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Assessment of Age-Related Changes in Pediatric Gastrointestinal Solubility

Anil R Maharaj1, Andrea N Edginton1, Nikoletta Fotaki2

  • 1School of Pharmacy, University of Waterloo, Waterloo, Ontario, Canada.

Pharmaceutical Research
|July 30, 2015
PubMed

Insights

Pediatric gastrointestinal (GI) fluid composition changes significantly from adulthood, impacting drug solubility. Six of seven tested compounds showed altered solubility in pediatric GI fluids, suggesting potential changes in oral drug performance for children.

Area of Science:

  • Biopharmaceutical Sciences
  • Pediatric Drug Development
  • Gastrointestinal Physiology

Background:

  • Compound solubility is a key predictor of oral drug bioavailability.
  • Gastrointestinal (GI) fluid composition undergoes significant developmental changes from infancy to adulthood.
  • Understanding these changes is crucial for accurate pediatric drug dosing and formulation.

Purpose of the Study:

  • To investigate the impact of developmental changes in GI fluid composition on compound solubility.
  • To assess age-specific differences in drug solubility between pediatric and adult populations.
  • To evaluate the performance of Biopharmaceutics Classification System (BCS) Class II compounds in pediatric GI conditions.

Main Methods:

  • Developed pediatric biorelevant media simulating neonatal and infant GI fluid conditions.
  • Utilized established adult media (FaSSGF, FeSSGF, FaSSIF.v2, FeSSIF.v2) as references.
  • Measured solubility of seven BCS Class II compounds at 37 °C in both pediatric and adult media.

Main Results:

  • Six out of seven BCS Class II compounds exhibited solubility outside the 80-125% range of adult values in at least one pediatric medium.
  • Significant age-related alterations in compound solubility were observed.
  • These findings highlight potential challenges in predicting oral drug performance in pediatric populations based on adult data.

Conclusions:

  • Developmental shifts in GI fluid composition significantly influence luminal compound solubility.
  • Discrepancies in solubility between pediatric and adult populations can impact drug efficacy and safety.
  • Further research is needed to optimize pediatric drug formulations considering age-specific physiological differences.
Abstract

Keywords:
biopharmaceuticsbiorelevantpediatricsolubility

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