Development and Stability Study of an Omeprazole Suppository for Infants.
Arginine
/ chemistry
Chemistry, Pharmaceutical
/ methods
Chromatography, High Pressure Liquid
Drug Compounding
/ methods
Drug Stability
Excipients
/ chemistry
Humans
Infant
Omeprazole
/ administration & dosage
Proton Pump Inhibitors
/ administration & dosage
Suppositories
Temperature
Triglycerides
/ chemistry
Journal
European journal of drug metabolism and pharmacokinetics
ISSN: 2107-0180
Titre abrégé: Eur J Drug Metab Pharmacokinet
Pays: France
ID NLM: 7608491
Informations de publication
Date de publication:
Oct 2020
Oct 2020
Historique:
pubmed:
1
7
2020
medline:
3
7
2021
entrez:
29
6
2020
Statut:
ppublish
Résumé
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. 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. 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. 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.
Sections du résumé
BACKGROUND AND OBJECTIVE
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
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
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
CONCLUSIONS
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.
Identifiants
pubmed: 32594306
doi: 10.1007/s13318-020-00629-1
pii: 10.1007/s13318-020-00629-1
pmc: PMC7511457
doi:
Substances chimiques
Excipients
0
Proton Pump Inhibitors
0
Suppositories
0
Triglycerides
0
witepsol
12713-12-1
Arginine
94ZLA3W45F
Omeprazole
KG60484QX9
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
627-633Références
Eur J Drug Metab Pharmacokinet. 2020 Oct;45(5):635-643
pubmed: 32594305
Eur J Pediatr Surg. 2013 Jun;23(3):175-81
pubmed: 23720211
Curr Drug Metab. 2013 Feb;14(2):178-85
pubmed: 22935063
Arch Pediatr Adolesc Med. 2008 Nov;162(11):1042-6
pubmed: 18981352
J Pediatr Gastroenterol Nutr. 2007 Jul;45(1):50-5
pubmed: 17592364
Indian Pediatr. 1969 Jun;6(6):422-5
pubmed: 5366304
J Pediatr Gastroenterol Nutr. 2018 Mar;66(3):516-554
pubmed: 29470322
Paediatr Drugs. 2003;5(1):25-40
pubmed: 12513104
Clin Pharmacokinet. 1991 Jan;20(1):38-49
pubmed: 2029801
J Pain Symptom Manage. 1998 Mar;15(3):144-5
pubmed: 9564112
Clin Ther. 2001 May;23(5):660-79; discussion 645
pubmed: 11394727
Clin Pharmacokinet. 2005;44(5):441-66
pubmed: 15871633
J Pediatr Gastroenterol Nutr. 2010 Oct;51(4):448-53
pubmed: 20512059
World J Gastroenterol. 2015 Jul 28;21(28):8508-15
pubmed: 26229394
J Pharm Sci. 1996 Aug;85(8):893-4
pubmed: 8863285