Investigation of the Drug Release and Surface Morphological Properties of Film-Coated Pellets and Physical Thermal and Mechanical Properties of Free Films as a Function of Various Curing Conditions

摘要

The purpose of the present investigation was to elucidate the influence of curing on different physical properties of Eudragit® NE and RS coating systems. Increased curing times resulted in decreased drug release rates from Eudragit® NE-coated beads. However, an increase in drug release rates was noticed at longer curing times and higher temperatures for the Eudragit® RS coating system. The surface morphological changes of the film-coated beads revealed that there were no visible macroscopic changes as a result of curing. The absence of any ibuprofen melting peak in the DSC thermograms of cured NE and RS coated beads confirmed that there was no surface crystallization of ibuprofen. These results indicated that the increase in drug release rates from RS coated pellets, when subjected to long curing times, resulted from loss of plasticizer. Free films of Eudragit® NE exhibited an increase in tensile strength with increased curing times, whereas Eudragit® RS free films showed a decrease in tensile strength beyond 4 h of curing at 70 and 90 °C. The film thicknesses and weights of free films of Eudragit® RS prepared with triethyl citrate plasticizer were found to change more dramatically with curing than did free films of Eudragit® RS prepared with ibuprofen as the plasticizer. An increase in pore volume was also observed with increased curing times for Eudragit® RS free films. Such changes with curing were shown to be due to the loss of plasticizer molecules, leading to the formation of molecular-scale voids and channels.