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Effect of β-cyclodextrin on disposition of hexobarbital and phenobarbital in mice

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Abstract

The effect of β-cyclodextrin (β-CD) on the disposition of hexobarbital (HBA) and phenobarbital (PhBA) after intravenous administration, with the simultaneous administration with β-CD, was investigated in mice.

In the case of HBA, the whole blood concentration was slightly heightened, the brain and liver concentrations were significantly lowered, and the kidney concentration was significantly heightened. Moreover, β-CD also influenced the disposition and formation of 3′-hydroxy- and 3′-keto-HBA. On the other hand, in the case of PhBA, the whole blood concentration was slightly lowered, the time at maximum brain concentration (t-max) was prolonged about 30 to 60 min, the kidney concentration was significantly heightened at the initial stage, while the liver concentration did not show a clear difference by the simultaneous administration with β-CD. These results suggest that the disposition of drugs might be modified by the use of CD.

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Shirakura, O., Nambu, N. & Nagai, T. Effect of β-cyclodextrin on disposition of hexobarbital and phenobarbital in mice. Journal of Inclusion Phenomena 2, 613–621 (1984). https://doi.org/10.1007/BF00662227

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