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dc.creatorĐuriš, Jelena
dc.creatorNikolakakis, Ioannis
dc.creatorIbrić, Svetlana
dc.creatorĐurić, Zorica
dc.creatorKachrimanis, Kyriakos
dc.date.accessioned2019-09-02T11:36:28Z
dc.date.available2019-09-02T11:36:28Z
dc.date.issued2013
dc.identifier.issn0939-6411
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/1997
dc.description.abstractHot-melt extrusion (HME) is a dust- and solvent-free continuous process enabling the preparation of a variety of solid dosage forms containing solid dispersions of poorly soluble drugs into thermoplastic-polymers. Miscibility of drug and polymer is a prerequisite for stable solid dispersion formation. The present study investigates the feasibility of forming solid dispersions of carbamazepine (CBZ) into polyethyleneglycol-polyvinyl caprolactam-polyvinyl acetate grafted copolymer (Soluplus (R)) by hot-melt extrusion. Physicochemical properties of the raw materials, extrudates, co-melted products, and corresponding physical mixtures were characterized by thermo-gravimetric analysis (TGA), differential. scanning calorimetry (DSC), attenuated total reflectance infrared (ATR-FTIR) spectroscopy and hot stage microscopy (HSM), while miscibility of CBZ and Soluplus (R) was estimated on the basis of the Flory-Huggins theory, Hansen solubility parameters, and solid-liquid equilibrium equation. It was found that hot-melt extrusion of carbamazepine and Soluplus (R) is feasible on a single-screw hot-melt extruder without the addition of plasticizers. DSC analysis and FTIR spectroscopy revealed that a molecular dispersion is formed when the content of CBZ does not exceed similar to 5% w/w while higher CBZ content results in a microcrystalline dispersion of CBZ form III crystals, with the molecularly dispersed percentage increasing with extrusion temperature, at the risk of inducing transformation to the undesirable form I of CBZ. Thermodynamic modeling elucidated potential limitations and temperature dependence of solubility/dispersibility of carbamazepine in Soluplus (R) hot-melt extrudates. The results obtained by thermodynamic models are in agreement with the findings of the HME processing, encouraging therefore their further application in the HME process development.en
dc.publisherElsevier Science BV, Amsterdam
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/34007/RS//
dc.rightsrestrictedAccess
dc.sourceEuropean Journal of Pharmaceutics and Biopharmaceutics
dc.subjectHot-melt extrusionen
dc.subjectCarbamazepineen
dc.subjectSoluplusen
dc.subjectFlory-Hugginsen
dc.subjectHansen solubility parameteren
dc.subjectSolid dispersionen
dc.titlePreparation of carbamazepine-Soluplus (R) solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fittingen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractКацхриманис, Кyриакос; Ђурић, Зорица; Ђуриш, Јелена; Николакакис, Иоаннис; Ибрић, Светлана;
dc.citation.volume84
dc.citation.issue1
dc.citation.spage228
dc.citation.epage237
dc.citation.other84(1): 228-237
dc.citation.rankM21
dc.identifier.wos000319234600024
dc.identifier.doi10.1016/j.ejpb.2012.12.018
dc.identifier.pmid23333900
dc.identifier.scopus2-s2.0-84876933684
dc.identifier.rcubconv_2853
dc.type.versionpublishedVersion


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