Development and testing in healthy adults of oral hydrocortisone granules with taste masking for the treatment of neonates and infants with adrenal insufficiency

J Clin Endocrinol Metab. 2015 Apr;100(4):1681-8. doi: 10.1210/jc.2014-4060. Epub 2015 Feb 3.

Abstract

Background: Treatment of neonates and infants with adrenal insufficiency is unsatisfactory because unlicensed hydrocortisone formulations are used.

Objectives: The objectives were to survey current hydrocortisone prescribing practice and develop a novel hydrocortisone formulation, Infacort.

Methods: The use of hydrocortisone by European pediatric endocrinologists was surveyed. Based on this, an oral hydrocortisone granule formulation, Infacort, with taste masking was developed and evaluated in vitro and then in vivo in a phase I pharmacokinetic study.

Results: The survey showed that pediatricians use a variety of unlicensed compounded adult medications at doses of between 0.5 and 5 mg. Infacort was formulated with a taste-masking layer stable for at least 5 minutes in aqueous media and was produced in unit doses of 0.5, 1, 2, and 5 mg. Infacort 10 mg is the bioequivalent of a 10-mg hydrocortisone tablet (mean area under the curve from zero to infinity [AUC(0-inf)] ratio, 101%; 90% confidence interval, 96-107%). Mean cortisol maximum concentration (C(max)) and AUC(0-inf) values after administration of Infacort were linear with dose and dose proportional when adjusted for saturable plasma protein binding. Subjects rated Infacort as "not good or bad" for smell (86%), feel in the mouth (71%), and taste (79%). No serious adverse events were reported.

Conclusions: This phase 1 study demonstrates that Infacort is safe, well tolerated, of neutral taste, bioequivalent to hydrocortisone licensed for adults, and shows dose proportionality with respect to cortisol exposure. Infacort is expected to facilitate optimization of hydrocortisone dosing in neonates and children with adrenal insufficiency; however, clinical studies will be required to demonstrate efficacy in this patient age group.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adrenal Insufficiency / congenital*
  • Adrenal Insufficiency / drug therapy
  • Adult
  • Cross-Over Studies
  • Dosage Forms
  • Healthy Volunteers
  • Humans
  • Hydrocortisone / administration & dosage*
  • Hydrocortisone / adverse effects
  • Hydrocortisone / blood
  • Hydrocortisone / pharmacokinetics
  • Infant, Newborn
  • Male
  • Middle Aged
  • Palate
  • Taste* / drug effects
  • Therapeutic Equivalency
  • Young Adult

Substances

  • Dosage Forms
  • Hydrocortisone

Supplementary concepts

  • Adrenal Insufficiency, Congenital