Absorption, metabolism and excretion after oral administration of a new Ca antagonist, 14C-benidipine hydrochloride to man
| Autor: | P. D. Dalrymple, S. Kobayashi, S. G. Wood, L. F. Chasseaud, H. Kobayashi |
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| Rok vydání: | 1997 |
| Předmět: |
Adult
Male Dihydropyridines Chromatography Gas Health Toxicology and Mutagenesis Metabolite Biological Availability Urine Pharmacology Toxicology Biochemistry Intestinal absorption Excretion Feces chemistry.chemical_compound Pharmacokinetics Oral administration Electrochemistry Humans Chromatography High Pressure Liquid Chemistry Half-life Blood Proteins General Medicine Calcium Channel Blockers Intestinal Absorption Area Under Curve Benidipine Half-Life Protein Binding |
| Zdroj: | Xenobiotica. 27:597-608 |
| ISSN: | 1366-5928 0049-8254 |
| DOI: | 10.1080/004982597240370 |
| Popis: | 1. In healthy male volunteers, the absorption, metabolite profiles and excretion of 14C-benidipine hydrochloride, a new Ca antagonist, were investigated after oral administration at a dose of 8 mg. 2. 14C-benidipine hydrochloride was rapidly absorbed, and the plasma concentration of radioactivity and unchanged drug reached a maximum of 71.2 ng eq./ml at 1.1 h and 2.56 ng/ml at 0.6 h respectively, and then declined bi-exponentially. The half-life in the elimination phase was 14.7 and 5.3 h respectively, AUC of unchanged drug was low, about 1% of that of radioactivity. 3. Five days after administration, 36.4% of the administered radioactivity was excreted in urine and 58.9% in faeces. 4. The metabolite profiles in plasma, urine and faeces were analysed by hplc. At 1 h after administration the predominant metabolites in plasma were M9 and M2, which accounted for 13.8 and 8.2% of the radioactivity respectively, whereas unchanged drug represented 1.2%. Predominant metabolites in urine 12 h after administration were M3 and M8, which accounted for 2.22 and 2.21% of the administered radioactivity respectively. Metabolites excreted in faeces 120 h after administration were very complex and poorly separated by hplc and could not be characterized: unchanged drug was not detected in the faeces. |
| Databáze: | OpenAIRE |
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