Absorption and Elimination of Cyclodextrin Derivatives by Rabbits and Rats

Summary

The intestinal absorption, digestibility by the colon bacterial flora and urinary elimination of the β-cyclodextrin and its methylated derivatives were studied. The in vitro absorption of the methylated derivatives of cyclodextrin proved to be slow, and could not be inhibited by phloretin. The absorption is concentration dependent, and shows no saturation limit. The results point to a passive transport mechanism. The β-cyclodextrin and its methylated derivative could be digested by a culture of colonic symbionts. The results render quite probable that these compounds may be converted into glucose by the colon bacteria. Following oral administration the urinary elimination was rather low, while following the intramuscular injection the heptakis(2,6-di-0-methyl)-β -cyclodextrin was excreted from the organism quantitatively in 24 hours. The plasma concentration of intravenously injected heptekis-(2,6-di-0-methyl)-β -cyclodextrin decreased abruptly in 1–2 hours, and after 6 hours, it could be detected in blood plasma only in traces.