Considerations when deriving compound-specific limits for extractables and leachables from pharmaceutical products: Four case studies

Regul Toxicol Pharmacol. 2020 Dec:118:104802. doi: 10.1016/j.yrtph.2020.104802. Epub 2020 Oct 7.

Abstract

Leachables from pharmaceutical container closure systems are a subset of impurities that present in drug products and may pose a risk to patients or compromise product quality. Extractable studies can identify potential leachables, and extractables and leachables (E&Ls) should be evaluated during development of the impurity control strategy. Currently, there is a lack of specific regulatory guidance on how to risk assess E&Ls; this may lead to inconsistency across the industry. This manuscript is a cross-industry Extractables and Leachables Safety Information Exchange (ELSIE) consortium collaboration and follow-up to Broschard et al. (2016), which aims to provide further clarity and detail on the conduct of E&L risk assessments. Where sufficient data are available, a health-based exposure limit termed Permitted Daily Exposure (PDE) may be calculated and to exemplify this, case studies of four common E&Ls are described herein, namely bisphenol-A, butylated hydroxytoluene, Irgafos® 168, and Irganox® 1010. Relevant discussion points are further explored, including the value of extractable data, how to perform route-to-route extrapolations and considerations around degradation products. By presenting PDEs for common E&L substances, the aim is to encourage consistency and harmony in approaches for deriving compound-specific limits.

Keywords: BHT; BPA; Extractables; Irgafos® 168; Irganox® 1010; Leachables; PDE.

MeSH terms

  • Animals
  • Benzhydryl Compounds / analysis*
  • Benzhydryl Compounds / pharmacokinetics
  • Benzhydryl Compounds / toxicity
  • Butylated Hydroxytoluene / analogs & derivatives*
  • Butylated Hydroxytoluene / analysis*
  • Butylated Hydroxytoluene / pharmacokinetics
  • Butylated Hydroxytoluene / toxicity
  • Cricetinae
  • Decision Trees
  • Drug Contamination*
  • Drug Packaging*
  • Humans
  • Mice
  • Patient Safety
  • Pharmaceutical Preparations / analysis*
  • Phenols / analysis*
  • Phenols / pharmacokinetics
  • Phenols / toxicity
  • Phosphites / analysis*
  • Phosphites / pharmacokinetics
  • Phosphites / toxicity
  • Rats
  • Risk Assessment
  • Toxicity Tests*
  • Toxicokinetics

Substances

  • Benzhydryl Compounds
  • Pharmaceutical Preparations
  • Phenols
  • Phosphites
  • Butylated Hydroxytoluene
  • tris-(2,4-di-tert-butylphenyl) phosphite
  • Irganox 1010
  • bisphenol A