Tozaki H, Emi Y, Horisaka E, Fujita T, Yamamoto A, Muranishi S
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.
Biol Pharm Bull. 1995 Jun;18(6):929-31. doi: 10.1248/bpb.18.929.
The metabolism of insulin and calcitonin by microorganisms was examined in rat cecal contents. Both insulin and calcitonin were markedly degraded. Calcitonin was more susceptible to proteolysis in rat cecal contents than insulin. Calcitonin was also rapidly degraded in supernatant, while we found few degradation products of insulin. These findings suggest that care should be taken to metabolize the peptide drugs by microorganisms when they are administered to the large intestine for colon-specific drug delivery.
在大鼠盲肠内容物中检测了微生物对胰岛素和降钙素的代谢情况。胰岛素和降钙素均被显著降解。在大鼠盲肠内容物中，降钙素比胰岛素更易受到蛋白水解作用的影响。降钙素在上清液中也迅速降解，而我们发现胰岛素的降解产物很少。这些发现表明，当将肽类药物用于结肠特异性给药而投放到大肠时，应注意微生物对其的代谢作用。
