Development and characterization of extended release Kollidon (R) SR mini-matrices prepared by hot-melt extrusion


ÖZGÜNEY I. , SHUWISITKUL D., BODMEIER R.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, cilt.73, ss.140-145, 2009 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 73 Konu: 1
  • Basım Tarihi: 2009
  • Doi Numarası: 10.1016/j.ejpb.2009.04.006
  • Dergi Adı: EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
  • Sayfa Sayıları: ss.140-145

Özet

Kollidon (R) SR as a drug carrier and two model drugs with two different melting points, ibuprofen and theophylline, were studied by hot-melt extrusion. Powder mixtures containing Kollidon (R) SR were extruded using a twin-screw extruder at temperatures 70 and 80 degrees C for ibuprofen and 80 and 90 degrees C for theophylline. The glass transition temperature (T(g)) and maximum torque were inversely related to ibuprofen concentrations, indicating its plasticizing effect. The results of differential scanning calorimetry (DSC) and Xray diffraction analysis showed that ibuprofen remained in an amorphous or dissolved state in the extrudates containing drug up to 35%, whereas theophylline was dispersed in the polymer matrix. The increase in amounts of ibuprofen or theophylline in the hot-melt extrudates resulted in the increase in the drug release rates. Theophylline release rate in hot-melt extruded matrices decreased as the extrusion temperature increased. In contrast, a higher processing temperature caused the higher ibuprofen release. This was a clear indication of the plasticizing effect of ibuprofen on Kollidon (R) SR and a result from water uptake. Theophylline release rate from hot-melt extrudates decreased with increasing triethyl citrate (TEC) level because of the formation of a denser matrix. By adding of Klucel (R) LF as a water-soluble additive to the hot-melt extruded matrices, an increase in ibuprofen and theophylline release rates was obtained. (c) 2009 Elsevier B.V. All rights reserved.