Temperature- and moisture-induced crystallization of amorphous lactose in composite particles with sodium alginate prepared by spray-drying

• Published in: Pharmaceutical development and technology Vol. 5; no. 3; p. 355
• Main Authors: Takeuchi, H, Yasuji, T, Yamamoto, H, Kawashima, Y
• Format: Journal Article
• Language: English
• Published: England 2000
• Subjects: Alginates - administration & dosage; Calorimetry, Differential Scanning; Crystallization; Glucuronic Acid; Hexuronic Acids; Lactose - administration & dosage; Lactose - chemistry; Temperature
• ISSN: 1083-7450
• DOI: 10.1081/PDT-100100551

The purpose of this study was to investigate the temperature- and moisture-induced crystallization of amorphous lactose in the composite particles prepared by spray-drying an aqueous solution of crystalline lactose and sodium alginate. The temperature-induced crystallization of amorphous lactose in the composite particles was suppressed by increasing the amount of sodium alginate in the particles. The stabilizing effect of sodium alginate on amorphous lactose in the composite particles was greater than that in physical mixtures having the same formulating ratios. The improved stability of amorphous lactose in the composite particles was attributed to an increase in the glass transition temperature (Tg) of the mixture. Moisture-induced crystallization of amorphous lactose was also retarded by increasing the amount of sodium alginate in composite particles. Although the Tg of the mixture was reduced by increasing the water content of the particles, the values were higher than that of 100% amorphous lactose when particles of the same water content were compared. The change in the Tg of the composite particles with increasing water content was interpreted as involving three components of the Gordon-Taylor equation. In the amorphous lactose-sodium alginate systems, the Tg values of the composite particles containing sodium alginate were higher than the theoretical line predicted by two components of the Gordon-Taylor equation. These results suggested that there was a specific interaction between the sodium alginate and lactose molecules. This specific interaction was suggested by the fact that only very little amorphous lactose was measured in the spray-dried composite particles stored under humid conditions using differential scanning calorimetry. This molecular interaction may also be partly responsible for the suppression of both the temperature- and moisture-induced crystallization of amorphous lactose in the composite particles.