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Titolo:
CONTROL OF PLASMA CHOLESTEROL-LOWERING ACTION OF PROBUCOL WITH VARIOUS LIPID CARRIER SYSTEMS
Autore:
TAKINO T; KOREEDA N; NOMURA T; SAKAEDA T; YAMASHITA F; TAKAKURA Y; HASHIDA M;
Indirizzi:
KYOTO UNIV,GRAD SCH PHARMACEUT SCI,DEPT DRUG DELIVERY RES,SAKYO KU,YOSHIDA SHIMOADUCHI CHO KYOTO 6068501 JAPAN KYOTO UNIV,GRAD SCH PHARMACEUT SCI,DEPT DRUG DELIVERY RES,SAKYO KU KYOTO 6068501 JAPAN SHIONOGI & CO LTD,SHIONOGI RES LABS,FUKUSHIMA KU OSAKA 5530002 JAPAN
Titolo Testata:
Biological & pharmaceutical bulletin
fascicolo: 5, volume: 21, anno: 1998,
pagine: 492 - 497
SICI:
0918-6158(1998)21:5<492:COPCAO>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
DELIVERY SYSTEMS; LIPOPHILIC DRUGS; DISPOSITION; SERUM;
Keywords:
PROBUCOL; BIODISTRIBUTION CONTROL; CHOLESTEROL-LOWERING ACTION; LIPID CARRIER SYSTEM; POLYOXYETHYLENE HYDROGENATED CASTOR OIL (HCO-60) MICELLE; O/W EMULSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
T. Takino et al., "CONTROL OF PLASMA CHOLESTEROL-LOWERING ACTION OF PROBUCOL WITH VARIOUS LIPID CARRIER SYSTEMS", Biological & pharmaceutical bulletin, 21(5), 1998, pp. 492-497

Abstract

In order to explore the relationship between the pharmacokinetic properties and pharmacological actions of lipophilic drugs injected with lipid carrier systems, probucol as selected as a model drug with high lipophilicity, and the effect of disposition control on cholesterol-lowering activities was evaluated. Both large emulsion, with mean diameter of 280 nm, and long-circulating type small emulsion containing egg sphingomyelin with mean diameter of 100 nm, showed stable incorporationof probucol. The former produced rapid accumulation of probucol in the liver, while the latter demonstrated prolonged systemic circulation and gradual hepatic uptake. On the other hand, inject-ion of a micellasolution with HCO-60 (polyoxyethylene hydrogenated castor oh) showed a rapid decrease in plasma concentration and a high hepatic uptake of probucol, similar to injections with serum, suggesting the rapid release of the drug from the micelles, However, probucol in a micellar solution showed higher cholesterol-lowering action than that in emulsion formulations. These results suggested that the pharmacological action of probucol in the liver might be affected by the uptake mode and sequential disposition in the organ, depending on the drug retention properties of the lipid carrier particles.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 16:03:54