Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrug.
- Author:
Min SU
1
;
Qin HE
;
Zhi-rong ZHANG
;
Bin HU
;
Shi-wei LIU
Author Information
- Publication Type:Journal Article
- MeSH: Absorptiometry, Photon; Animals; Bone Density; drug effects; Drug Delivery Systems; Female; Kidney; metabolism; Male; Mice; Prednisolone; metabolism; pharmacokinetics; Prodrugs; metabolism; pharmacokinetics; Rats; Rats, Wistar
- From: Acta Pharmaceutica Sinica 2003;38(8):627-630
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo study the in vivo distribution of N-acetyl-L-glutamic prednisolone (ACEP) and to investigate the renal targeting characteristics of the prodrug.
METHODSThe concentrations of prednisolone in organs at predetermined time were assayed by HPLC after intravenous administration of ACEP or prednisolone to Kunming mice. The adverse effects were evaluated by testing the bone mineral densities (BMD) of Wistar rats.
RESULTSThe concentrations of prednisolone in kidney 15 min after i.v. administration were (86 +/- 8) microgram.g-1 for ACEP group, (57 +/- 4) microgram.g-1 for prednisolone group; 60 min after i.v. administration were (67 +/- 5) microgram.g-1 for ACEP group, (42 +/- 4) microgram.g-1 for prednisolone group. BMDs were (0.08 +/- 0.03) g.cm-2 and (0.14 +/- 0.06) g.cm-2 for prednisolone and ACEP-treated Wistar rats respectively.
CONCLUSIONCompared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n = 5, P < 0.001).
