PMID- 32594306
OWN - NLM
STAT- MEDLINE
DCOM- 20210702
LR  - 20210702
IS  - 2107-0180 (Electronic)
IS  - 0378-7966 (Print)
IS  - 0378-7966 (Linking)
VI  - 45
IP  - 5
DP  - 2020 Oct
TI  - Development and Stability Study of an Omeprazole Suppository for Infants.
PG  - 627-633
LID - 10.1007/s13318-020-00629-1 [doi]
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  degrees 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.
FAU - Bestebreurtje, Petra
AU  - Bestebreurtje P
AD  - Department of Clinical Pharmacology, Tergooi Hospital, Hilversum, The 
      Netherlands.
FAU - Roeleveld, Nel
AU  - Roeleveld N
AD  - Department for Health Evidence, Radboud Institute for Health Sciences, Radboud 
      University Medical Center, Nijmegen, The Netherlands.
FAU - Knibbe, Catherijne A J
AU  - Knibbe CAJ
AD  - Department of Clinical Pharmacology, St Antonius Hospital, Nieuwegein, The 
      Netherlands.
AD  - Division of Pharmacology, Leiden Academic Centre for Drug Research, Leiden 
      University, Leiden, The Netherlands.
FAU - van Sorge, Adriaan A
AU  - van Sorge AA
AD  - Department of Clinical Pharmacology, Rijnstate Hospital, Arnhem, The Netherlands.
FAU - Plotz, Frans B
AU  - Plotz FB
AUID- ORCID: 0000-0003-3212-2048
AD  - Department of Paediatrics, Tergooi Hospital, Hilversum, The Netherlands. 
      fbplotz@tergooi.nl.
AD  - Department of Paediatrics, Emma Children's Hospital, Amsterdam UMC, Amsterdam, 
      The Netherlands. fbplotz@tergooi.nl.
FAU - de Wildt, Saskia N
AU  - de Wildt SN
AD  - Department of Pharmacology and Toxicology, Radboud Institute Health Sciences, 
      Radboud University Medical Center, Nijmegen, The Netherlands.
AD  - Paediatric Intensive Care and Department of Paediatric Surgery, Erasmus MC 
      Sophia, Rotterdam, The Netherlands.
LA  - eng
PT  - Journal Article
PL  - France
TA  - Eur J Drug Metab Pharmacokinet
JT  - European journal of drug metabolism and pharmacokinetics
JID - 7608491
RN  - 0 (Excipients)
RN  - 0 (Proton Pump Inhibitors)
RN  - 0 (Suppositories)
RN  - 0 (Triglycerides)
RN  - 12713-12-1 (witepsol)
RN  - 94ZLA3W45F (Arginine)
RN  - KG60484QX9 (Omeprazole)
SB  - IM
MH  - Arginine/chemistry
MH  - Chemistry, Pharmaceutical/methods
MH  - Chromatography, High Pressure Liquid
MH  - Drug Compounding/*methods
MH  - Drug Stability
MH  - Excipients/*chemistry
MH  - Humans
MH  - Infant
MH  - Omeprazole/administration & dosage/*chemistry
MH  - Proton Pump Inhibitors/administration & dosage/*chemistry
MH  - Suppositories
MH  - Temperature
MH  - Triglycerides/chemistry
PMC - PMC7511457
COIS- The authors declare no conflict of interest.
EDAT- 2020/07/01 06:00
MHDA- 2021/07/03 06:00
PMCR- 2020/06/27
CRDT- 2020/06/29 06:00
PHST- 2020/07/01 06:00 [pubmed]
PHST- 2021/07/03 06:00 [medline]
PHST- 2020/06/29 06:00 [entrez]
PHST- 2020/06/27 00:00 [pmc-release]
AID - 10.1007/s13318-020-00629-1 [pii]
AID - 629 [pii]
AID - 10.1007/s13318-020-00629-1 [doi]
PST - ppublish
SO  - Eur J Drug Metab Pharmacokinet. 2020 Oct;45(5):627-633. doi: 
      10.1007/s13318-020-00629-1.