Structure-Property Relationship of Amorphous Maltitol as Tableting Excipient
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Research Article Structure-Property Relationship of Amorphous Maltitol as Tableting Excipient Franck Bourduche,1,2,3 Noelia M. Sanchez-Ballester,1 Bernard Bataille,1 Philippe Lefèvre,2 and Tahmer Sharkawi1
Received 13 May 2020; accepted 14 September 2020 Abstract. Maltitol shows interesting properties compared with mannitol or sorbitol, two other polyols, which are widely used as a pharmaceutical excipients for tablet compaction. For this study, the properties of an amorphous polyol, maltitol, were investigated using a tablet press simulator. The aim of this study was to evaluate the behavior of amorphous maltitol compared to SweetPearl® P 200, a pure product, and SweetPearl® P 300 DC, a textured crystalline maltitol excipient for direct compression. The physicochemical and pharmacotechnical properties were compared, revealing a major change in properties after amorphization. The study of the tabletability, mean yield pressure, elastic properties, etc. shows that the compression behavior of amorphous powders has been significantly altered. The results showed specific properties of amorphous maltitol with good tabletability at low compaction pressure. The stability of the amorphous and the evolution of its behavior in compression were then studied, showing a direct link between its recrystallization and the change in its properties. The use of a stabilizing agent, maltotriitol, slowed down the recrystallization, maintaining the specific properties of the amorphous material in compression for a longer period of time. KEY WORDS: maltitol; amorphous state; physicochemical characterizations; direct compression; stability study.
INTRODUCTION Polyols are substances increasingly used for different applications as low caloric sweeteners or in pharmaceutical industry as tableting excipients. Maltitol is widely used in food, in particular in low carb food and non-cariogenic products (1,2). In the pharmaceutical field, mannitol and sorbitol are the most frequently used polyols. Compared with these products, maltitol also has interesting properties. With chemical formula C12H24O11 (4-O-α-glucopyranosylD-sorbitol), maltitol is chemically very stable (3); it has good sweetening power, very similar to sucrose (4,5). The laxative effect of polyols may be a concern when incorporated at high dose, but fortunately maltitol is the besttolerated polyol (5). Furthermore, maltitol structural properties have already been studied in the literature (6–9). This excipient possesses only one crystalline form which can present different habits and one amorphous form (8,10,11). Another benefit of maltitol is its suitability for pediatric use (12). With all these properties, maltitol is starting to be
1
ICGM, Univ Montpellier, CNRS, ENSCM, Montpellier, France. Customer Technical Service Pharma, Roquette Frères, Lestrem, France. 3 To whom correspondence should be addressed. (e–mail: FRANCK. [email protected]; [email protected]) 2
extensively used in solid and liquid oral dosage formulations (13,14). Compared to other polyols
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