TY - JOUR
T1 - The role of formulation excipients in the development of lyophilised fast-disintegrating tablets
AU - Chandrasekhar, Rahul
AU - Hassan, Zahra
AU - AlHusban, Farhan
AU - Smith, Alan M.
AU - Mohammed, Afzal R.
PY - 2009/5
Y1 - 2009/5
N2 - Despite recent success, many fast-disintegrating tablets (FDTs) still face problems of low mechanical strength, poor mouth-feel and higher disintegration times. This study aimed to optimise FDTs using a progressive three-stage approach. A series of hardness, fracturability and disintegration time tests were performed on the formulations at each stage. During Stage I, tablets were prepared in concentrations between 2% and 5% w/w, and were formulated at each concentration as single and combination bloom strength gelatin (BSG) using 75 and 225 BSGs. Analysis revealed that both hardness and disintegration time increased with an increase in gelatin concentration. A combination (5% gelatin) FDT comprising a 50:50 ratio of 75:225 BSGs (hardness: 13.7 ± 0.9 N and disintegration time: 24.1 ± 0.6 s) was judged the most ideal, and was carried forward to Stage II: the addition of the saccharides sorbitol, mannitol and sucrose in concentrations between 10% and 80% w/w. The best properties were exhibited by mannitol-containing formulations (50%-hardness: 30.9 ± 2.8 N and disintegration time: 13.3 ± 2.1 s), which were carried forward to the next stage: the addition of viscosity-modifying polymers to improve mouth-feel and aid pre-gastric retention. Addition of carbopol 974P-NF resulted in the enhancement of viscosity with a compromise of the hardness of the tablet, whereas Pluronic F127 (6%) showed an increase in disintegration time and viscosity with retention of mechanical properties.
AB - Despite recent success, many fast-disintegrating tablets (FDTs) still face problems of low mechanical strength, poor mouth-feel and higher disintegration times. This study aimed to optimise FDTs using a progressive three-stage approach. A series of hardness, fracturability and disintegration time tests were performed on the formulations at each stage. During Stage I, tablets were prepared in concentrations between 2% and 5% w/w, and were formulated at each concentration as single and combination bloom strength gelatin (BSG) using 75 and 225 BSGs. Analysis revealed that both hardness and disintegration time increased with an increase in gelatin concentration. A combination (5% gelatin) FDT comprising a 50:50 ratio of 75:225 BSGs (hardness: 13.7 ± 0.9 N and disintegration time: 24.1 ± 0.6 s) was judged the most ideal, and was carried forward to Stage II: the addition of the saccharides sorbitol, mannitol and sucrose in concentrations between 10% and 80% w/w. The best properties were exhibited by mannitol-containing formulations (50%-hardness: 30.9 ± 2.8 N and disintegration time: 13.3 ± 2.1 s), which were carried forward to the next stage: the addition of viscosity-modifying polymers to improve mouth-feel and aid pre-gastric retention. Addition of carbopol 974P-NF resulted in the enhancement of viscosity with a compromise of the hardness of the tablet, whereas Pluronic F127 (6%) showed an increase in disintegration time and viscosity with retention of mechanical properties.
KW - Carbopol 974P
KW - Fast-disintegrating tablets
KW - Gelatin
KW - Lyophilisation
KW - Pluronic F127
KW - Saccharides
UR - http://www.scopus.com/inward/record.url?scp=62949148690&partnerID=8YFLogxK
UR - https://www.journals.elsevier.com/european-journal-of-pharmaceutics-and-biopharmaceutics/
U2 - 10.1016/j.ejpb.2008.11.011
DO - 10.1016/j.ejpb.2008.11.011
M3 - Article
C2 - 19073253
AN - SCOPUS:62949148690
VL - 72
SP - 119
EP - 129
JO - European Journal of Pharmaceutics and Biopharmaceutics
JF - European Journal of Pharmaceutics and Biopharmaceutics
SN - 0939-6411
IS - 1
ER -