EFFECT OF POLYSORBATE 80 ON SOLUBILITY AND IN VIVO AVAILABILITY OF 2-BUTYL-3-BENZOFURANYL 4-[2-(DIETHYLAMINO)ETHOXY]-3,5-DIIODOPHENYL KETONE HYDROCHLORIDE (SKANDF 33134-A)

被引:25
作者
RAVIN, LJ
SHAMI, EG
INTOCCIA, A
RATTIE, E
JOSEPH, G
机构
[1] Research and Development Division of Smith Kline & French Laboratories, Philadelphia, Pennsylvania
关键词
2‐Butyl‐3‐benzofuranyl 4‐[2‐(diethylamino) ethoxy]‐3,5‐diiodophenyl ketone hydrochloride (SK&F 33134‐A), [!sup]14[!/sup]C‐ labeled–solubility, availability; Biliary; urinary excretion–SK&F 33134‐A‐[!sup]14[!/sup]C; Polysorbate 80 effect–SK&F 33134‐A‐[!sup]14[!/sup]C solubility; in vivo availability; Scintillometry–analysis;
D O I
10.1002/jps.2600581018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 vivo 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. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company
引用
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页码:1242 / &
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