Optimization of the manufacturing process of a pediatric omeprazole enteric pellets suspension: Full Factorial Design.

Abstract

Objective: The purpose of the present study was to apply the design of experiments (DoE) to develop an omeprazole enteric pellets suspension for use in the pediatric population.

Methodology: This experimental study employed a Full Factorial Design for drug development, encompassing three factors (Aerosil^® R972, cetostearyl alcohol, and Span 80) at two levels (2% and 6% for factor A (Aerosil^® R972) and 2% and 4% for factors B and C (cetostearyl alcohol and Span 80, respectively)).

Results: Following the statistical optimization, the suspension F10 was formulated and subjected to a stability study for one month. The dissolution test results were suboptimal, achieving only an 22% release. Subsequently, eight additional suspensions were devised using hydrophilic oily vehicles (Labraphac Hydrophile WL 1219, Labrafil M2125 CS, and Labrafil M 1944 CS) and excipients (Gelucire 44/14 and Aerosil^® 200) to enhance the dissolution profile. Suspension F17 showed over 75% within 30 min, displaying superior sedimentation time when compared to all other formulations, along with effortless resuspension.

Conclusion: The findings suggest that the optimal vehicle for the administration of omeprazole enteric pellets in suspension is the formulation comprising Labrafil M 1944 CS, Span 80, and Aerosil^® 200. This study has paved the way for an oily suspension vehicle, opening new avenues of research for developing pediatric omeprazole formulations that fulfill gastro-resistance requirements.