Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
SK-AND-F 97426-A - A NOVEL BILE-ACID SEQUESTRANT WITH HIGHER AFFINITIES AND SLOWER DISSOCIATION RATES FOR BILE-ACIDS IN-VITRO THAN CHOLESTYRAMINE
Autore:
BENSON GM; ALSTON DR; HICKEY DMB; JAXACHAMIEC AA; WHITTAKER CM; HAYNES C; GLEN A; BLANCHARD S; CRESSWELL SR; SUCKLING KE;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,THE FRYTHE WELWYN GARDEN CIT AL6 9AR HERTS ENGLAND
Titolo Testata:
Journal of pharmaceutical sciences
fascicolo: 1, volume: 86, anno: 1997,
pagine: 76 - 81
SICI:
0022-3549(1997)86:1<76:S9-ANB>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
GASTROINTESTINAL TRANSIT; SMALL-INTESTINE; PROPULSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
G.M. Benson et al., "SK-AND-F 97426-A - A NOVEL BILE-ACID SEQUESTRANT WITH HIGHER AFFINITIES AND SLOWER DISSOCIATION RATES FOR BILE-ACIDS IN-VITRO THAN CHOLESTYRAMINE", Journal of pharmaceutical sciences, 86(1), 1997, pp. 76-81

Abstract

SK&F 97426-A is a novel bile acid sequestrant that is threefold more potent than cholestyramine at increasing bile acid excretion in the hamster, SK&F: 97426-A is a quaternary alkylammonium polymethacrylate that was selected for comparison with cholestyramine in vivo because of its superior in vitro bile acid binding properties. Association, dissociation, affinity, and capacity experiments were performed under physiologically relevant conditions with the most abundant bile acids foundin human bile. The bile acids came to equilibrium with SK&F 97426-A and cholestyramine within similar to 30 min and 6 min, respectively, SK&F 97426-A and cholestyramine had similar capacities for all the bile acids (between 2.5 and 4 mmol/g) and both had similar, very high affinities and slow dissociation rates far the dihydroxy bile acids. However, SK&F 97426-A had much higher affinities for the trihydroxy bile acids glycocholic acid and taurocholic acid than did cholestyramine. Dissociation of glycocholic acid and taurocholic acid from SK&F 97426-A was also much slower (27 and 25%, respectively, dissociated after 60 min) than from cholestyramine (89 and 84%, respectively, dissociated after 60 min). The higher affinities and slower dissociation rates of the trihydroxy bile acids for and from SK&F 97426-A probably account for the increased potency of SK&F 97426-A over cholestyramine in vivo.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 01:05:26