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Article: Cocrystal Engineering of Itraconazole with Suberic acid via Rotary Evaporation and Spray Drying

TitleCocrystal Engineering of Itraconazole with Suberic acid via Rotary Evaporation and Spray Drying
Authors
Issue Date2019
PublisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/crystal
Citation
Crystal Growth & Design, 2019, v. 19 n. 5, p. 2736-2745 How to Cite?
AbstractCocrystallization represents an emerging approach to tackle the issues associated with pharmaceutical product performance and processing, owing to its capability of modifying a variety of physicochemical properties. In this study, we sought to modify the crystal form of itraconazole (ITZ) with suberic acid (SUB) via rapid solvent removal methods, namely rotary evaporation and spray drying. A phase pure ITZ-SUB cocrystal, which could not be obtained by traditional cocrystallization methods, was successfully prepared by rotary evaporation. The new cocrystal was confirmed by powder X-ray diffraction, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. Spray drying was further employed for particle engineering of ITZ-SUB to achieve optimal pulmonary delivery. By manipulating the critical processing parameters, inhalable ITZ-SUB agglomerates with a mass median aerodynamic diameter of 2.56 ± 2.27 μm and fine particle fraction of 64.10% w/w were reproducibly prepared. The inhalable powders contained mainly coamorphous ITZ-SUB, while a small portion of cocrystals still exists. Compared with the raw ITZ, the intrinsic dissolution rate of the ITZ-SUB cocrystal was ∼39 times faster, and a significantly larger fraction of ITZ-SUB agglomerates was dissolved after 180 min of the test. Besides, both products remained stable after 1-month storage at 60 °C.
Persistent Identifierhttp://hdl.handle.net/10722/269603
ISSN
2019 Impact Factor: 4.089
2015 SCImago Journal Rankings: 1.328

 

DC FieldValueLanguage
dc.contributor.authorWeng, J-
dc.contributor.authorWong, SN-
dc.contributor.authorXu, X-
dc.contributor.authorXUAN, B-
dc.contributor.authorWang, C-
dc.contributor.authorChen, R-
dc.contributor.authorSun, CC-
dc.contributor.authorLakerveld, R-
dc.contributor.authorKwok, PCL-
dc.contributor.authorChow, SF-
dc.date.accessioned2019-04-24T08:11:02Z-
dc.date.available2019-04-24T08:11:02Z-
dc.date.issued2019-
dc.identifier.citationCrystal Growth & Design, 2019, v. 19 n. 5, p. 2736-2745-
dc.identifier.issn1528-7483-
dc.identifier.urihttp://hdl.handle.net/10722/269603-
dc.description.abstractCocrystallization represents an emerging approach to tackle the issues associated with pharmaceutical product performance and processing, owing to its capability of modifying a variety of physicochemical properties. In this study, we sought to modify the crystal form of itraconazole (ITZ) with suberic acid (SUB) via rapid solvent removal methods, namely rotary evaporation and spray drying. A phase pure ITZ-SUB cocrystal, which could not be obtained by traditional cocrystallization methods, was successfully prepared by rotary evaporation. The new cocrystal was confirmed by powder X-ray diffraction, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. Spray drying was further employed for particle engineering of ITZ-SUB to achieve optimal pulmonary delivery. By manipulating the critical processing parameters, inhalable ITZ-SUB agglomerates with a mass median aerodynamic diameter of 2.56 ± 2.27 μm and fine particle fraction of 64.10% w/w were reproducibly prepared. The inhalable powders contained mainly coamorphous ITZ-SUB, while a small portion of cocrystals still exists. Compared with the raw ITZ, the intrinsic dissolution rate of the ITZ-SUB cocrystal was ∼39 times faster, and a significantly larger fraction of ITZ-SUB agglomerates was dissolved after 180 min of the test. Besides, both products remained stable after 1-month storage at 60 °C.-
dc.languageeng-
dc.publisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/crystal-
dc.relation.ispartofCrystal Growth & Design-
dc.rightsThis document is the Accepted Manuscript version of a Published Work that appeared in final form in Crystal Growth & Design, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://pubs.acs.org/doi/10.1021/acs.cgd.8b01873#-
dc.titleCocrystal Engineering of Itraconazole with Suberic acid via Rotary Evaporation and Spray Drying-
dc.typeArticle-
dc.identifier.emailChow, SF: asfchow@hku.hk-
dc.identifier.authorityChow, SF=rp02296-
dc.description.naturepostprint-
dc.identifier.doi10.1021/acs.cgd.8b01873-
dc.identifier.scopuseid_2-s2.0-85064167455-
dc.identifier.hkuros297422-
dc.identifier.volume19-
dc.identifier.issue5-
dc.identifier.spage2736-
dc.identifier.epage2745-
dc.publisher.placeUnited States-

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