Influence of Formulation Factors on Tablet Formulations with Liquid Permeation Enhancer Using Factorial Design

For a drug with low bioavailability, a matrix tablet with liquid permeation enhancer (Labrasol®) was formulated. Factorial design was used to evaluate the effect of three formulation factors: drug percentage, polymer type (Methocel® K100M or Eudragit® L 100-55), and tablet binder percentage (Plasdon...

Full description

Saved in:
Bibliographic Details
Published in:AAPS PharmSciTech 2009-12, Vol.10 (4), p.1437-1443, Article 1437
Main Authors: Bejugam, Naveen K., Parish, Helen J., Shankar, Gita N.
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Chemistry, Pharmaceutical
Glycerides
Hardness Tests
Methylcellulose - chemistry
Organic Chemicals - chemistry
Permeability
Pharmacology/Toxicology
Pharmacy
Research Article
Solubility
Tablets
Tensile Strength
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:For a drug with low bioavailability, a matrix tablet with liquid permeation enhancer (Labrasol®) was formulated. Factorial design was used to evaluate the effect of three formulation factors: drug percentage, polymer type (Methocel® K100M or Eudragit® L 100-55), and tablet binder percentage (Plasdone® S-630) on tablet characteristics. Tablets were prepared by direct compression and characterized. Compressibility index values ranged between 15.90% and 29.87% and tablet hardness values from 7.8 to 29.78 Kp. Eudragit®-containing formulations had better compressibility index values with higher tablet hardness. Time for 75% of drug release ( T 75 ) was calculated, and formulations containing Eudragit® L 100-55 had faster release rates than tablet formulations with Methocel® K100M. Formulations with Methocel® K100M fit well in the Higuchi model as indicated by their R 2 values (>0.98). Among all the formulation factors studied, polymer type displayed the highest and statistically significant effect on compressibility index, tablet hardness, and dissolution rate. Statistical design helped in better understanding the effect of formulation factors on tablet characteristics important for designing formulations with desired characteristics.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-009-9345-8