systems, Caffeine-Oxalic acid, Nicotinamide-trans cinnamic acid, Carbamazepine-Saccharin, and ...
Karthik Nagapudi +4 more
doaj +1 more source
Daidzein cocrystals: An opportunity to improve its biopharmaceutical parameters
The present study involves the contribution of cocrystallization towards the modification of the biopharmaceutical parameters of poorly watersoluble plant-originated isoflavone, daidzein (DAID). The cocrystals were prepared with GRAS status coformers i.e.
Yashika Bhalla +3 more
doaj +1 more source
Low aqueous solubility and concomitant oral bioavailability are the major glitches found in converting the active pharmaceutical ingredients to new pharmaceutical products. Many methods are in existence to improve the solubility of poorly water-soluble drugs.
Vinod Kumar K +5 more
openaire +1 more source
Energetic cocrystals – structural studies of nitrotriazolone salts and cocrystals [PDF]
Hayleigh J. Lloyd +2 more
openaire +1 more source
The cocrystals of isorhamnetin and isoliquiritigenin with 4,4'-bipyridine: system characterization, stability, dissolution and anticancer activity. [PDF]
Liu Y +8 more
europepmc +1 more source
Systematic Scale-Up of Mechanochemical Paracetamol-Oxalic Acid Cocrystal Synthesis across Multiple Milling Technologies. [PDF]
Schöbel JH, Gopinath D, Felderhoff M.
europepmc +1 more source
Heavy-atom functionalization promotes triplet-assisted charge-transfer exciton transport in organic cocrystals. [PDF]
Xiao Y +8 more
europepmc +1 more source
Crystals as Rockets: Modulation of the Salient Temperature in Cocrystals by Solvent Mixture Composition. [PDF]
Hernández-Morales EA +5 more
europepmc +1 more source

