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

Abstract

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.