YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
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
大西 憲明横山 照由梅田 常雄清原 義史黒田 勤喜多 良昭黒田 耕司
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1986 年 106 巻 12 号 p. 1131-1136

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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.

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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