Pharmacokinetics of Acemetacin, a New Anti-inflammatory Agent : Comparison with Indomethacin and Particle-size Effect on Oral Absorption
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The particle-size effect of acemetacin on oral absorption was evaluated in three normal male subjects with standardized breakfast. Two sieved particle-size formulations were used: one with crystals with mean equivalent spherical diameter of 27.6μm and the other with crystals with mean equivalent spherical diameter of 3.8μm.<BR>Plasma acemetacin and indomethacin concentrations and urinary drug excretion were used to determine the relative absorption of the two formulations. Particle-size had a dramatic effect on oral absorption of the drug. The smaller crystals produced higher plasma indomethacin concentrations and more rapid peak concentration attainment.<BR>The pharmacokinetics of acemetacin was compared with indomethacin after a single oral dosing in three normal male subjects with standardized breakfast. Mean absorption parameters for 30 mg acemetacin, 25 mg indomethacin of conventional capsule and 25 mg indomethacin of timed-release capsule were as follows. Mean C<SUB>max</SUB> of plasma indomethacin concentrations were 481, 754 and 684 ng/ml and t<SUB>max</SUB>. were 3, 2 and 4 hr after dosing, respectively. With acemetacin t1/2 (α) of plasma indomethacin concentrations was 0.6 hr and t1/2 (β) was 3 hr. Aceme tacin was mainly metabolized to indomethacin and, in part, to deschlorobenzoylacemetacin and desmethylacemetacin in man. The possibility that the characteri stics of acemetacin kinetics may be related to the decrease of indomethacininduced side effects in clinical situation was discussed.
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- Pharmacokinetics of Acemetacin, a New Anti-inflammatory Agent : Comparison with Indomethacin and Particle-size Effect on Oral Absorption