“Soft Tableting”: A New Concept to Tablet Pressure Sensitive Materials
- 1 January 2004
- journal article
- Published by Taylor & Francis Ltd in Pharmaceutical Development and Technology
- Vol. 9 (1), 107-121
- https://doi.org/10.1081/pdt-120027426
Abstract
The aim of this study was to confirm the hypothesis that tableting using excipients with greater elastic deformation results in improved performance of pressure-sensitive drugs relative to the excipients with low elastic deformation. Tableting with highly elastic deforming excipients and the resultant minimization of the process damage is referred to in this article as "soft tableting." Carrageenans, chitosans, and polyethylene oxides were tested as potentially useful tableting excipients. alpha-Amylase, amorphous indomethacin, theophylline monohydrate, and enteric-coated pellets were used as models for pressure-sensitive materials. Three-dimensional modeling of the tableting data and elastic recovery of the tablets were the tools for mechanical characterization. The crushing force of the tablets was analyzed. Inactivation of alpha-amylase was determined by using the starch iodine reaction method. Pseudopolymorphic and polymorphic changes were analyzed using Fourier transform (FT) Raman spectroscopy. The effects of pressure on the integrity of the pellets were tested by release studies and scanning electron microscopy. The process of tablet formation was characterized for potentially useful tableting excipients. The results were compared with the results of traditional excipients as microcrystalline cellulose (MCC), dicalcium phosphate dihydrate, and hydroxypropyl methylcellulose (HPMC). A ranking order for soft tableting was deduced from the mechanical properties. The tableting excipients were ranked according to their general plasticity (GP): GP(carrageenans)<GP(chitosans)<GP(MCC)<GP(HPMC)<GP(polyethylene oxides). This theoretical order of suitability has been experimentally proven to be valid for the pressure-sensitive materials. In conclusion, the new concept for soft tableting is valid.Keywords
This publication has 22 references indexed in Scilit:
- Time Dependence of Elastic Recovery for Characterization of Tableting MaterialsPharmaceutical Development and Technology, 2001
- An Evaluation of Three-Dimensional Modeling of Compaction Cycles by Analyzing the Densification Behavior of Binary and Ternary MixturesPharmaceutical Development and Technology, 2001
- Matrix Tablets of Carrageenans. I. A Compaction Study*Drug Development and Industrial Pharmacy, 1999
- Principles, tenets and notions of tablet bonding and measurements of strengthEuropean Journal of Pharmaceutics and Biopharmaceutics, 1997
- Tableting of coated pelletsEuropean Journal of Pharmaceutics and Biopharmaceutics, 1997
- Research in Solid Dosage Forms-An Obsolete Topic?Pharmaceutical Development and Technology, 1997
- Effects of grinding and compression on crystal structure of anhydrous caffeineInternational Journal of Pharmaceutics, 1993
- Effect of tabletting on the degree of crystallinity and on the dehydration and decomposition points of cephalexin crystalline powder.CHEMICAL & PHARMACEUTICAL BULLETIN, 1985
- Polymorphic Transformation of Some Drugs Under CompressionDrug Development and Industrial Pharmacy, 1985
- The influence of the moisture content of the fibrous support of a nasal inhaler upon the concentration of drug in the air streamJournal of Pharmacy and Pharmacology, 1972