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The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets

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Abstract
It was the aim of this study to elucidate the impact of the injection mold temperature upon the polymer crystallinity, its microstructure and the resulting drug release from immediate and sustained release tablets containing semi-crystalline polymers. The immediate release formulation contained 20% (w/w) ketoprofen (KETO) in poly (ethylene oxide) (PEO) and the sustained release formulation contained 20-40% (w/w) metoprolol tartrate (MPT) in polycaprolactone (PCL). Physical mixtures of drug-polymer were characterized via isothermal crystallization experiments using DSC and rheological measurements to elucidate the impact of the drug solid-state upon the crystallization kinetics. Tablets were prepared using various thermal histories (extrusion barrel temperature and injection mold temperatures). Polymer crystallinity and microstructure in the tablets was characterized via DSC and polarized optical microscopy. The polymer microstructure was altered by the various applied thermal histories. The differences in PEO crystallinity induced by the various mold temperatures did not affect the KETO dissolution from the tablets. On the other hand, MPT (20-40% w/w) dissolution from the PCL matrix when extruded at 80 degrees C and injection molded at 25 and 35 degrees C was significantly different due to the changes in the polymer microstructure. More perfect polymer crystals are obtained with higher mold temperatures, decreasing the drug diffusion rate through the PCL matrix. The results presented in this study imply that the injection mold temperature should be carefully controlled for sustained release formulations containing hydrophobic semi-crystalline polymers.
Keywords
Solid dispersion, Injection molding, Semi-crystalline polymers, Rheology, Crystallization, HOT-MELT EXTRUSION, POLY(ETHYLENE OXIDE), POLYETHYLENE OXIDE, MOLECULAR-WEIGHT, DELIVERY, FILMS, CRYSTALLINITY, DEGRADATION, BEHAVIOR, BLENDS

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Chicago
Van Renterghem, Jeroen, Heleen Dhondt, Glenn Verstraete, Michiel De Bruyne, Chris Vervaet, and Thomas De Beer. 2018. “The Impact of the Injection Mold Temperature Upon Polymer Crystallization and Resulting Drug Release from Immediate and Sustained Release Tablets.” International Journal of Pharmaceutics 541 (1-2): 108–116.
APA
Van Renterghem, J., Dhondt, H., Verstraete, G., De Bruyne, M., Vervaet, C., & De Beer, T. (2018). The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 541(1-2), 108–116.
Vancouver
1.
Van Renterghem J, Dhondt H, Verstraete G, De Bruyne M, Vervaet C, De Beer T. The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets. INTERNATIONAL JOURNAL OF PHARMACEUTICS. 2018;541(1-2):108–16.
MLA
Van Renterghem, Jeroen et al. “The Impact of the Injection Mold Temperature Upon Polymer Crystallization and Resulting Drug Release from Immediate and Sustained Release Tablets.” INTERNATIONAL JOURNAL OF PHARMACEUTICS 541.1-2 (2018): 108–116. Print.
@article{8572085,
  abstract     = {It was the aim of this study to elucidate the impact of the injection mold temperature upon the polymer crystallinity, its microstructure and the resulting drug release from immediate and sustained release tablets containing semi-crystalline polymers. The immediate release formulation contained 20% (w/w) ketoprofen (KETO) in poly (ethylene oxide) (PEO) and the sustained release formulation contained 20-40% (w/w) metoprolol tartrate (MPT) in polycaprolactone (PCL). Physical mixtures of drug-polymer were characterized via isothermal crystallization experiments using DSC and rheological measurements to elucidate the impact of the drug solid-state upon the crystallization kinetics. Tablets were prepared using various thermal histories (extrusion barrel temperature and injection mold temperatures). Polymer crystallinity and microstructure in the tablets was characterized via DSC and polarized optical microscopy. The polymer microstructure was altered by the various applied thermal histories. The differences in PEO crystallinity induced by the various mold temperatures did not affect the KETO dissolution from the tablets. On the other hand, MPT (20-40% w/w) dissolution from the PCL matrix when extruded at 80 degrees C and injection molded at 25 and 35 degrees C was significantly different due to the changes in the polymer microstructure. More perfect polymer crystals are obtained with higher mold temperatures, decreasing the drug diffusion rate through the PCL matrix. The results presented in this study imply that the injection mold temperature should be carefully controlled for sustained release formulations containing hydrophobic semi-crystalline polymers.},
  author       = {Van Renterghem, Jeroen and Dhondt, Heleen and Verstraete, Glenn and De Bruyne, Michiel and Vervaet, Chris and De Beer, Thomas},
  issn         = {0378-5173},
  journal      = {INTERNATIONAL JOURNAL OF PHARMACEUTICS},
  keywords     = {Solid dispersion,Injection molding,Semi-crystalline polymers,Rheology,Crystallization,HOT-MELT EXTRUSION,POLY(ETHYLENE OXIDE),POLYETHYLENE OXIDE,MOLECULAR-WEIGHT,DELIVERY,FILMS,CRYSTALLINITY,DEGRADATION,BEHAVIOR,BLENDS},
  language     = {eng},
  number       = {1-2},
  pages        = {108--116},
  title        = {The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2018.01.053},
  volume       = {541},
  year         = {2018},
}

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