TY - JOUR
T1 - Noveon AA1 as enhancer of HPMC as a direct compression matrix for controlled release
AU - Laguna-López, Sara
AU - Villafuerte-Robles, Leopoldo
N1 - Publisher Copyright:
© 2014 Sara Laguna-López and Leopoldo Villafuerte-Robles.
PY - 2014
Y1 - 2014
N2 - This work aimed the assessment of the effect of different proportions of Noveon AA1 on performance of HPMC as a controlled release agent for direct compression tablets. The functionality of polymer blends was determined using dissolution profiles, compactibility profiles and the powders compressibility index. Ten percent HPMC allows a metronidazole release after 3 h of 85%, an exponent n=0.48 and a release constant K=6.9. The increasing polymer substitution by Noveon AA1 decreases drug dissolution up to 36%, increases the exponent to 1.0 and decreases the release constant to 0.2%. The metronidazole/HPMC blend shows a slower increasing and a lower potential of tablets compactibility (20 N) while its increasing substitution by Noveon AA1 attains faster increasing and higher potential compactibilities (39 N). The metronidazole/HPMC (90:10) blend shows a low compressibility index (14%) that increases up to 33.2% with increasing Noveon AA1 proportions. Noveon AA1 proportions ≥ 5% display good/passable powder flowabilities. Noveon AA1 enhances the overall controlled release performance of HPMC, inducing zero order release patterns without lag or burst effects and reducing drug release more efficiently. Noveon AA1 also improves the compactibility of metronidazole/HPMC blends, however, decreases their flowability; flowability is acceptable only at lesser polymer proportions.
AB - This work aimed the assessment of the effect of different proportions of Noveon AA1 on performance of HPMC as a controlled release agent for direct compression tablets. The functionality of polymer blends was determined using dissolution profiles, compactibility profiles and the powders compressibility index. Ten percent HPMC allows a metronidazole release after 3 h of 85%, an exponent n=0.48 and a release constant K=6.9. The increasing polymer substitution by Noveon AA1 decreases drug dissolution up to 36%, increases the exponent to 1.0 and decreases the release constant to 0.2%. The metronidazole/HPMC blend shows a slower increasing and a lower potential of tablets compactibility (20 N) while its increasing substitution by Noveon AA1 attains faster increasing and higher potential compactibilities (39 N). The metronidazole/HPMC (90:10) blend shows a low compressibility index (14%) that increases up to 33.2% with increasing Noveon AA1 proportions. Noveon AA1 proportions ≥ 5% display good/passable powder flowabilities. Noveon AA1 enhances the overall controlled release performance of HPMC, inducing zero order release patterns without lag or burst effects and reducing drug release more efficiently. Noveon AA1 also improves the compactibility of metronidazole/HPMC blends, however, decreases their flowability; flowability is acceptable only at lesser polymer proportions.
KW - Compactibility
KW - Compressibility index
KW - Dissolution mechanisms
KW - Dissolution profile
KW - Metronidazole
KW - Powder flowability
KW - Tablet hardness
UR - http://www.scopus.com/inward/record.url?scp=84927078893&partnerID=8YFLogxK
U2 - 10.7324/JAPS.2014.41111
DO - 10.7324/JAPS.2014.41111
M3 - Artículo
SN - 2231-3354
VL - 4
SP - 62
EP - 68
JO - Journal of Applied Pharmaceutical Science
JF - Journal of Applied Pharmaceutical Science
IS - 11
ER -