徐放性テオフィリン製剤の体内動態モデルとin vivo溶出の評価

概要

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A pharmacokinetic model including the drug release process was proposed to simulate kinetically some complicated plasma concentration profiles of theophylline after single oral dose (300mg) of the 3 commercial sustained-release theophylline preparations (Theolong^<[○!R]>, Theodur^<[○!R]>, Slo-bid^<[○!R]>) on separate occasions into 4 healthy adult volunteers on empty stomach. In this model, the two step release process consisting of zero-order and first-order rate was assumed, which was connected to the one-compartment model with first-order elimination process. The parameters in drug release process were estimated by fittings of plasma concentration data to the mathematical model and individual plasma concentration data of the 3 different slow release products could be appropriately simulated by the same mathematical model. The drug release-time profiles, calculated by using the estimated parameters, were compared between subjects and between products. From the present single oral dose studies on empty stomach, the marked differences in release rat between products were observed and Theodur^<[○!R]> tablets seemed to be more adequate formulations for a twice daily dosage regimen.
日本医療薬学会の論文
1988-12-20