Relationship between drug absorption enhancing activity and membrane perturbing effects of acylcarnitines.

摘要: Acylcarnitines with chain lengths of 2 to 18 carbon atoms were tested for their effects on rat intestinal brush border membrane order (S) by fluorescence polarization 1,6-diphenyl-l ,3,5-hexatriene (DPH). These results compared the previously reported effectiveness acylcarnitines as absorption enhancers poorly absorbed antibiotic cefoxitin. fatty acids less than 12 units in length ineffective increasing drug and perturbing order. Long-chain (12–18 carbons) significantly increased bioavailability cefoxitin decreased lipid membranes. The suggest that, promote absorption, must surpass a critical (10 units) partition effectively into and, addition, perturb beyond threshold value (15–20%). Membrane capacity may serve an indicator enhancing potential other aliphatic-type compounds.