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Theophylline cocrystals prepared by spray drying: physicochemical properties and aerosolization performance
Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.ORCID-id: 0000-0002-6050-0432
Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
Department of Pharmaceutics, School of Pharmacy, University College London.
Chemistry and Drug Delivery Group, Medway School of Pharmacy, University of Kent.
Vise andre og tillknytning
2013 (engelsk)Inngår i: AAPS PharmSciTech, ISSN 1530-9932, E-ISSN 1530-9932, Vol. 14, nr 1, s. 265-276Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

The purpose of this work was to characterize theophylline (THF) cocrystals prepared by spray drying in terms of the physicochemical properties and inhalation performance when aerosolized from a dry powder inhaler. Cocrystals of theophylline with urea (THF-URE), saccharin (THF-SAC) and nicotinamide (THF-NIC) were prepared by spray drying. Milled THF and THF-SAC cocrystals were also used for comparison. The physical purity, particle size, particle morphology and surface energy of the materials were determined. The in vitro aerosol performance of the spray-dried cocrystals, drug-alone and a drug-carrier aerosol, was assessed. The spray-dried particles had different size distributions, morphologies and surface energies. The milled samples had higher surface energy than those prepared by spray drying. Good agreement was observed between multi-stage liquid impinger and next-generation impactor in terms of assessing spray-dried THF particles. The fine particle fractions of both formulations were similar for THF, but drug-alone formulations outperformed drug-carrier formulations for the THF cocrystals. The aerosolization performance of different THF cocrystals was within the following rank order as obtained from both drug-alone and drug-carrier formulations: THF-NIC > THF-URE > THF-SAC. It was proposed that micromeritic properties dominate over particle surface energy in terms of determining the aerosol performance of THF cocrystals. Spray drying could be a potential technique for preparing cocrystals with modified physical properties.

sted, utgiver, år, opplag, sider
2013. Vol. 14, nr 1, s. 265-276
HSV kategori
Forskningsprogram
Hälsovetenskap
Identifikatorer
URN: urn:nbn:se:ltu:diva-15810DOI: 10.1208/s12249-012-9883-3ISI: 000319798100031PubMedID: 23297166Scopus ID: 2-s2.0-84878573834Lokal ID: f5eab951-e3b2-4449-b860-3e53ef2c821bOAI: oai:DiVA.org:ltu-15810DiVA, id: diva2:988785
Merknad
Validerad; 2013; 20130110 (andbra)Tilgjengelig fra: 2016-09-29 Laget: 2016-09-29 Sist oppdatert: 2018-07-10bibliografisk kontrollert

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Alhalaweh, AmjadKaialy, WaseemVelaga, Sitaram

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