“Compound solubility serves as a surrogate indicator of oral biopharmaceutical performance. Between infancy and adulthood, marked compositional changes in gastrointestinal (GI) fluids occur.” – Maharaj, et al. Pharm Res. 2016; 33: 52-71
Solubility is an important aspect in the development of oral drugs. It is especially important for developers to take into consideration during the development of oral pediatric drugs. Poorly soluble oral pediatric drugs can cause local tissue injury, reduced bioavailability and adverse events.
Solubility affects a drug’s therapeutic index by causing issues with permeability through cell membranes at the site of action. This means that formulation are often created to impact the solubility profile of an oral drug.
Solubility has other factors that are particularly important for pediatric patients. A 2015 article in the British Journal of Clinical Pharmacology explains that the importance of considering how a drug’s solubility affects taste. The authors write, “The solubility of the drug needs to be balanced with taste-masking as highly soluble drugs will activate taste receptors on the tongue if they dissolve in saliva within the oral cavity.” According to an Orbis-led focus group of pediatric pharmacists, taste is the most important aspect of pediatric dosage forms.
Poorly soluble oral pediatric drugs can also cause adverse events. According to a 2011 review article, “Many active ingredients are not readily soluble in water. Therefore, other solvents such as alcohols, glycerin, polyethylene glycol and propylene glycol are also used.” The authors state that alcohols can be toxic, especially to the very young. Toxicity leads to adverse events, so pediatric formulations often try to avoid using alcohols, causing a dilemma when formulating the poorly soluble drug.
Pediatric drug formulations take the issue of solubility beyond bioavailability and into taste masking and complications with excipients. Orbis Biosciences® uses Precision Particle FabricationTM technology to design with the patient’s needs in mind and to develop format-flexible drugs for patients of all ages. Orbis understands the importance of solubility and prioritizes the health of even the youngest among us.