Ibuprofen lysine salt complexed with β-cyclodextrin oral suspension: an innovative pediatric formulation with clinical advantages.

BACKGROUND

Fever and acute pain are frequent symptoms in pediatric age requiring prompt relief when necessary. International guidelines recommend a standard treatment including ibuprofen and acetaminophen. Ibuprofen is an analgesic and antipyretic agent with anti-inflammatory activity. Since the ibuprofen standard formulation is acid and lipophilic, the solubility in an aqueous environment (typically the gastrointestinal mucosa) is poor. As a result, the absorption and action onset are consequently negatively affected. To solve this drawback, salifying with lysine hastens gastrointestinal absorption and increases gastrointestinal tolerability. In addition, complexation with β-cyclodextrin (β-CD) improves hydro-solubility, increasing and prolonging plasmatic concentrations.

METHODS

This compound is presently available as oral suspension indicated in children and adolescents. Thus, the present article reviews and discusses the pharmacological profile of this product.

RESULTS

Although ibuprofen lysine salt complexed with β-cyclodextrin (ILS-β-CD) has a similar safety profile to other NSAIDs, its quick absorption and high and prolonged plasmatic concentrations make it ideal for managing acute conditions. Two clinical studies investigated this product.

CONCLUSIONS

Based on this evidence, ILS-β-CD may represent a beneficial option for managing fever and pain in children and adolescents. This formulation may provide a rapid onset of action and prolonged concentrations, assuring adequate therapeutic concentrations, optimal tolerability, and a valuable safety profile.