dc.contributor.author | Caron, Vincent | |
dc.contributor.author | Hu, Yun | |
dc.contributor.author | Tajber, Lidia | |
dc.contributor.author | Erxleben, Andrea | |
dc.contributor.author | Corrigan, Owen I. | |
dc.contributor.author | McArdle, Patrick | |
dc.contributor.author | Healy, Anne Marie | |
dc.date.accessioned | 2018-09-20T16:02:47Z | |
dc.date.available | 2018-09-20T16:02:47Z | |
dc.date.issued | 2013-02-07 | |
dc.identifier.citation | Caron, Vincent; Hu, Yun; Tajber, Lidia; Erxleben, Andrea; Corrigan, Owen I. McArdle, Patrick; Healy, Anne Marie (2013). Amorphous solid dispersions of sulfonamide/soluplus® and sulfonamide/pvp prepared by ball milling. AAPS PharmSciTech 14 (1), 464-474 | |
dc.identifier.issn | 1530-9932 | |
dc.identifier.uri | http://hdl.handle.net/10379/10706 | |
dc.description.abstract | The aim of this paper is to investigate the physicochemical properties of binary amorphous dispersions of poorly soluble sulfonamide/polymeric excipient prepared by ball milling. The sulfonamides selected were sulfathiazole (STZ), sulfadimidine (SDM), sulfamerazine (SMZ) and sulfadiazine (SDZ). The excipients were polyvinylpyrrolidone (PVP) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer, commercially known as Soluplus (R). Co-milled systems were characterised by powder X-ray diffraction and differential scanning calorimetry. PVP was shown to form amorphous dispersions over a wider composition range than Soluplus (R) for the four sulfonamides tested. Moreover, amorphous dispersions made with PVP were homogeneous [single glass transition (Tg)], while amorphous dispersions made from Soluplus (R) were heterogeneous (two Tgs). This behaviour is consistent with the fact that all the sulfonamides tested presented a lower solubility in Soluplus (R) than in PVP, as evidenced by Flory-Huggins parameters determined. Amorphous dispersions of SDM with Soluplus (R) could be produced even though SDM does not amorphise alone upon milling and Soluplus (R) presents Tg at a lower temperature than SDM. Amorphous dispersions of SMZ could be prepared with a lower excipient concentration compared to STZ, SDM and SDZ, which may reflect the one-dimensional H-bonding network in SMZ compared to the 2D or 3D H-bonding network found in the other sulfonamides. Stability tests (60% RH/25 degrees C) revealed that dispersions made with Soluplus (R) remained dry and powdery compared to those made with PVP that formed a sticky paste in less than 2 weeks, indicating a possible advantage of using Soluplus (R) in terms of increased physical stability under high humidity storage conditions. | |
dc.publisher | American Association of Pharmaceutical Scientists (AAPS) | |
dc.relation.ispartof | AAPS PharmSciTech | |
dc.rights | Attribution-NonCommercial-NoDerivs 3.0 Ireland | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/3.0/ie/ | |
dc.subject | amorphous dispersions | |
dc.subject | milling | |
dc.subject | polyvinylpyrrolidone | |
dc.subject | soluplus | |
dc.subject | sulphonamide | |
dc.subject | spray-dried composites | |
dc.subject | glass-transition | |
dc.subject | sulfamerazine polymorphs | |
dc.subject | state amorphization | |
dc.subject | molecular mobility | |
dc.subject | powder diffraction | |
dc.subject | crystallization | |
dc.subject | pharmaceuticals | |
dc.subject | indomethacin | |
dc.subject | systems | |
dc.title | Amorphous solid dispersions of sulfonamide/soluplus® and sulfonamide/pvp prepared by ball milling | |
dc.type | Article | |
dc.identifier.doi | 10.1208/s12249-013-9931-7 | |
dc.local.publishedsource | http://europepmc.org/articles/pmc3581644?pdf=render | |
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