Until now, raloxifene transport and metabolism have not been studied adequately, even though they strongly affect raloxifene pharmacokinetics. Therefore, human and porcine liver and intestinal microsomes and diffusion chambers were used to adress this issue. The results showed a pronounced similarity between human and porcine raloxifene conjugation kinetics in intestinal microsomes and a very high metabolic clearance both in liver and intestinal microsomes. Our results explain the extremely low bioavailability of raloxifene (<2%) and its slow intestinal absorption.
COBISS.SI-ID: 2382705
In order to study raloxifene pharmacokinetics in vivo, a new assay was developed and validated for determination of raloxifene and its two metabolites M1 and M2 in human plasma and serum. The method is based on solid phase extraction (SPE) and liquid chromatography with tandem mass spectrometry (LC-MS-MS).
COBISS.SI-ID: 2415729