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Titolo:
PHARMACOKINETICS OF SDZ-64-412, A NOVEL ANTIASTHMATIC AGENT, FOLLOWING INTRAVENOUS, ORAL, AND INHALATION DOSING IN THE RAT
Autore:
CHARNICK SB; YU ZL; ATHILL LV; KARARA AH; TSE FLS; LAU DTW;
Indirizzi:
SANDOZ INC,RES INST,DEPT DRUG METAB & PHARMACOKINET E HANOVER NJ 07936 SANDOZ INC,RES INST,DEPT DRUG METAB & PHARMACOKINET E HANOVER NJ 07936 SANDOZ INC,RES INST,DEPT CLIN PHARMACOL E HANOVER NJ 07936
Titolo Testata:
Biopharmaceutics & drug disposition
fascicolo: 4, volume: 15, anno: 1994,
pagine: 317 - 327
SICI:
0142-2782(1994)15:4<317:POSANA>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
PAF;
Keywords:
ABSORPTION; INHALATION; PHARMACOKINETICS; DECONVOLUTION; ASTHMA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
12
Recensione:
Indirizzi per estratti:
Citazione:
S.B. Charnick et al., "PHARMACOKINETICS OF SDZ-64-412, A NOVEL ANTIASTHMATIC AGENT, FOLLOWING INTRAVENOUS, ORAL, AND INHALATION DOSING IN THE RAT", Biopharmaceutics & drug disposition, 15(4), 1994, pp. 317-327

Abstract

The pharmacokinetics of SDZ 64-412, an antiasthmatic agent, were investigated following intravenous, oral, and inhalation dosing in rats. C-14-SDZ 64-412 was administered intravenously (2.75 mg kg(-1)) and orally (5.5 mg kg(-1), 110 mg kg(-1)), whereas non-radiolabeled drug (5.04 mg kg(-1)) was-administered using nose-only inhalation chambers. Radioactivity and parent drug concentrations in blood, lung, and excreta were determined at designated times post-dose. SDZ 64-412 was rapidly and extensively (similar to 80%) absorbed following both oral doses, although absorption appeared to be prolonged with increasing dose. The absorbed drug was shown to undergo extensive and saturable first-pass metabolism. The bioavailability of the parent drug, calculated by dose-normalized AUC and deconvolution methods, was only 10-15% from the low dose, but increased to similar to 40% following the high dose. Following inhalation dosing, SDZ 64-412 concentrations in blood and lungs increased rapidly, and did nor decline immediately after termination ofdosing. The inhalation dose yielded a bioavailability of similar to 40%, and AUC of the drug in lungs was approximately 25 times greater than in blood. In general, SDZ 64-412 was extensively distributed and rapidly eliminated from the systemic circulation. Biliary excretion was the predominant route of radioactivity excretion. The present findingssuggest that inhalation administration provides a viable means of delivery of SDZ 64-412.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 19:16:45