Stereoselective plasma protein binding of ibuprofen enantiomers
- 1 January 1989
- journal article
- research article
- Published by Springer Science and Business Media LLC in European Journal of Clinical Pharmacology
- Vol. 36 (3), 283-290
- https://doi.org/10.1007/bf00558161
Abstract
We have developed a novel and reproducible method for determining the plasma protein binding of the two ibuprofen enantiomers in the presence of each other. The method involves the use of radiolabelled racemic ibuprofen, equilibrium dialysis, derivatization of the enantiomers to diastereomeric amides, high-performance liquid chromatography, and radiochemical analysis. We have determined the plasma protein binding of R(−)- and S(+)-ibuprofen in 6 healthy male volunteers after the oral administration of 800 mg racemic ibuprofen. The mean time-averaged percentage unbound of the R(−)-enantiomer, 0.419 was significantly less than that of the S(+)-enantiomer, 0.643, consistent with stereoselective plasma protein binding. The percentage unbound of each ibuprofen enantiomer was concentration-dependent over the therapeutic concentration range and was influenced by the presence of its optical antipode.This publication has 20 references indexed in Scilit:
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