In-vitro and in-vivo evaluation of taste-masked ibuprofen formulated in oral dry emulsions

Abstract

Objective

The aim of this study was to develop a pediatric oral preparation for ibuprofen.

Significance

Ibuprofen is widely used for defervescence in children, but medication compliance is poor due to its bitter taste. Dry emulsions possess good stability and can be transported and stored in solid form; they can be dispersed into liquid emulsions with water and easily administered to children.

Methods

In this study, a dry emulsion excipient was prepared by spray drying: a mixture of orange peel and corn oils (3:7, w/w) was used as the oil phase and solvent for ibuprofen; gum arabic and gum tragacanth were chosen as emulsifiers; and maltodextrin was used as a solid carrier.

Results

The particle sizes of the liquid and reconstituted emulsions were 5.75 µm and 6.11 µm, respectively; the average particle size distribution of the dry emulsion powder was 8.13 µm; scanning electron microscopy showed that the dry emulsion powder was composed of evenly distributed smooth spheres. At a drug loading of 36.52 ± 1.15 mg/g, 90% of ibuprofen was released from the dry emulsion excipient within 30 min. Sensory evaluations using human volunteers, rats, and an electronic tongue demonstrated that the emulsion had a taste-masking effect on ibuprofen. It was further corroborated by in vivo studies using a rat model that highlighted a 1.76-fold increase in ibuprofen absorption when the drug was administered as an emulsion compared with granules.

Conclusions

These results indicate that the dry emulsion for taste-masking is promising and valuable in the development of ibuprofen for pediatrics.

Keywords:

• Ibuprofen
• pediatric oral preparations
• dry emulsions
• taste masking
• pharmacokinetics

Acknowledgments

The authors express their gratitude to EditSprings (https://www.editsprings.com/) for the expert linguistic services provided.

Author contributions

HQ: methodology, data curation, and writing––original draft preparation; JD: methodology and investigation; FZ: resources and formal analysis; XQ: conceptualization, methodology, project administration, and writing––review & editing.

Disclosure statement

No potential conflict of interest was reported by the author(s).