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Titolo:
Biotransformation in vitro of the 22R and 22S epimers of budesonide by human liver, bronchus, colonic mucosa and skin
Autore:
Cortijo, J; Urbieta, E; Bort, R; Castell, JV; Ruiz-Bravo, C; Martinez, J; Palacios-Pelaez, R; Lledo, S; Morcillo, EJ;
Indirizzi:
Univ Valencia, Fac Med & Odontol, Dept Pharmacol, Valencia, Spain Univ Valencia Valencia Spain & Odontol, Dept Pharmacol, Valencia, Spain Univ Valencia, Fac Med & Odontol, Dept Biochem & Mol Biol, Valencia, SpainUniv Valencia Valencia Spain , Dept Biochem & Mol Biol, Valencia, Spain Univ Valencia, Fac Med & Odontol, Dept Surg, Valencia, Spain Univ Valencia Valencia Spain Med & Odontol, Dept Surg, Valencia, Spain Univ Valencia, Hosp La Fe, Res Ctr, Unit Expt Hepatol, Valencia, Spain Univ Valencia Valencia Spain es Ctr, Unit Expt Hepatol, Valencia, Spain Ifidesa Aristegui Pharmaceut & Special Ind, Madrid, Spain Ifidesa Aristegui Pharmaceut & Special Ind Madrid Spain , Madrid, Spain Univ Valencia, Univ Clin Hosp, Surg Serv, Valencia, Spain Univ Valencia Valencia Spain Univ Clin Hosp, Surg Serv, Valencia, Spain
Titolo Testata:
FUNDAMENTAL & CLINICAL PHARMACOLOGY
fascicolo: 1, volume: 15, anno: 2001,
pagine: 47 - 54
SICI:
0767-3981(200102)15:1<47:BIVOT2>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
STEREOSELECTIVE SULFATE CONJUGATION; GLUCOCORTICOID BUDESONIDE; EPITHELIAL-CELLS; METABOLISM; LUNG; SULFOTRANSFERASE; TISSUE; IDENTIFICATION; HEPATOCYTES; SALBUTAMOL;
Keywords:
biotransformation; budesonide; epimer; human; in vitro;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Cortijo, J Univ Valencia, Fac Med & Odontol, Dept Pharmacol, Valencia, Spain Univ Valencia Valencia Spain Dept Pharmacol, Valencia, Spain
Citazione:
J. Cortijo et al., "Biotransformation in vitro of the 22R and 22S epimers of budesonide by human liver, bronchus, colonic mucosa and skin", FUN CL PHAR, 15(1), 2001, pp. 47-54

Abstract

The pharmacological effects of glucocorticoids are greatly influenced by their pharmacokinetic properties. In the present report, the in vitro biotransformation of the 22R and 22S epimers of the topical steroid budesonide was studied in the S-9 fraction of human liver, bronchus, skin and colonic mucosa. The disappearance of unchanged epimers of budesonide was measured during 90 min of incubation by high performance liquid chromatography. The rate of disappearance was high in human liver while little biotransformation occurred in bronchial tissue and colonic mucosa, and none was detected in the skin, A marked decay of the initial concentration of unchanged budesonide epimers was noticed after 2 h incubation in cultured human hepatocytes, while only a small decrease was observed after 24 h incubation in cultured human airway smooth muscle cells and BEAS-2B cells. The 22R epimer of budesonide suffered greater in vitro biotransformation than the 22S epimer in human hepatic, bronchial and colonic tissues. These findings extend those of other studies, and confirm that the high therapeutic ratio of budesonide is due to negligible local biotransformation combined with high level of liver metabolism for locally absorbed budesonide.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 23:58:03