Identification of paliperidone metabolites in humans
| Metabolite | Identification Method | [M + H]+ | Characteristic Product Ions (m/z) | Identification | Plasma | Urine | Feces |
|---|---|---|---|---|---|---|---|
| UDa | LC-MS/MS cochromatography | 427 | 207, 179, 165, 110 | Paliperidone | + | + | N.D. |
| M1a | LC-MS/MS | 239 | 175, 177 | Oxidative N-dealkylation-acid metabolite | N.D. | + | N.D. |
| M9 | LC-MS/MS | 443 | 223 | Monohydroxylation of alicyclic ring of paliperidone | N.D. | + | N.D. |
| M10 | Coelution with rat feces metabolite LC-MS/MS | 446 | 205, 223 | Benzisoxazole scission and monohydroxylation of alicyclic ring | N.D. | N.D. | + |
| M11a | Coelution with rat feces metabolite LC-MS/MS | 430 | 207 | Benzisoxazole scission | N.D. | N.D. | + |
| M12a | LC-MS/MS cochromatography | 425 | 205, 233 | Alcohol dehydrogenation-ketone metabolite at the 9-hydroxy function of paliperidone | N.D. | + | N.D. |
| M16 | LC-MS/MS enzymatic hydrolysis | 606 | 207, 430 | Benzisoxazole scission and glucuronidation (glucuronide of M11) | N.D. | + | N.D. |
| N.D. | No spectrum available | Unknown metabolite | N.D. | N.D. | + |
N.D., not detected.
↵ a Identification was confirmed by comparison with authentic standard.