Palatability and Stability Studies to Optimize a Carvedilol Oral Liquid Formulation for Pediatric Use
Blanca Chiclana-Rodríguez1, Encarnacion Garcia-Montoya1,2, Miquel Romero-Obon1
1Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain.
Pharmaceutics
|January 23, 2024
Summary
Developing a palatable liquid formulation of carvedilol (CARV) is crucial for pediatric cardiovascular disease treatment. This study successfully created a stable, great-tasting CARV liquid, improving patient acceptance.
Area of Science:
- Pharmaceutical Sciences
- Pediatric Pharmacology
- Drug Formulation
Background:
- Carvedilol (CARV) is an alpha- and beta-blocker used off-label for pediatric cardiovascular conditions.
- A need exists for a pediatric-appropriate liquid formulation of CARV, as none are currently marketed.
- Palatability is critical for pediatric formulation acceptance, directly impacting adherence and therapeutic outcomes.
Purpose of the Study:
- To develop and assess the palatability and acceptability of novel CARV liquid formulations for pediatric use.
- To identify the optimal CARV formulation with enhanced taste and odor profiles.
- To evaluate the physicochemical and microbiological stability of the selected CARV formulation.
Main Methods:
- Preparation of CARV solutions with varying concentrations of flavoring agents and sweeteners (sucralose).
- In vivo taste assessment using adult volunteers to evaluate palatability and sensory attributes via questionnaires and sensory tests.
- Stability testing of the optimized formulation under various temperature conditions (25°C, 30°C, 40°C) for 6 months and in-use stability for 15 days at 25°C.
Main Results:
- Palatability scores significantly increased from 1.60 (unflavored) to 7.65 (optimized flavored formulation) on a 10-point scale.
- Bitterness was reduced from 66.67% to 17.86%, and taste pleasantness improved from 25/100 to 73/100 in the optimized formulation.
- The optimized CARV liquid formulation demonstrated confirmed physicochemical and microbiological stability over 6 months and during in-use conditions.
Conclusions:
- A palatable and stable liquid formulation of carvedilol suitable for pediatric use has been successfully developed.
- The optimized formulation incorporates pediatric-appropriate excipients, including sucralose and specific flavoring agents.
- This development addresses a critical unmet need for an acceptable and stable CARV oral solution in pediatric patients.
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