dc.creator | Đuriš, Jelena | |
dc.creator | Nikolakakis, Ioannis | |
dc.creator | Ibrić, Svetlana | |
dc.creator | Đurić, Zorica | |
dc.creator | Kachrimanis, Kyriakos | |
dc.date.accessioned | 2019-09-02T11:36:28Z | |
dc.date.available | 2019-09-02T11:36:28Z | |
dc.date.issued | 2013 | |
dc.identifier.issn | 0939-6411 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/1997 | |
dc.description.abstract | Hot-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.publisher | Elsevier Science BV, Amsterdam | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/34007/RS// | |
dc.rights | restrictedAccess | |
dc.source | European Journal of Pharmaceutics and Biopharmaceutics | |
dc.subject | Hot-melt extrusion | en |
dc.subject | Carbamazepine | en |
dc.subject | Soluplus | en |
dc.subject | Flory-Huggins | en |
dc.subject | Hansen solubility parameter | en |
dc.subject | Solid dispersion | en |
dc.title | Preparation of carbamazepine-Soluplus (R) solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Кацхриманис, Кyриакос; Ђурић, Зорица; Ђуриш, Јелена; Николакакис, Иоаннис; Ибрић, Светлана; | |
dc.citation.volume | 84 | |
dc.citation.issue | 1 | |
dc.citation.spage | 228 | |
dc.citation.epage | 237 | |
dc.citation.other | 84(1): 228-237 | |
dc.citation.rank | M21 | |
dc.identifier.wos | 000319234600024 | |
dc.identifier.doi | 10.1016/j.ejpb.2012.12.018 | |
dc.identifier.pmid | 23333900 | |
dc.identifier.scopus | 2-s2.0-84876933684 | |
dc.type.version | publishedVersion | |