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Titolo:
PHARMACOKINETIC STUDY OF LOPRINONE HYDROCHLORIDE, A NEW CARDIOTONIC AGENT, IN BEAGLE DOGS
Autore:
UEMURA Y; TANAKA S; IDA S; YUZURIHA T;
Indirizzi:
EISAI & CO LTD,TSUKUBA RES LABS,5-1-3 TOKOUDAI TSUKUBA IBARAKI 30026 JAPAN
Titolo Testata:
Journal of Pharmacy and Pharmacology
fascicolo: 12, volume: 45, anno: 1993,
pagine: 1077 - 1081
SICI:
0022-3573(1993)45:12<1077:PSOLHA>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
DRUGS SUBJECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
12
Recensione:
Indirizzi per estratti:
Citazione:
Y. Uemura et al., "PHARMACOKINETIC STUDY OF LOPRINONE HYDROCHLORIDE, A NEW CARDIOTONIC AGENT, IN BEAGLE DOGS", Journal of Pharmacy and Pharmacology, 45(12), 1993, pp. 1077-1081

Abstract

Pharmacokinetic parameters and bioavailability of a new cardiotonic agent, loprinone hydrochloride, in beagle dogs were determined by measuring plasma levels of loprinone after intravenous bolus and oral administration. The plasma half-life after intravenous administration of loprinone varied among individuals over the range 2.65-15.40 h. The bioavailability after oral administration of loprinone as a solution was 37.1%. Effects of enterohepatic circulation on the time-course of plasma levels after intravenous administration of the drug were also studied in bile-duct-cannulated beagle dogs. The amounts of Ioprinone and its glucuronide excreted in bile during 8 h after administration were 25.4 and 8.6% of the dose, respectively, indicating the possibility of enterohepatic circulation. The plasma half-life in bile-duct-cannulatedbeagle dogs was 1.98 h. These results indicate that the variation in the half-life in beagle dogs resulted from enterohepatic circulation and that the true half-life is about 2 h. The relative bioavailability after oral administration of the drug as a powder in a capsule compared with a solution was 95.7%. In addition, the amounts of loprinone andits glucuronide excreted in bile, and the AUC of plasma level after infusion for 30 min into the portal vein in bile-duct-cannulated beagledogs were similar to those after bolus intravenous administration. These results show that the low bioavailability reflects incomplete absorption.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 00:44:19