Ketamine has been widely used for analgesia in patients with neuropathic pain. However, only injectable forms of ketamine are commercially available in Japan. We have previously reported a new oral preparation of ketamine, the ketamine Agar-Gel. In the present study, we examined the pharmacokinetic characteristics of ketamine and norketamine after oral administration of the Agar-Gel in comparison with those after buccal administration. Four healthy volunteers were given the ketamine Agar-Gel orally or buccally in random order. Venous blood samples were obtained before and up to 6 hour after administration, and plasma concentrations of ketamine and norketamine, a metabolite form of ketamine, were measured by high-performance liquid chromatograph. The plasma concentration of norketamine was significantly higher than that of ketamine after oral administration (p<0.05). The AUC
0→6h value of ketamine after buccal administration was about twofold higher than that after oral administration, while the AUC
0→6h of norketamine after buccal administration was lower than that after oral administration. These results indicate that the extensive first-pass metabolism of ketamine would be inhibited by the buccal route.
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