Enhancement of Bioavailability of Cinnarizine from Its β-Cyclodextrin Complex on Oral Administration with DL-Phenylalanine as a Competing Agent
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説明
The present investigation is concerned with an improvement of the bioavailability of cinnarizine by administering its β-cyclodextrin complex together with another compound which competes with the pcyclodextrin molecule in complex formation in aqueous solution (competing agent). The bioavailability of cinnarizine on oral administration of the cinnarizine-β-cyclodextrin inclusion complex was enhanced by the simultaneous administration of dl-phenylalanine as a competing agent, e.g., the AUC was 1.9 and 2.7 times as large as those of the cinnarizine–β-cyclodextrin complex alone and cinnarizine alone, respectively. The enhancement of AUC and Cmax completely depended on the dose of dl-phenylalanine. It was found from these results that dl-phenylalanine acted as a competing agent in the GI tract and the minimum effective dose required of dl-phenylalanine might be 1 g for 50 mg of cinnarizine in the cinnarizine–β-cyclodextrin complex. Evaluating the competing effect of dl-phenylalanine in vitro using an absorption simulator, it was found that the decreased penetration rate of cinnarizine through the artificial lipid barrier with addition of pcyclodextrin was restored with the addition of dl-phenylalanine.
収録刊行物
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- Journal of Pharmaceutical Sciences
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Journal of Pharmaceutical Sciences 74 (4), 496-497, 1985-04
Elsevier BV
