Pharmaceutical solid state · Industry updates · Page 2
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A laboratory study compared single-stage and two-stage MSMPR crystallization for paracetamol Form I and carbamazepine Form III at matched total active volume and residence time. Staging improved particle uniformity, reduced fouling, and shortened filtration times while preserving solid-state and chemical quality. The findings attribute the benefit to supersaturation distribution rather than additional crystallizer capacity.
Electron diffraction established the previously unresolved structure of buspirone hydrochloride Form 2. The study also prepared 15 multicomponent solids, including cocrystals, an ionic cocrystal, and salts, and compared conformations and thermal behavior. This expands structural knowledge of a long-marketed drug and provides a solid-form exploration example without demonstrating improved clinical performance for the newly prepared materials.
Molecular dynamics simulations examined tecovirimat across solvent and concentration conditions. Molecular conformations changed relatively little, while intermolecular association patterns differed substantially between benzene and ethyl acetate. Those associations resembled packing motifs in known anhydrous polymorphs IV and VI. The study offers a mechanistic computational explanation; it does not establish prospective experimental prediction of polymorph outcomes.
Researchers prepared myricetin cocrystals with diprophylline and theobromine and evaluated structure, stability, moisture sensitivity, dissolution, and in vivo absorption. Both forms improved in vitro solubility and reduced hygroscopicity. However, their pharmacokinetic behavior did not simply track the solubility gains, reinforcing the need to assess solid-form performance across laboratory and biological endpoints rather than a single property.
A new review surveys pharmaceutical cocrystals beyond the commonly studied 1:1 stoichiometry, covering preparation methods, characterization, and relationships between composition and physical properties. It discusses solution crystallization, mechanochemistry, and vapor-induced transformations alongside challenges in formation-rule prediction, metastable-phase stabilization, and scale-up. This is a research synthesis, not a new clinical result or regulatory endorsement of particular cocrystal products.
Researchers studied flurbiprofen–polyvinylpyrrolidone amorphous solid dispersions using controlled nucleation and real-time synchrotron X-ray diffraction after contact with water. Higher nucleation density shortened the lag before crystallization and accelerated drug crystallization. The work proposes that evaluating latent nuclei is important to maintaining supersaturation, rather than assuming the absence of visible crystals demonstrates a robust amorphous formulation.
The authors reported a cryo-MicroED structure of cefadroxil, characterizing its molecular geometry, stereochemistry, and intermolecular packing. The crystallographic model also supported complementary molecular-dynamics analysis. This is a structural case study of an established beta-lactam antibiotic; the accompanying computational work should not be interpreted as clinical evidence of a new neurotherapeutic benefit or a general performance guarantee.
Revisiting ritonavir’s polymorph landscape, the authors examined whether crystal structure prediction could have flagged the risk posed by the less soluble Form 2. They also solved the previously unresolved Form 4 structure using 3D electron diffraction, modeling, and powder X-ray diffraction, finding disorder and thermodynamic instability. The retrospective analysis informs risk assessment rather than guaranteeing future polymorph prediction.
MicroED identified two polymorphic structures of oxyacanthine dihydrochloride monohydrate in samples mislabeled as berbamine dihydrochloride. The forms differed principally in the conformation of a tetrahydroisoquinoline ring. Structural, energetic, and packing analyses suggested a thermodynamic preference between them. The study demonstrates how crystallographic analysis can expose both identity problems and polymorphism in complex natural-product samples.
3D ED/MicroED determined casopitant mesylate Forms 1 and 3 from one batch of fine powder containing an inseparable polymorphic mixture. Their structures differed through a small packing shift, explaining their very similar powder X-ray diffraction patterns. The work demonstrates how selecting individual microcrystals can resolve structurally similar phases that remain difficult to separate or distinguish in bulk measurements.
This study characterized indomethacin–nicotinamide cocrystals using MicroED together with solid-state NMR, Raman spectroscopy, and powder X-ray diffraction. MicroED supplied the crystal structure, while NMR helped examine molecular interactions. The combined approach addressed properties that individual methods could not establish alone, offering a pharmaceutical cocrystal workflow relevant to API powders and formulations containing excipients.
The study examined API crystals directly in Allegra, Clarith, and Ibrance tablets using selected-area 3D ED/MicroED. Fexofenadine hydrochloride Form I and clarithromycin Form II retained their polymorphs, while palbociclib Form A showed slight lattice shrinkage. The results demonstrate formulation-level structural analysis and emphasize that a lattice change and a new polymorph are different findings.
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