Effect of polysorbate 80 on the solubility and in vivo availability of 2-butyl-3-benzofuranyl 4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl ketone hydrochloride (SK&F 33134-a)

✍ Scribed by Louis J. Ravin; Elie G. Shami; Alfred Intoccia; Elisabeth Rattie; Gerald Joseph

• Publisher: John Wiley and Sons
• Year: 1969
• Tongue: English
• Weight: 425 KB
• Volume: 58
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600581018

✦ Synopsis

Polysorbate 80 has been shown to have a significant effect on the solubility of 2-butyl-3-benzofuranyl 4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl ketone hydrochloride (SK&F 33134-A). Subsequent in uiuo studies in bile-cannulated rats with SK&F 33134-A-14C indicated that the drug was better absorbed when it was solubilized with polysorbate 80. Biliary excretion served as an index of absorption of orally administered drug in the rat. A twofold increase in the amount of drug excreted through the bile was observed for the solubilized form. The data also suggest that urinary excretion measurements should not be used to indicate the degree of absorption of this drug in the rat.

Keyphrases 0 2-Butyl-3-benzofuranyl 4-[2-(diethylamino) ethoxyl-3,5-diiodophenyl ketone hydrochloride (SK & F 33 134-A), laclabeled-solubility, availability 0 Polysorbate 80 effect-SK& F 33134-A-14C solubility, in uiuo availability 0 Biliary, urinary excretion-SKCt F 33134-A-14C 0 Scintillometry-analysis