Involvement of intestinal P-glycoprotein in the restricted absorption of methylprednisolone from rat small intestine.

Involvement of intestinal P-glycoprotein in the restricted absorption of methylprednisolone from rat small intestine.
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肠P-糖蛋白参与限制大鼠小肠吸收甲泼尼龙。

DOI:
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发表时间:
1998
期刊:
Journal of Pharmacy and Science
影响因子:
--
通讯作者:
M. Takada
M. Takada
中科院分区:
--
文献类型:
--
作者:
H. Saitoh;M. Hatakeyama;O. Eguchi;M. Oda;M. Takada

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采用大鼠在体小肠吸收实验研究了甾体激素与小肠P-糖蛋白的相互作用。泼尼松龙和氢化可的松从整个小肠迅速吸收。相反,甲泼尼龙吸收显着延迟空肠和回肠的肠道外排系统。在维拉帕米和奎尼丁的存在下,甲基强的松龙的延迟吸收完全恢复,这表明P-糖蛋白是负责甲基强的松龙吸收的独特功能。肠P-糖蛋白底物的一个必要条件似乎是类固醇结构中的6 α-甲基。肠P-糖蛋白对类固醇激素的底物特异性部分不同于肾上腺等其他组织。所有三种类固醇激素在大鼠小肠粘膜匀浆上清液中几乎没有消失,表明这些类固醇激素的肠代谢相对较小。
The interaction between steroid hormones and intestinal P-glycoprotein was investigated by measuring intestinal absorption from rat small intestine in situ. Prednisolone and hydrocortisone were rapidly absorbed from the entire small intestine. In contrast, methylprednisolone absorption was significantly retarded in jejunum and ileum by an intestinal efflux system. In the presence of verapamil an quinidine, the retarded absorption of methylprednisolone was completely recovered, suggesting that P-glycoprotein is responsible for the unique features of methylprednisolone absorption. A requisite for the substrate of intestinal P-glycoprotein seemed to be 6 alpha-methyl group in the steroid structure. Substrate specificity of intestinal P-glycoprotein to steroid hormones was shown to be in part different from those in other tissues such as adrenal gland. Little of all three steroid hormones disappeared in the supernatant of mucosal homogenate from rat small intestine, indicating that intestinal metabolism of these steroid hormones was relatively small.
DOI: --
发表时间: 1990-09
影响因子: 21.1
作者:
J. M. Ford;W. Hait
通讯作者: J. M. Ford;W. Hait
甲基强的松龙及其琥珀酸钠前药在体内和大鼠灌注肝脏中的处置:非线性和顺序首过消除。
DOI: 10.1002/jps.2600800502
发表时间: 1991
影响因子: 3.8
作者:
Kong,AN;Jusko,WJ
通讯作者: Jusko,WJ
DOI: 10.1016/0016-5085(92)90173-v
发表时间: 1992
期刊: Gastroenterology
影响因子: 29.4
作者:
Hsing,S;Gatmaitan,Z;Arias,IM
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