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Dissolution and precipitation behavior of ternary solid dispersions of Ezetimibe in biorelevant media: AAPS annual meeting and Exposition2014 USA
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0002-2273-457X
Umeå university.
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0002-0654-5410
2014 (English)Conference paper, Poster (with or without abstract) (Other academic)
Abstract [en]

PurposeTo prepare ternary solid dispersions of Ezetimibe (EZ) and investigate their powder dissolution and precipitation behavior(supersaturation) in simulated gastric and intestinal fluidsMethodsTernary solid dispersions of EZ were prepared with PVPK30 and Poloxamer 188 at different ratios. Spray drying and meltquenching methods were used for the preparation of these solid dispersions. The solid dispersions were characterized bybasic to advanced solid-state tools including Modulated differential scanning calorimetry (MDSC), Powder X-ray diffractionand Fourier transform infrared spectroscopy .Biorelevant simulated media (FaSSIF pH 6.5 and FaSSGF pH1.6) were used tostudy the supersaturating solubility of the ternary solid dispersions. HPLC was used to determine the drug concentrationsResultsTernary solid dispersions were successfully prepared by spray drying and melt quench methods. All prepared soliddispersions showed broadening of the XRD peaks indicating amorphous nature. MDSC analysis revealed disappearance ofthe melting peak of Ezetimibe indicating that molecular dispersion of the drug in polymer matrix. The solid dispersions withhigher PVPK30 content showed single Tg at 158.54 °C (spray drying) and 169.32 °C (melt quench). About 10 folds increasein the apparent solubility was observed for solid dispersions prepared by both methods. However, melt quenched soliddispersions had maintained the supersaturation solubility in FaSSIF longer than spray dried solid dispersions. Dissolutionstudies in FaSSGF are ongoingConclusionAmorphous ternary solid dispersions of Ezetimibe containing PVP K30 and Poloxamer 188 could be prepared by spraydrying and melt quenching methods. These solid dispersions showed improved solubility and prolonged supersaturation inbiorelevant media

Place, publisher, year, edition, pages
2014.
National Category
Other Health Sciences
Research subject
Health Science
Identifiers
URN: urn:nbn:se:ltu:diva-28058Local ID: 1b64f18a-f4dd-4068-8c13-ae4b154ec0bfOAI: oai:DiVA.org:ltu-28058DiVA, id: diva2:1001251
Conference
AAPS Annual Meeting and Exposition : 02/11/2014 - 06/11/2014
Note

Godkänd; 2014; 20141209 (amayou)

Available from: 2016-09-30 Created: 2016-09-30 Last updated: 2018-04-16Bibliographically approved

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Al-Hayali, Amani Ibraheem YounisVelaga, Sitaram

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