Suesskind-Schwendi, Marietta von and Gruber, Michael and Touraud, Didier and Kunz, Werner and Schmid, Christof and Hirt, Stephan W. and Lehle, Karla (2013) Pharmacokinetics of a self-microemulsifying drug delivery system of tacrolimus. BIOMEDICINE & PHARMACOTHERAPY, 67 (6). pp. 469-473. ISSN 0753-3322,
Full text not available from this repository. (Request a copy)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 ethyl 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 concentrations of tacrolimus from two study groups (oral application of SMEDDS Tac and Prograf (R)) were determined using ELISA technique following tacrolimus administration in rats. There was no difference between area under the whole blood concentration-time curve in the SEDDM Tac group and the Prograf (R) group. Maximum concentrations 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 (R) group (P < 0.05). However, the Tac concentration 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 composition might have advantage as an alternative oral dosage form for Tac. (C) 2013 Elsevier Masson SAS. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CLINICAL PHARMACOKINETICS; ORGAN-TRANSPLANTATION; ORAL BIOAVAILABILITY; LIPID FORMULATIONS; LIPOPHILIC DRUGS; WHOLE-BLOOD; SOLUBILITY; ABSORPTION; EMULSION; EFFICACY; FK 506; Blood levels; Rats |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Medicine > Lehrstuhl für Anästhesiologie Medicine > Lehrstuhl für Herz-, Thorax- und herznahe Gefäßchirurgie Chemistry and Pharmacy > Institut für Physikalische und Theoretische Chemie > Chair of Chemistry VI - Physical Chemistry (Solution Chemistry) > Prof. Dr. Werner Kunz |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 06 Apr 2020 13:01 |
| Last Modified: | 06 Apr 2020 13:01 |
| URI: | https://pred.uni-regensburg.de/id/eprint/16397 |
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