Treating pediatric population presents challenges due to the limited availability of age-appropriate dosage forms, lack in clinical studies involving children and difficulty of administration. In addition, excipients commonly used in dosage forms for adults can be harmful for children. For this reason, the safety and suitability of excipients and formulations must be carefully considered when developing pediatric medicines. Much research explored granules, multiparticle aggregates, as pediatric solid oral dosage form.

The selection of granules offers several advantages, since they can effectively mask the unpleasant taste of drugs and enhance patient compliance, as they are generally easier to administer than tablets, which can be difficult for children to swallow. In this study the influence of polymers on granule technological properties and manufacturing process were investigated. Specifically, synthetic polymers (polyvinylpyrrolidone or hydroxyethyl cellulose) were compared to natural polysaccharides obtained from starch. Paracetamol was used as model drug and wet granulation was selected as manufacturing process. A library of formulation were explored to prepare granules and characterized determining flow properties, sizes, solubility, excipient interactions by FTIR and DSC and morphology by SEM.

All granules showed sizes lower than 1 mm and good technological properties. In vitro dissolution rate of paracetamol in granules was faster than commercial paracetamol powder granules. The best granule formulations were selected and submitted to industry for the industrial scale-up.

The results demonstrated the possibility to use polysaccharides in granulating fluids producing optimal granules properties for pediatric formulations and industrial applications.

Acknowledgments

research was funded by Università degli Studi di Milano, Piano di Sostegno alla Ricerca 2023, Linea 2.