TY - JOUR
T1 - Floating and sustained-release characteristics of effervescent tablets prepared with a mixed matrix of eudragit L-100-55 and eudragit E PO
AU - Bani-Jaber, Ahmad Khaled
AU - Alkawareek, Mahmoud Yousef
AU - Al-Gousous, Jozef Jawad
AU - Abu Helwa, Ahmad Yousef
PY - 2011/2
Y1 - 2011/2
N2 - The aim of this study was to evaluate the influence of Na-bicarbonate as an effervescent agent on the floating and sustained-release characteristics in 0.1 M HCl of tablets made of Eudragit E PO (EE) and/or Eudragit L-100-55 (EL) as matrix formers at different EE : EL weight ratios: 0 : 100, 25 : 75, 50 : 50, 75 : 25, and 100 : 0. The tablets were made by direct compression utilizing metronidazole as a model drug. Effervescent tablets with 50EE/50EL (w/w) showed the best floating and sustained drug release properties in the dissolution medium. The corresponding noneffervescent tablets were nonfloating and showed significantly faster drug release. Effervescent tablets with single polymers showed an immediate drug release pattern. These results were explained by Fourier-transform infrared spectroscopy and elemental analysis, which showed strong evidence of interpolyelectrolyte complexation between EE and EL when they were exposed to 0.1 M HCl as an effervescent hybrid matrix, but not as a noneffervescent hybrid matrix. The role of Na-bicarbonate in allowing EE-EL complexation during dissolution was explained as due to raising the pH around EL particles for sufficient polymer ionization and ionic-interaction with the ionized EE.
AB - The aim of this study was to evaluate the influence of Na-bicarbonate as an effervescent agent on the floating and sustained-release characteristics in 0.1 M HCl of tablets made of Eudragit E PO (EE) and/or Eudragit L-100-55 (EL) as matrix formers at different EE : EL weight ratios: 0 : 100, 25 : 75, 50 : 50, 75 : 25, and 100 : 0. The tablets were made by direct compression utilizing metronidazole as a model drug. Effervescent tablets with 50EE/50EL (w/w) showed the best floating and sustained drug release properties in the dissolution medium. The corresponding noneffervescent tablets were nonfloating and showed significantly faster drug release. Effervescent tablets with single polymers showed an immediate drug release pattern. These results were explained by Fourier-transform infrared spectroscopy and elemental analysis, which showed strong evidence of interpolyelectrolyte complexation between EE and EL when they were exposed to 0.1 M HCl as an effervescent hybrid matrix, but not as a noneffervescent hybrid matrix. The role of Na-bicarbonate in allowing EE-EL complexation during dissolution was explained as due to raising the pH around EL particles for sufficient polymer ionization and ionic-interaction with the ionized EE.
KW - Eudragit E
KW - Eudragit L
KW - Floating tablet
KW - Gastroretentive system
KW - Sustained release
UR - http://www.scopus.com/inward/record.url?scp=79551469868&partnerID=8YFLogxK
U2 - 10.1248/cpb.59.155
DO - 10.1248/cpb.59.155
M3 - Article
C2 - 21297292
AN - SCOPUS:79551469868
SN - 0009-2363
VL - 59
SP - 155
EP - 160
JO - Chemical and Pharmaceutical Bulletin
JF - Chemical and Pharmaceutical Bulletin
IS - 2
ER -