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Title: | Solid State Solubility of Miconazole in Poly[(ethylene glycol)-g-vinyl alcohol] Using Hot-Melt Extrusion | Authors: | Litvinov, V. M. Guns, S. ADRIAENSENS, Peter Scholtens, B. J. R. Quaedflieg, M. P. CARLEER, Robert Van den Mooter, G. |
Issue Date: | 2012 | Publisher: | AMER CHEMICAL SOC | Source: | MOLECULAR PHARMACEUTICS, 9 (10), p. 2924-2932 | Abstract: | The use of hot-melt extrusion for preparing homogeneous API-excipient mixtures is studied for miconazole-PEG-g-PVA [poly(ethylene glycol) - poly(vinyl alcohol) graft copolymer] solid dispersions with a 5 cm(3) table-top, twin-screw corotating microcompounder (DSM Xplore). Phase behavior of PEG-g-PVA, miscibility of miconazole in PEG-g-PVA and the partitioning of miconazole between PEG and PVA amorphous phases are characterized using a combination of modulated DSC, XRPD, and solid-state H-1 and C-13 NMR methods. The H-1 NMR transverse magnetization relaxation (T-2 relaxation) method is used to analyze the phase composition and molecular mobility of the copolymer. The T-2 relaxation decay of pure PEG-g-PVA can be described by four T-2 relaxation components in the temperature range studied. PVA crystallinity is not largely affected by hot-melt extrusion and the presence of the drug. Miconazole preferably resides in the PEG amorphous phase, and its molecules are well dispersed in the PEG-g-PVA matrix using hot-melt extrusion mixing. Miconazole forms amorphous nanoclusters whose average size equals approximately 1.6 nm, indicating solid solution formation (molecular level dispersion) of the drug in the polymer. | Notes: | [Guns, S.; Van den Mooter, G.] Katholieke Univ Leuven, Lab Pharmacotechnol & Biopharm, B-3000 Louvain, Belgium. [Litvinov, V. M.] DSM Resolve, NL-6160 MD Geleen, Netherlands. [Adriaensens, P.; Carleer, R.] Hasselt Univ, IMO, Div Chem, B-3590 Diepenbeek, Belgium. [Scholtens, B. J. R.; Quaedflieg, M. P.] DSM Xplore, NL-6160 MD Geleen, Netherlands. Victor.Litvinov@DSM.com; Guy.VandenMooter@pharm.kuleuven.be | Keywords: | Pharmacology & Pharmacy; solid state NMR; solid dispersion; hot-melt extrusion; Kollicoat IR; miconazole;solid state NMR; solid dispersion; hot-melt extrusion; Kollicoat IR; miconazole | Document URI: | http://hdl.handle.net/1942/14311 | ISSN: | 1543-8384 | e-ISSN: | 1543-8392 | DOI: | 10.1021/mp300280k | ISI #: | 000309314900014 | Category: | A1 | Type: | Journal Contribution | Validations: | ecoom 2013 |
Appears in Collections: | Research publications |
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Solid state Solubility of miconazole.pdf Restricted Access | Published version | 1.63 MB | Adobe PDF | View/Open Request a copy |
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