Pharmacokinetics and Bioavailability of Tacrolimus in Rats with Experimental Renal Dysfunction
| Autor: | Hiromi Okabe, Ken-ichi Inui, Yukiya Hashimoto |
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| Rok vydání: | 2000 |
| Předmět: |
Male
medicine.medical_specialty Metabolic Clearance Rate medicine.medical_treatment Intraperitoneal injection Biological Availability Pharmaceutical Science Renal function Tacrolimus Intestinal absorption Blood Urea Nitrogen Pharmacokinetics Oral administration Internal medicine medicine Animals Aspartate Aminotransferases Renal Insufficiency Rats Wistar Infusions Intravenous Blood urea nitrogen Pharmacology business.industry Alanine Transaminase Rats Bioavailability surgical procedures operative Endocrinology Intestinal Absorption Area Under Curve Creatinine Cisplatin business Immunosuppressive Agents |
| Zdroj: | Journal of Pharmacy and Pharmacology. 52:1467-1472 |
| ISSN: | 2042-7158 0022-3573 |
| Popis: | The effects of renal failure on the pharmacokinetics and bioavailability of tacrolimus were investigated in rats. Experimental renal dysfunction was induced by intraperitoneal injection of cisplatin (5 mg kg−1) into rats. The blood concentration of tacrolimus was measured after intravenous and intra-intestinal administration of the drug. The blood concentration of tacrolimus after intravenous administration (1 mg kg−1) was slightly increased (up to 1.3 fold) by induction of renal dysfunction. In contrast, the peak tacrolimus concentration after intra-intestinal administration (1 mg kg−1 or 3 mg kg−1) in rats with renal failure was about 2-fold higher than that in normal controls. The bioavailability was increased by about 35% in rats with impaired renal function as compared with normal controls. These results suggested that the bioavailability of tacrolimus, which is mainly metabolized in the liver and intestine after oral administration, is also influenced by renal function. |
| Databáze: | OpenAIRE |
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