Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrug / 药学学报
Acta Pharmaceutica Sinica
; (12): 627-630, 2003.
Article
en Zh
| WPRIM
| ID: wpr-266621
Biblioteca responsable:
WPRO
ABSTRACT
<p><b>AIM</b>To study the in vivo distribution of N-acetyl-L-glutamic prednisolone (ACEP) and to investigate the renal targeting characteristics of the prodrug.</p><p><b>METHODS</b>The 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.</p><p><b>RESULTS</b>The 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.</p><p><b>CONCLUSION</b>Compared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n = 5, P < 0.001).</p>
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Índice:
WPRIM
Asunto principal:
Prednisolona
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Farmacocinética
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Profármacos
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Absorciometría de Fotón
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Densidad Ósea
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Sistemas de Liberación de Medicamentos
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Ratas Wistar
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Riñón
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Metabolismo
Límite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2003
Tipo del documento:
Article