TY - JOUR
T1 - Development and Stability Study of an Omeprazole Suppository for Infants
AU - Bestebreurtje, Petra
AU - Roeleveld, Nel
AU - Knibbe, Catherijne A. J.
AU - van Sorge, Adriaan A.
AU - Plötz, Frans B.
AU - de Wildt, Saskia N.
PY - 2020/10/1
Y1 - 2020/10/1
N2 - Background and Objective: Omeprazole is a proton pump inhibitor (PPI) that is used in acid suppression therapy in infants. In this study we aimed to develop a pediatric omeprazole suppository, with good physical and chemical stability, suitable for pharmaceutical batch production. Methods: The composition of the suppository consisted of omeprazole, witepsol H15 and arginine (L) base. To achieve evenly distributed omeprazole suspension suppositories, the temperature, stirring rate, and arginine (L) base amount were varied. A previously validated quantitative high-performance liquid chromatography–ultraviolet method was modified and a long-term stability study was performed for one year. Results: Evenly distributed omeprazole suspension suppositories were obtained by adding 100 mg arginine (L) base and pouring at a temperature of 34.7 °C and a stirring speed of 200 rpm. The long-term stability study showed no signs of discoloration and a stable omeprazole content between 90 and 110% over 1 year if stored in the dark at room temperature. Conclusion: We developed a pediatric omeprazole suppository. This formulation may provide a good alternative to manipulated commercial or extemporaneously compounded omeprazole oral formulations for infants. Clinical studies are needed to establish efficacy and safety in this young population.
AB - Background and Objective: Omeprazole is a proton pump inhibitor (PPI) that is used in acid suppression therapy in infants. In this study we aimed to develop a pediatric omeprazole suppository, with good physical and chemical stability, suitable for pharmaceutical batch production. Methods: The composition of the suppository consisted of omeprazole, witepsol H15 and arginine (L) base. To achieve evenly distributed omeprazole suspension suppositories, the temperature, stirring rate, and arginine (L) base amount were varied. A previously validated quantitative high-performance liquid chromatography–ultraviolet method was modified and a long-term stability study was performed for one year. Results: Evenly distributed omeprazole suspension suppositories were obtained by adding 100 mg arginine (L) base and pouring at a temperature of 34.7 °C and a stirring speed of 200 rpm. The long-term stability study showed no signs of discoloration and a stable omeprazole content between 90 and 110% over 1 year if stored in the dark at room temperature. Conclusion: We developed a pediatric omeprazole suppository. This formulation may provide a good alternative to manipulated commercial or extemporaneously compounded omeprazole oral formulations for infants. Clinical studies are needed to establish efficacy and safety in this young population.
UR - http://www.scopus.com/inward/record.url?scp=85087314304&partnerID=8YFLogxK
U2 - https://doi.org/10.1007/s13318-020-00629-1
DO - https://doi.org/10.1007/s13318-020-00629-1
M3 - Article
C2 - 32594306
SN - 0378-7966
VL - 45
SP - 627
EP - 633
JO - European Journal of Drug Metabolism and Pharmacokinetics
JF - European Journal of Drug Metabolism and Pharmacokinetics
IS - 5
ER -