Pharmaceutical solid state · Industry updates · Page 4
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MicroED determined a powder-derived cocrystal of 2-aminopyrimidine and succinic acid prepared by solid-state grinding. The mechanically generated phase was not accessible through the solution-crystallization route examined. This is a model organic cocrystal rather than an API efficacy study, illustrating how electron diffraction can characterize crystal-engineering products without first recreating them as large solution-grown crystals.
Researchers analyzed micron-sized powders of SMTP-7 and its diastereomer to resolve stereochemical assignments. Kinematical refinement combined with additional chiral information and dynamical refinement provided complementary routes. The work demonstrates absolute-configuration analysis for complex, hard-to-crystallize drug candidates with limited material, while distinguishing what can be inferred from conventional refinement and what requires dynamical treatment.
This review examines three-dimensional electron diffraction for beam-sensitive small-molecule nanocrystals, with a pharmaceutical-industry perspective. It discusses experimental strategies, diffraction completeness, dynamical scattering, and structural applications that extend beyond conventional large-crystal requirements. It provides a methods-oriented framework for interpreting published demonstrations; it does not establish a universal preparation method or replace sample-specific feasibility assessment.
Three-dimensional electron diffraction and scanning transmission electron microscopy resolved the layered structure and stacking variations of bismuth subsalicylate, a long-used pharmaceutical ingredient. Clustering compatible diffraction datasets helped obtain the ordered structural model, while imaging exposed disorder. The paper shows why complementary electron-crystallography techniques can be valuable when small crystals and structural defects obstruct conventional characterization.
The authors determined the absolute configuration of a preclinical API by forming a salt with a chiral reference and analyzing its microcrystalline powder using MicroED. This approach transfers known stereochemical information from the salt former to the API. It addresses situations where large crystals cannot be obtained, but depends on a suitable, well-characterized chiral reference.
Three-dimensional electron diffraction showed that solution-grown and melt-grown materials previously grouped as delta-indomethacin have different crystal structures. The authors retained delta for the solution-grown form and proposed theta for the melt-grown form. Both displayed plastic bending associated with molecular slip. This case demonstrates how structural measurements can resolve longstanding ambiguity in polymorph identity.
Researchers solved a previously unresolved indomethacin form by three-dimensional electron diffraction and related its packing to infrared and Raman observations. They measured faster dissolution than the better-characterized alpha and gamma forms and observed a solid-state transition to alpha. This is a solid-form structure–property study; laboratory dissolution results do not by themselves establish improved human bioavailability.
Researchers described a pharmaceutical MicroED service workflow after examining more than fifty client-submitted small-molecule samples. Most yielded diffraction data suitable for structure solution, and validation examples included common reference compounds and teniposide. The paper documents preparation, collection, processing, and typical obstacles; its selected service cohort does not establish a universal success rate.
This study combined MicroED with crystal structure prediction to support solid-form selection for remdesivir. Experimentally determined structural information was evaluated alongside computational crystal-energy analysis, demonstrating a joint experimental and modeling approach when conventional large-crystal growth is difficult. The work concerns solid-state characterization and selection, not a new assessment of antiviral efficacy or clinical performance.
Researchers combined room-temperature, limited-resolution three-dimensional electron diffraction with density-functional energy minimization to determine metastable loratadine Form II. Direct methods were insufficient because of resolution, disorder, and possible beam-induced amorphization. Simulated annealing generated candidate models, and computational validation selected the correct structure, illustrating a complementary experimental and computational workflow for challenging pharmaceutical polymorphs.
Combining cryogenic specimen preparation with three-dimensional electron diffraction, researchers followed glycine crystallization from water. Different samples captured the sequential appearance of its three ambient-pressure polymorphs, including a short-lived beta form before alpha became dominant. Structures could be obtained from very small crystallites, demonstrating how diffraction can reveal phases missed by slower bulk measurements.
Researchers solved the previously unknown crystal structure of orthocetamol, a pharmaceutical compound that had not yielded single crystals suitable for X-ray diffraction. The approach combined low-dose three-dimensional electron-diffraction acquisition with a single-electron detector. The case illustrates structure determination from challenging small crystals rather than requiring successful growth of larger specimens first.
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