Pharmacokinetic Evaluation of a Single Intramuscular High Dose versus an Oral Long-Term Supplementation of Cholecalciferol

PLoS One. 2017 Jan 23;12(1):e0169620. doi: 10.1371/journal.pone.0169620. eCollection 2017.

Abstract

Background and objectives: Vitamin D deficiency is frequent during the winter and occurs throughout the year in the elderly or patients suffering from autoimmune diseases. The objective of this study was to evaluate the pharmacokinetic properties of oral supplementation versus a single intramuscular injection of cholecalciferol in healthy individuals.

Research design and methods: Up to 8,000 I.U. oral cholecalciferol was administered daily for 84 days in a 4 week dose-escalation setting to vitamin D deficient individuals. In another cohort, a single intramuscular injection of 100,000 I.U. cholecalciferol was given. In both cohorts, individuals without vitamin D intake served as the comparison group. 25-hydroxyvitamin D (25(OH)D) concentrations were measured in all individuals at defined time points throughout the studies.

Results: The mean 25(OH)D serum concentration increased significantly after oral cholecalciferol intake compared to the control group (day 28: 83.4 nmol/l and 42.5 nmol/l; day 56: 127.4 nmol/l and 37.3 nmol/l; day 84: 159.7 nmol/l and 30.0 nmol/l). In individuals receiving 100,000 I.U. cholecalciferol intramuscular, the mean 25(OH)D serum concentration peaked after 4 weeks measuring 70.9 nmol/l compared to 32.7 nmol/l in the placebo group (p = 0.002). The increase of 25(OH)D serum concentrations after 28 days was comparable between both routes of administration (p = 0.264).

Conclusions: Oral and intramuscular cholecalciferol supplementation effectively increased serum 25(OH)D concentrations.

MeSH terms

  • Administration, Oral
  • Adult
  • Cholecalciferol / administration & dosage*
  • Cholecalciferol / pharmacokinetics
  • Cohort Studies
  • Female
  • Humans
  • Injections, Intramuscular
  • Male
  • Vitamin D / analogs & derivatives
  • Vitamin D / blood

Substances

  • Vitamin D
  • Cholecalciferol
  • 25-hydroxyvitamin D

Grants and funding

The clinical trials were supported by the Deutsche Forschungsgemeinschaft (DFG - SFB650/TP5) (oral study) and by Heyl Chemisch-pharmazeutische Fabrik GmbH & Co. KG (i.m. study).