dc.contributor.author
Huang, Zun
dc.contributor.author
Staufenbiel, Sven
dc.contributor.author
Bodmeier, Roland
dc.date.accessioned
2022-06-03T08:48:14Z
dc.date.available
2022-06-03T08:48:14Z
dc.identifier.uri
https://refubium.fu-berlin.de/handle/fub188/35219
dc.identifier.uri
http://dx.doi.org/10.17169/refubium-34937
dc.description.abstract
Purpose
Solubility and dissolution rate are essential for the oral absorption and bioavailability of poorly soluble drugs. The aim of this study was to prepare nano-co-crystals by combination of nanocrystal and co-crystal technologies, and investigate its effect, in situ, on increased kinetic solubility and dissolution rate.
Methods
Co-crystals of itraconazole-fumaric acid, itraconazole-succinic acid, indomethacin-saccharin and indomethacin-nicotinamide were prepared and nano-sized by wet milling. The particle size and solid state of the co-crystals were characterized by optical microscope, LD, PCS, DSC and XRPD before and after milling.
Results
300-450 nm sized nano-co-crystals with a stable physical solid state were successfully prepared. Nano-co-crystals exhibited a lower crystallinity reduction than nanocrystals after wet milling. The particle size effect on the kinetic solubility of co-crystals was analysed for macro-, micro- and nano-co-crystals with in situ kinetic solubility studies. The maximum kinetic solubility of nano-co-crystals increased with excess conditions until a plateau. The highest increase was obtained with itraconazole-succinic acid nano-co-crystals with a kinetic solubility of 263.5 ± 3.9 μg/mL which was 51.5 and 6.6 times higher than the solubility of raw itraconazole and itraconazole-succinic acid co-crystal.
Conclusions
The synergistic effect of nanocrystals and co-crystals with regard to increased kinetic solubility and dissolution rate was proven. The combination of the advantages of nanocrystals and co-crystals is a promising formulation strategy to increase both the solubility and dissolution rate of poorly soluble drugs.
en
dc.format.extent
13 Seiten
dc.rights.uri
https://creativecommons.org/licenses/by/4.0/
dc.subject
nanocrystals
en
dc.subject
nano-co-crystals
en
dc.subject
in situ methods
en
dc.subject
kinetic solubility
en
dc.subject.ddc
500 Naturwissenschaften und Mathematik::540 Chemie::540 Chemie und zugeordnete Wissenschaften
dc.title
Combination of co-crystal and nanocrystal techniques to improve the solubility and dissolution rate of poorly soluble drugs
dc.type
Wissenschaftlicher Artikel
dcterms.bibliographicCitation.journaltitle
Pharmaceutical Research
dcterms.bibliographicCitation.number
5
dcterms.bibliographicCitation.pagestart
949
dcterms.bibliographicCitation.pageend
961
dcterms.bibliographicCitation.volume
39
refubium.affiliation
Biologie, Chemie, Pharmazie
refubium.affiliation.other
Institut für Pharmazie
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refubium.funding
Springer Nature DEAL
refubium.note.author
Die Publikation wurde aus Open Access Publikationsgeldern der Freien Universität Berlin gefördert.
refubium.resourceType.isindependentpub
no
dcterms.accessRights.openaire
open access
dcterms.isPartOf.eissn
1573-904X