Miniaturized X-ray powder diffraction assay (MixRay) for quantitative kinetic analysis of solvent-mediated phase transformations in pharmaceutics

dc.accessRightsAnonymous
dc.audienceScience
dc.contributor.authorKirchmeyer, Wiebke
dc.contributor.authorWyttenbach, Nicole
dc.contributor.authorAlsenz, Jochem
dc.contributor.authorKuentz, Martin
dc.contributor.authorGrassmann, Olaf
dc.date.accessioned2016-12-16T11:08:03Z
dc.date.available2016-12-16T11:08:03Z
dc.date.issued2016-11-30
dc.description.abstractMany pharmaceutical compounds exhibit polymorphism, which may result in solvent-mediated phase transformations. Since the polymorphic form has an essential influence on physicochemical characteristics such as solubility or dissolution rate, it is crucial to know the exact polymorphic composition of a drug throughout pharmaceutical development. This study addressed the need to perform quantitative X-ray analysis of polymorphic mixtures on a 96-well scale (MixRay). A calibration of polymorphic mixtures (anhydrate and hydrate) was performed with three model drugs, caffeine, piroxicam, and testosterone, and linear correlations were obtained for all compounds. The MixRay approach for piroxicam was applied to a solubility and residual solid screening assay (SORESOS) to quantify the amount of hydrate and anhydrate corresponding to kinetic bulk concentrations. Changes in these drug concentrations correlated well with the kinetic changes in the residual solid. The influence of excipients on the solid state and kinetic concentrations of piroxicam was also studied. Excipients strongly affected polymorphic transformation kinetics of piroxicam and concentrations after 24h depended on the excipient used. The new calibration X-ray method combined with bulk concentration analysis provides a valuable tool for both pharmaceutical profiling and early formulation development.
dc.description.urihttp://www.sciencedirect.com/science/article/pii/S0731708516304733
dc.identifier.doihttp://dx.doi.org/10.1016/j.jpba.2016.08.028
dc.identifier.issn0731-7085
dc.identifier.issn1873-264X
dc.identifier.urihttp://hdl.handle.net/11654/23743
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofJournal of Pharmaceutical and Biomedical Analysisen_US
dc.subjectMiniaturized assay
dc.subjectQuantitative analysis
dc.subjectSolid state transformation
dc.subjectX-ray diffraction
dc.titleMiniaturized X-ray powder diffraction assay (MixRay) for quantitative kinetic analysis of solvent-mediated phase transformations in pharmaceutics
dc.type01A - Beitrag in wissenschaftlicher Zeitschrift
dc.volume131
dspace.entity.typePublication
fhnw.InventedHereYes
fhnw.IsStudentsWorkno
fhnw.PublishedSwitzerlandNo
fhnw.ReviewTypeAnonymous ex ante peer review of a complete publication
fhnw.affiliation.hochschuleHochschule für Life Sciencesde_CH
fhnw.affiliation.institutInstitut für Pharma Technologyde_CH
fhnw.pagination195-201
fhnw.publicationOnlineJa
fhnw.publicationStatePublished
relation.isAuthorOfPublication74c6fb42-528f-4e81-8dcb-dc9d77a405a4
relation.isAuthorOfPublication68819448-8611-488b-87bc-1b1cf9a6a1b4
relation.isAuthorOfPublication.latestForDiscovery68819448-8611-488b-87bc-1b1cf9a6a1b4
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