[Study on the enzyme dependant colon targeting prodrug--dexamethasone succinate dextran and its tablets].
OBJECTIVE
To develop an orally administered colon targeting drug delivery system dexamethasone succinate dextran (DSD) tablets.


METHODS
Dexamethasone succinate dextran was synthesized in an anhydrous environment. Using 4-dimethyl aminopyridine and 1,1'-carbonyldiimidazole as the catalyzer. The chemical structure was identified by UV, IR, NMR and MS. The contents of dexamethasone in various samples were determined by HPLC.


RESULTS
Dexamethasone was distributed mainly in plasma and gastric contents after the oral administration of common tablets. In contrast, after oral administration of DSD tablets, the recovery of dexamethasone in plasma and gastric contents decreased significantly, while the percentage of dexamethasone in cecum and colon increased obviously.


CONCLUSIONS
The experimental results showed the good colon targeting property of DSD prodrug compared with free dexamethasone.
Pang
Y N
YN
West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Zhang
Z R
ZR
Pang
Q J
QJ
Li
T L
TL
D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D002432:Cecum / Q000378:metabolism; D003106:Colon / Q000378:metabolism*; D003907:Dexamethasone / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D003911:Dextrans / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D008297:Male; D011355:Prodrugs; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D013607:Tablets
D000893:Anti-Inflammatory Agents; D003911:Dextrans; D011355:Prodrugs; D013607:Tablets; C481153:dexamethasone succinate dextran; D003907:Dexamethasone