Controlled Release of a Poorly Water-Soluble Drug from Hot-Melt Extrudates Containing Acrylic Polymers.

Autor: Zhu, Yucun, Shah, Navnit H., Waseem Malick, A., Infeld, Martin H., McGinity, James W.
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Zdroj: Drug Development & Industrial Pharmacy; Jun2006, Vol. 32 Issue 5, p569-583, 15p, 1 Black and White Photograph, 5 Charts, 12 Graphs
Abstrakt: Controlled release tablets containing a poorly water-soluble drug, indomethacin (IDM), acrylic polymers (Eudragit ® RD 100, Eudragit ® L 100, or Eudragit ® S 100), and triethyl citrate (TEC) were prepared by hot-melt extrusion. The physicochemical and IDM release properties of the controlled release hot-melt extrudates were investigated. Indomethacin (IDM) was found to be both thermally and chemically stable following hot-melt extrusion processing and displayed a plasticizing effect on Eudragit ® RL PO as demonstrated by a decrease in the glass transition temperatures of the polymer. The inclusion of either Pluronic ® F68, Eudragit ® L 100, or Eudragit ® S 100 in the powder blend containing Eudragit ® RD 100 prior to processing increased the rate of release of the IDM from the extrudates. An increase in the media pH and a decrease in the granule particle size also increased the rate of release of IDM. The inclusion of TEC up to 8% in the granule formulation or compressing the granules into tablets had no significant effect on the drug release rate. Indomethacin (IDM) was transformed from a crystalline Form I into an amorphous form in the Eudragit ® RD 100 granules following hot-melt extrusion. The thermal processing facilitated the formation of a solid solution with a continuous matrix structure that was shown to control drug diffusion from the extrudates. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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