The role of formulation excipients in the development of lyophilised fast-disintegrating tablets

Rahul Chandrasekhar, Zahra Hassan, Farhan AlHusban, Alan M. Smith, Afzal R. Mohammed

Research output: Contribution to journalArticle

52 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)119-129
Number of pages11
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume72
Issue number1
Early online date3 Dec 2008
DOIs
Publication statusPublished - May 2009
Externally publishedYes

Fingerprint

Excipients
Tablets
Hardness
Gelatin
Viscosity
UCON 50-HB-5100
Mannitol
Mouth
Poloxamer
Sorbitol
Sucrose
Stomach
Polymers

Cite this

Chandrasekhar, Rahul ; Hassan, Zahra ; AlHusban, Farhan ; Smith, Alan M. ; Mohammed, Afzal R. / The role of formulation excipients in the development of lyophilised fast-disintegrating tablets. In: European Journal of Pharmaceutics and Biopharmaceutics. 2009 ; Vol. 72, No. 1. pp. 119-129.
@article{aaf0209cb6f24d9caffb8e4cabf10ec4,
title = "The role of formulation excipients in the development of lyophilised fast-disintegrating tablets",
abstract = "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.",
keywords = "Carbopol 974P, Fast-disintegrating tablets, Gelatin, Lyophilisation, Pluronic F127, Saccharides",
author = "Rahul Chandrasekhar and Zahra Hassan and Farhan AlHusban and Smith, {Alan M.} and Mohammed, {Afzal R.}",
year = "2009",
month = "5",
doi = "10.1016/j.ejpb.2008.11.011",
language = "English",
volume = "72",
pages = "119--129",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",
number = "1",

}

The role of formulation excipients in the development of lyophilised fast-disintegrating tablets. / Chandrasekhar, Rahul; Hassan, Zahra; AlHusban, Farhan; Smith, Alan M.; Mohammed, Afzal R.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 72, No. 1, 05.2009, p. 119-129.

Research output: Contribution to journalArticle

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

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 -