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CHARACTERISTICS OF A NEW ESOMEPRAZOLE PACKET (SACHET) FORMULATION FOR SUSPENSION

N Bladh, E Blychert, K Johansson, G Pettersson, A Törngren
Pharmaceutical and Analytical R&D, AstraZeneca R&D, Lund and Mölndal, Sweden

AIMS: A packet (sachet) formulation of esomeprazole for suspension has recently been developed for patients who have difficulty swallowing solid dosage forms. We report here the characteristics of this new formulation of esomeprazole, including in-suspension stability and suitability for administration orally or via enteral tubes.
METHODS: In-suspension stability was assessed after reconstitution of esomeprazole packet formulations (2.5-40 mg) at different pH (3.4-5.0) in strength-appropriate volumes of water (according to the label handling instructions) held at temperatures ranging from 5°C to 37°C for up to 60 minutes. Suitability for oral administration was examined (2.5 mg and 40 mg strengths) in terms of reconstitution time and the actual dose delivered after simulated oral administration, as well as actual dose delivered via a range of commercially available enteral tubes (6-20 French diameter). Chemical stability and suspension characteristics were also analyzed using applesauce, apple juice and orange juice as alternative reconstitution vehicles.
RESULTS: Across the pH and temperature ranges investigated, the packet formulation was stable for up to 60 minutes after reconstitution. Functionality (dissolution and dispersion) was maintained throughout the permitted resting time of 30 minutes during suspension with water. Chemical degradation was very low (<0.1%) for all reconstitution vehicles investigated. Reconstitution time was 2 minutes with water and 9-10 minutes with either juice. Mean dose delivery was at least 98% after simulated oral administration, and was generally >95% via enteral tubes.
CONCLUSION: The packet (sachet) formulation of esomeprazole has a short reconstitution time, is chemically stable in suspension (remaining fully dispersed for at least 30 minutes) and may be successfully administered orally or via enteral tubes, thereby providing a reliable, flexible and convenient dosing alternative for a wide range of patients who are unable or unwilling to swallow solid dosage forms.
Supported by AstraZeneca. All authors are employees of AstraZeneca

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