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Chitinosans as tableting excipients for modified release delivery systems
P R Rege1, D J Shukla, L H Block
1Department of Medicinal Chemistry and Pharmaceutics, 437 Mellon Hall of Science, School of Pharmacy, Duquesne University, Pittsburgh, PA 15282, USA.
International Journal of Pharmaceutics
|June 17, 1999
Summary
Chitinosans, derived from chitin and chitosan, can modify drug release in delivery systems. These compounds significantly impacted drug release and tablet strength, showing promise as pharmaceutical excipients.
Area of Science:
- Polymer Science
- Materials Science
- Pharmaceutical Science
Background:
- Chitinosans, acetylated poly(N-glucosamines), possess protonated amines at acidic pH, enabling interactions with charged drug ions.
- These interactions can be leveraged to control drug release kinetics in various drug delivery systems.
- Commercial chitinosan compounds with varying deacetylation degrees and molecular weights are available for pharmaceutical applications.
Purpose of the Study:
- To investigate the influence of chitinosans on the properties and drug release profiles of modified-release tablets.
- To evaluate the impact of compression pressure and tablet press type on tablet characteristics.
- To assess the suitability of commercial chitinosan compounds as excipients in drug delivery.
Main Methods:
- Tablets were prepared by physically mixing salicylic acid (model drug) with five commercial chitinosan compounds and magnesium stearate.
- Tablets were compressed using a Carver and a single punch tablet press at varying pressures (5000, 10000, 15000 psig).
- Differential scanning calorimetry (DSC) was used to analyze drug-excipient interactions, while ANOVA assessed the effects of compression pressure, press type, and chitinosan type on crushing strength and drug release.
Main Results:
- Differential scanning calorimetry confirmed interactions between chitinosans and salicylic acid in the powder blend.
- Compression pressure and tablet press type did not significantly affect tablet crushing strength or drug release profiles (P > 0.05).
- Chitinosan type significantly influenced both tablet crushing strength and the release profile of salicylic acid (P < 0.05).
Conclusions:
- Chitinosans significantly affect the mechanical properties and drug release characteristics of matrix tablets.
- Commercial chitinosan compounds demonstrate potential as effective excipients for developing modified-release drug delivery systems.
- Compression parameters and manufacturing equipment had minimal impact on the evaluated tablet properties, highlighting the critical role of the chitinosan material itself.