mg/kg/day were given once daily for 8 days in the bolus intravenous injection groups. In the continuous intravenous infusion groups, tacrolimus was infused using an Alzet ® osmotic mini-pump for 9 days at the same doses. Pancreatic insulin content decreased dose-dependently in both the bolus intravenous injection es caused by the two dosing regimens. At 0.03 mg/kg, continuous intravenous infusion did not cause glu-erance. The pharmacokinetic data indicated that continuous intravenous infusion

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... sulted in a sustained blood drug concentration with an area under the curve (AUC) similar to that obtained with the bolus thoraxes of recipients. Tacrolimus doses of 0.01, 0.1, or 1 mg/kg/day were administered from day 0 to day 13. Both bolus intramuscular administration and continuous intravenous infusion prolonged skin allograft groups given the same doses. To summarize, the sustained-release of tacrolimus resulted in a steady blood drug concentration with an AUC similar to that of the bolus administration. In rats, it was better tolerated tion (Cmax). These results indicate that the sustained-release formulation has the potential to improve the safety of tacrolimus.