Sucrose Octaacetate Chemical Kinetics and Shelf Lives at Various Formulation pHs

Abstract

Developing pediatric friendly dosage forms is a high priority worldwide. Sucrose octaacetate (SOA) has been recommended for use as a surrogate for bitter tasting active pharmaceutical ingredients. Even though SOA has found a number of human use applications and has been employed for decades, there are no rigorous chemical kinetic studies reported. A recently reported SOA stability-indicating method was used to perform SOA chemical kinetic and stability studies. As part of the chemical kinetic study, reaction order, activation energies, extrapolated rate constants, pH–rate profiles at 4 and 25°C, and estimated shelf lives at 4 and 25°C at different buffer pHs are provided. The estimated SOA shelf lives at 25°C and pHs 4.00, 5.20, and 6.00 were 25.3, 114, and 27.4 days, respectively. At 4°C, SOA’s estimated shelf lives were 0.478, 5.26, and 1.47 years at pHs 4.00, 5.20, and 6.00, respectively. SOA can be formulated at pHs 4 to 6 and stored at 25°C for short-duration (less than 25 days) uses such as a bitter tasting surrogate for fundamental taste mechanism studies or brief taste masking assessment clinical studies. For longer term solution studies, like being used as a bitter tasting control for blinded clinical trials, SOA should be formulated at the optimum pH of 5.40 and refrigerated at 4°C for maximum stability. The reported data can be used as a starting point for developing stable SOA formulations and estimating shelf life.