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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.
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2013 (Engelska)Ingår i: AAPS PharmSciTech, ISSN 1530-9932, E-ISSN 1530-9932, Vol. 14, nr 1, s. 265-276Artikel i tidskrift (Refereegranskat) 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.

Ort, förlag, år, upplaga, sidor
2013. Vol. 14, nr 1, s. 265-276
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URN: urn:nbn:se:ltu:diva-15810DOI: 10.1208/s12249-012-9883-3ISI: 000319798100031PubMedID: 23297166Scopus ID: 2-s2.0-84878573834Lokalt ID: f5eab951-e3b2-4449-b860-3e53ef2c821bOAI: oai:DiVA.org:ltu-15810DiVA, id: diva2:988785
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Validerad; 2013; 20130110 (andbra)Tillgänglig från: 2016-09-29 Skapad: 2016-09-29 Senast uppdaterad: 2018-07-10Bibliografiskt granskad

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Alhalaweh, AmjadKaialy, WaseemVelaga, Sitaram

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