Drug partition chromatography on immobilized porcine intestinal brush border membranes.
We immobilized porcine intestinal brush border membrane vesicles (BBMVs) for chromatographic analyses of drug partitioning into the membranes determined as Ks, the drug retention per phospholipid amount. For positive and neutral drugs Ks decreased day by day, whereas Ks for negative drugs increased marginally. Similar results on vesicle-lipid liposomes indicated a gradual loss of negative charge from the columns. The Ks values for positive drugs were higher than those for negative drugs with the same octanol/water partitioning or the same Ks on egg yolk phospholipid bilayers. Electrostatic interactions seem to be important for the partitioning of charged drugs into brush border membranes.
Engvall
Caroline
C
Department of Biochemistry, Biomedical Center, Uppsala University, Box 576, SE-751 23 Uppsala, Sweden. caroline.engvall@biokem.uu.se
Lundahl
Per
P
D000042:Absorption; D000818:Animals; D015415:Biomarkers; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002845:Chromatography; D066298:In Vitro Techniques; D007422:Intestines / Q000737:chemistry*; D007700:Kinetics; D008055:Lipids / Q000737:chemistry; D008081:Liposomes; D008566:Membranes / Q000737:chemistry; D008871:Microvilli / Q000737:chemistry*; D000442:Octanols; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D010743:Phospholipids / Q000737:chemistry; D012995:Solubility; D012996:Solutions; D013552:Swine
D015415:Biomarkers; D008055:Lipids; D008081:Liposomes; D000442:Octanols; D004364:Pharmaceutical Preparations; D010743:Phospholipids; D012996:Solutions