イブプロフェンマイクロスフェアーを用いたサスペンジョン型経口徐放剤の薬物放出特性と生物学的利用能

概要

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The drug release behavior and bioavailability of newly developed controlled release suspensions of ibuprofen were investigated. The suspension was prepared by suspending spherical matrices(particle diameter 350-800 μm) of the drug with acrylic polymer in aqueous media containing sodium carboxymethylcellulose and D-sorbitol whose pH was adjusted below 3.0. The drug release behavior of suspension precisely followed to that of original spherical matrix, suggesting little leakage of the drug from the suspended matrices during storage, The bioavailability of rapid drug release suspensions administrated orally was determined by the initial drug release rate of the suspended matrices in vitro dissolution test. Whereas the bioavailability of sustained drug release suspension orally administrated depended on the particle sires of suspended matrices, even with same drug release behavior in vitro. Finally, twice a day regimen was successfully achieved by administering orally 225.0 mg of the sustained release matrices suspended to beagle dogs.