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New multifunctional pharmaceutical excipient in tablet formulation based on citric acid-cyclodextrin polymer
Maria José Garcia-Fernandez1, Nicolas Tabary2, Feng Chai3
1Université Lille 1, Unité Matériaux et Transformations (UMET) UMR CNRS 8207, Villeneuve d'Ascq, France; Univ. Lille, Inserm, CHU Lille, U1008 - Controlled Drug Delivery Systems and Biomaterials, F-59000 Lille, France.
International Journal of Pharmaceutics
|July 31, 2016
Summary
A novel beta-cyclodextrin (β-CD) polymer, in water-insoluble (PCD-I) and soluble (PCD-S) forms, functions as a versatile direct compression excipient for tablet formulation, demonstrating improved tablet properties and safety.
Area of Science:
- Pharmaceutical Technology
- Polymer Science
- Materials Science
Background:
- Direct compression (DC) is a preferred method for tablet manufacturing due to its efficiency.
- Excipients play a crucial role in DC, influencing tablet properties and performance.
- Beta-cyclodextrin (β-CD) derivatives are explored for their potential as multifunctional excipients.
Purpose of the Study:
- To develop and characterize a novel β-cyclodextrin polymer (PCD) as a multifunctional direct compression excipient.
- To evaluate the performance of PCD in its water-insoluble (PCD-I) and water-soluble (PCD-S) forms for tablet formulation.
- To assess the safety profile of PCD in a preclinical toxicity study.
Main Methods:
- β-cyclodextrin was crosslinked with citric acid to form PCD, processed into insoluble (PCD-I) and soluble (PCD-S) forms.
- PCD powders were characterized for physical properties including water vapor sorption, SEM, particle size, density, compressibility, and flowability.
- Tablets were prepared by direct compression using PCD-I, PCD-S, or their mixtures without additional excipients.
- Tablet properties (crushing strength, disintegration time) and animal toxicity were evaluated.
Main Results:
- PCD-I, spray-dried PCD-S, and a 90/10 PCD-I/PCD-S mixture exhibited optimal flow characteristics.
- Tablets formulated with PCD-I showed increased crushing resistance and disintegration times, with PCD-I acting as an effective disintegrant.
- PCD-I demonstrated rapid swelling upon contact with water, enhancing tablet disintegration.
- No clinical signs of toxicity were observed in Sprague-Dawley rats after 14 days of force-feeding PCD.
Conclusions:
- The developed β-cyclodextrin polymer (PCD) is a promising multifunctional excipient for direct compression tablet formulation.
- PCD, particularly PCD-I, offers improved tablet disintegration and mechanical properties.
- PCD exhibits a favorable safety profile, making it suitable for pharmaceutical applications.
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