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Enhancement of the bioavailability of cinnarizine from its .BETA.-cyclodextrin complex on oral administration with L-isoleucine as a competing agent.

1986; Pharmaceutical Society of Japan; Volume: 34; Issue: 3 Linguagem: Inglês

10.1248/cpb.34.1275

1347-5223

Tadakazu Tokumura, Yuki Tsushima, Kimio Tatsuishi, Masanori Kayano, Yoshiharu Machida, Tsuneji Nagai,

Cancer Treatment and Pharmacology

This investigation was aimed at the improvement of the bioavailability of cinnarizine (CN) by administering its β-cyclodextrin (β-CD) complex together with a competing agent. The ability of L-leucine (L-Leu) and L-isoleucine (L-Ileu) to act as competing agents was evaluated by determining the penetration rate of CN, employing a Sartorius absorption simulator. L-Ileu showed a stronger competing action than L-Leu. The bioavailability of CN, upon oral administration of the CN-β-CD inclusion complex, was enhanced by the simultaneous administration of L-Ileu as a competing agent; Cmax was 1.9 and 2.7 times those of CN-β-CD complex alone and CN alone, respectively. L-Leu showed no clear effect on the bioavailability. The in vivo competing effects of L-Leu and L-Ileu appeared to be in agreement with the in vitro evaluations.