Solid state properties and drug release behavior of co-amorphous indomethacin-arginine tablets coated with Kollicoat® Protect

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Autor/in:
Erscheinungsjahr:
2017
Medientyp:
Text
Schlagworte:
  • Pharmaceutical Preparations
  • Solubility
  • Melt extrusion
  • Nanoparticles
  • Tablets
  • Pharmaceutical Preparations
  • Solubility
  • Melt extrusion
  • Nanoparticles
  • Tablets
Beschreibung:
  • A promising approach to improve the solubility of poorly water-soluble drugs and to overcome the stability issues related to the plain amorphous form of the drugs, is the formulation of drugs as co-amorphous systems. Although polymer coatings have been proven very useful with regard to tablet stability and modifying drug release, there is little known on coating co-amorphous formulations. Hence, the aim of the present study was to investigate whether polymer coating of co-amorphous formulations is possible without inducing recrystallization. Tablets containing either a physical mixture of crystalline indomethacin and arginine or co-amorphous indomethacin-arginine were coated with a water soluble polyvinyl alcohol -polyethylene glycol graft copolymer (Kollicoat Protect) and stored at 23 degrees C/0\% RH and 23 degrees C175\% RH. The solid state properties of the coated tablets were analyzed by XRPD and FTIR and the drug release behavior was tested for up to 4 h in phosphate buffer pH 4.5. The results showed that the co-amorphous formulation did not recrystallize during the coating process or during storage at both storage conditions for up to three months, which confirmed the high physical stability of this co-amorphous system. Furthermore, the applied coating could partially inhibit recrystallization of indomethacin during drug release testing, as coated tablets reached a higher level of supersaturation compared to the respective uncoated formulations and showed a lower decrease of the dissolved indomethacin concentration upon precipitation. Thus, the applied coating enhanced the AUC of the dissolution curve of the co-amorphous tablets by about 30\%. In conclusion, coatings might improve the bioavailability of co-amorphous formulations. (C) 2017 Elsevier B.V. All rights reserved.
Lizenz:
  • info:eu-repo/semantics/restrictedAccess
Quellsystem:
Forschungsinformationssystem der UHH

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oai:www.edit.fis.uni-hamburg.de:publications/b35b8a3b-e96f-4c5e-90d2-47e6b934fd75