Abstract
This study evaluated the pharmacokinetics of tacrolimus (Tac) in a novel self-microemulsifying drug delivery system (SMEDDS) for improved oral administration. SMEDDS Tac consisted of Et oleate as the oily phase, Solutol HS 15 as the surfactant and glycofurol as the co-surfactant and contained 0.5 mg/mL tacrolimus. Blood and tissue concns. of tacrolimus from two study groups (oral application of ...
Abstract
This study evaluated the pharmacokinetics of tacrolimus (Tac) in a novel self-microemulsifying drug delivery system (SMEDDS) for improved oral administration. SMEDDS Tac consisted of Et oleate as the oily phase, Solutol HS 15 as the surfactant and glycofurol as the co-surfactant and contained 0.5 mg/mL tacrolimus. Blood and tissue concns. of tacrolimus from two study groups (oral application of SMEDDS Tac and Prograf) were detd. using ELISA technique following tacrolimus administration in rats. There was no difference between area under the whole blood concn.-time curve in the SEDDM Tac group and the Prograf group. Maximum concns. of the drug were three times higher (P < 0.05) in the SEDDM Tac group accompanied by a 3-fold earlier peak time. Elimination half-life was significantly lower in the SEDDM Tac group. Application of SMEDDS Tac increased tissue accumulation. Already after 15 min, Tac levels of small intestine, liver, kidney, spleen, heart and bone marrow were significantly higher in the SMEDDS Tac group than in the Prograf group (P < 0.05). However, the Tac concn. in the kidney was significantly lower in the SMEDDS Tac group. Formulation of SMEDDS did not affect blood-brain barrier function. The SMEDDS is a potentially useful method for a local delivery of Tac to target organs. The selection of the optimum SMEDDS Tac compn. might have advantage as an alternative oral dosage form for Tac. [on SciFinder(R)]
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