title: Sustained release of diltiazem HCl tableted after co-spray drying and physical mixing with PVAc and PVP.
abstract: In this work, aqueous diltiazem HCl and polyvinyl-pyrrolidone (PVP) solutions were mixed with Kollicoat SR 30D and spray dried to microparticles of different drug:excipient ratio and PVP content. Co-spray dried products and physical mixtures of drug, Kollidon SR and PVP were tableted. Spray drying process, co-spray dried products and compressibility/compactability of co-spray dried and physical mixtures, as well as drug release and water uptake of matrix-tablets was evaluated. Simple power equation fitted drug release and water uptake (R(2) > 0.909 and 0.938, respectively) and correlations between them were examined. Co-spray dried products with PVP content lower than in physical mixtures result in slower release, while at equal PVP content (19 and 29% w/w of excipient) in similar release (f2 > 50). Increase of PVP content increases release rate and co-spray drying might be an alternative, when physical mixing is inadequate. Co-spray dried products show better compressibility/compatibility but higher stickiness to the die-wall compared to physical mixtures. SEM observations and comparison of release and swelling showed that distribution of tableted component affects only the swelling, while PVP content for both co-spray dried and physical mixes is major reason for release alterations and an aid for drug release control.
authors.affiliation: a Faculty of Pharmaceutical Sciences, Hashemite University , Zarqa , Jordan .
authors.forename: Nizar
authors.initials: N
authors.lastname: Al-Zoubi
authors.affiliation: b Faculty of Pharmacy, Applied Science University , Amman , Jordan .
authors.forename: Ghada
authors.initials: G
authors.lastname: Al-Obaidi
authors.affiliation: c Department of Pharmaceutical Technology , Faculty of Pharmacy, Jordan University of Science and Technology , Irbid , Jordan , and.
authors.forename: Bassam
authors.initials: B
authors.lastname: Tashtoush
authors.affiliation: d Department of Pharmaceutical Technology , School of Pharmacy, Aristotle University of Thessaloniki , Thessaloniki , Greece.
authors.forename: Stavros
authors.initials: S
authors.lastname: Malamataris
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D004110:Diltiazem / Q000008:administration & dosage* / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D011145:Polyvinyls / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D012995:Solubility; D013607:Tablets
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D011145:Polyvinyls; D013607:Tablets; C013215:polyvinyl acetate; D004110:Diltiazem; D011205:Povidone
keywords: Kollicoat SR 30D; Kollidon SR; microparticles; spray drying; tabletability