Studies on the possible absorption of a sulphated glycopeptide (GLPS) in relation to its mode of action

Abstract

The absorption of an acute dose of glycopeptide sulphate, GLPS, has been studied in free-ranging rats, in rats and dogs after suppression of the gut microflora, in rats with histamine-induced gastric ulcers and in two human subjects, using tracer techniques. Unchanged GLPS is unabsorbed from the mammalian gut and ulcer lesions do not diminish the barrier against the ingress of drug into vascular circulation; differences in faecal excretion rates are readily explicable in terms of the suppression of the gut micro-flora in the antibiotic treated animals and the correspondingly uncomplicated passage of unchanged GLPS through the gut. The intestinal microflora does not bring about systematic degradation of GLPS, and the low proportion of sulphate hydrolysis, which occurs in the lumen of antibiotic treated and untreated animals, and which accounts for the excretion from the body of SO 4 2− and small organic sulphates, is compatible with that produced, for example, by dialysis in vitro. Available evidence suggests that GLPS may inhibit the inflammatory process by exerting a stabilizing effect on the cell membrane and adjacent small vessels.