Pharmacokinetics of clodronate after single intravenous, intramuscular and subcutaneous injections in rats

Pharmacol Toxicol. 1991 Nov;69(5):365-8. doi: 10.1111/j.1600-0773.1991.tb01312.x.

Abstract

The pharmacokinetics of clodronate was studied in rats after single intravenous, intramuscular and subcutaneous doses of a mixture of unlabelled and 14C-labelled disodium clodronate (25 mg/5 muCi/kg). The peak clodronate concentration in plasma was reached within 5 min., and the drug was eliminated with a half-life of about 1.5 hr regardless of administration route. Bioavailabilities after intramuscular and subcutaneous administration were 105% and 89%, respectively. During the 72 hr collection period, the mean share of clodronate recovered from the urine was about 53% of the dose regardless of administration route. Most of the drug was excreted during the first 24 hr. The amount of clodronate in bone (femur) was 186 micrograms/g tissue at 2 hr after intravenous administration, 188 micrograms/g after intramuscular administration and 157 micrograms/g after subcutaneous administration. It is concluded that absorption of clodronate after intramuscular and subcutaneous administration is rapid and good, and that the concentrations of the drug in bone after 2 hr are about the same as after intravenous administration.

Publication types

  • Comparative Study

MeSH terms

  • Absorption
  • Animals
  • Biological Availability
  • Clodronic Acid / administration & dosage
  • Clodronic Acid / pharmacokinetics*
  • Half-Life
  • Injections, Intramuscular
  • Injections, Intravenous
  • Injections, Subcutaneous
  • Male
  • Rats
  • Rats, Inbred Strains

Substances

  • Clodronic Acid