We conducted a cross-over single-dose pharmacokinetic study in 4 pigs to measure the bioavailability of ciclosporin (CS) after intravenous and intramuscular administration. Each animal was given 5 mg/kg i.v. followed by 20 mg/kg i.m. after 1 week. Serial blood samples were taken over 36 h after each dose, and the concentration of CS was assayed by radioimmunologic methods. The pharmacokinetic parameters after intravenous administration were (mean ± SD; n = 4): clearance = 327 ± 21 ml/h/kg; volume of distribution = 7.2 ± 2.8 liters/kg. The same parameters after intramuscular dosing were: clearance = 326 ± 59 ml/h/kg; volume of distribution = 6.9 ± 2.1 liters/kg. The percent bioavailability of intramuscular CS was 101.9 ± 13.3 with a mean absorption time of 10.6 ± 2.7 h. Our results indicate that following a single dose, the percent bioavailability of intramuscular CS in pigs is considerably greater than that reported in previous studies.

Keywords:
Ciclosporin, Pharmacokinetics, Intramuscular administration, Liver allotransplantation
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© 1990 S. Karger AG, Basel
1990
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