Pharmacokinetics of clodronate after single intravenous, intramuscular and subcutaneous injections in rats.
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.
Laurén
L
L
Biomedical Research Center, Huhtamäki Oy Leiras, Turku, Finland.
Osterman
T
T
Karhi
T
T
D000042:Absorption; D000818:Animals; D001682:Biological Availability; D004002:Clodronic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D007279:Injections, Subcutaneous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D004002:Clodronic Acid