固体分散を利用したニフェジピンの徐放性顆粒の調製と家兎への経口投与後の速度論的考察

概要

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In order to apply cellulose acetate phthalate (CAP)-polyethylene glycol 4000 (PEG) matrix to the oral sustained-release dosage form, CAP-PEG matrix granules including nifedipine (NF) were prepared by the fusion method. Oral administration of these matrix granules to rabbits resulted in sustained-release characteristics. From the results of the pharmacokinetic study, it was considered that the plasma concentration-time course of NF after oral administration of these matrix granules follows a one-compartment model with instantaneous release and two consecutive first-order input steps. It appeared that in CAP-PEG matrix granules, PEG partly acts as a fast-release compartment and enhances the bioavailability of NF, and CAP controls the release rate of the PEG-entrapped NF. The CAP-PEG matrix appeared to be a suitable carrier of the oral drug-delivery preparation offering sustained-release.
社団法人日本薬学会の論文
1986-12-25