Yes / In order to investigate the effect of using different
solid state forms and specific surface area (TBET) of active
pharmaceutical ingredients on tabletability and dissolution
performance, the mono- and dihydrated crystalline forms of
chlorothiazide sodium and chlorothiazide potassium (CTZK)
salts were compared to alternative anhydrous and amorphous
forms, as well as to amorphous microparticles of chlorothiazide
sodium and potassium which were produced by spray drying and
had a large specific surface area. The tablet hardness and tensile
strength, porosity, and specific surface area of single-component,
convex tablets prepared at different compression pressures were characterized. Results confirmed the complexity of the
compressibility mechanisms. In general it may be concluded that factors such as solid-state form (crystalline vs amorphous), type
of hydration (presence of interstitial molecules of water, dehydrates), or specific surface area of the material have a direct impact
on the tabletability of the powder. It was observed that, for powders of the same solid state form, those with a larger specific
surface area compacted well, and better than powders of a lower surface area, even at relatively low compression pressures.
Compacts prepared at lower compression pressures from high surface area porous microparticles presented the shortest times to
dissolve, when compared with compacts made of equivalent materials, which had to be compressed at higher compression
pressures in order to obtain satisfactory compacts. Therefore, materials composed of nanoparticulate microparticles (NPMPs)
may be considered as suitable for direct compaction and possibly for inclusion in tablet formulations as bulking agents, APIs,
carriers, or binders due to their good compactibility performance / Solid State Pharmaceutical Cluster (SSPC), supported by Science Foundation Ireland under Grant No. 07/SRC/B1158.
| Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/14342 |
| Date | 20 August 2013 |
| Creators | Paluch, Krzysztof J., Tajber, L., Corrigan, O.I., Healy, A.M. |
| Source Sets | Bradford Scholars |
| Language | English |
| Detected Language | English |
| Type | Article, Accepted Manuscript |
| Rights | This document is the Accepted Manuscript version of a Published Work that appeared in final form in Molecular Pharmaceutics, copyright © 2013 American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/mp400124z |
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