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Absorption kinetics of cyclosporin in the rat

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Abstract Cyclosporin was administered (6 mg kg−1, i.v.) over 15 min, or (10 mg kg−1) by gavage, to two groups of 5 rats. Following i.v. infusion, cyclosporin exhibited triphasic behaviour with mean ± s.e.m. disposition half-lives of 9·0 ± 1·3 min, 4·0 ± 0·5 h and 16·0 ± 1·7 h. Following oral administration, peak blood concentration (Cmax) of 1290 ± 93 ng mL−1 was reached after 5 h, when cyclosporin absorption essentially ceased. The absolute bioavailability (F) of cyclosporin was 24·0%. Standard laboratory rat chow consisting of 2% corn oil did not appear to alter cyclosporin absorption kinetics.
Title: Absorption kinetics of cyclosporin in the rat
Description:
Abstract Cyclosporin was administered (6 mg kg−1, i.
v.
) over 15 min, or (10 mg kg−1) by gavage, to two groups of 5 rats.
Following i.
v.
infusion, cyclosporin exhibited triphasic behaviour with mean ± s.
e.
m.
disposition half-lives of 9·0 ± 1·3 min, 4·0 ± 0·5 h and 16·0 ± 1·7 h.
Following oral administration, peak blood concentration (Cmax) of 1290 ± 93 ng mL−1 was reached after 5 h, when cyclosporin absorption essentially ceased.
The absolute bioavailability (F) of cyclosporin was 24·0%.
Standard laboratory rat chow consisting of 2% corn oil did not appear to alter cyclosporin absorption kinetics.

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