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强心甾类化合物的亲脂性与肠吸收(作者译)

[Lipophilicity and enteral absorption of cardenolides (author's transl)].

作者信息

Hempelmann F W, Heinz N, Flasch H

出版信息

Arzneimittelforschung. 1978;28(12):2182-5.

PMID:582927
Abstract

Intestinal absorption of 15 cardenolides has been examined in cats. The 3H-labelled substances were injected intraluminally into ligated duodenal loops of anaesthetized animals. 3H-Concentrations were followed in the portal circulation and in the bile. 1 h after drug administration the duodenal sac was removed, and the residual in the lumen then was washed out and assayed radiochemically. The decrease of radioactivity during 1 h was calculated as extent of absorption (QR). Cardenolide absorption was compared with the corresponding in vitro parameters of lipophilicity like octanol/water partition coefficients and Rm values from reversed phase thin-layer chromatography. The Spearman rank sum correlation test revealed coefficients of 0.95 to 0.97. The result lends support to the use of the easily available Rm values as a good tool to predict intestinal absorption of various cardenolides.

摘要

已在猫身上研究了15种强心苷的肠道吸收情况。将3H标记的物质经肠腔注入麻醉动物结扎的十二指肠肠袢中。监测门静脉循环和胆汁中的3H浓度。给药1小时后,取出十二指肠囊,冲洗肠腔内的残留物并进行放射化学分析。计算1小时内放射性的降低作为吸收程度(QR)。将强心苷的吸收与相应的亲脂性体外参数如正辛醇/水分配系数和反相薄层色谱的Rm值进行比较。Spearman秩和相关检验显示系数为0.95至0.97。该结果支持将易于获得的Rm值用作预测各种强心苷肠道吸收的良好工具。

相似文献

1
[Lipophilicity and enteral absorption of cardenolides (author's transl)].强心甾类化合物的亲脂性与肠吸收(作者译)
Arzneimittelforschung. 1978;28(12):2182-5.
2
[Partition coefficients and Rm-values of cardenolides (author's transl)].强心甾类化合物的分配系数和比移值(作者译)
Arzneimittelforschung. 1978;28(12):2179-82.
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[Lipophilicity-protein binding relationship in cardenolides (author's transl)].强心苷中亲脂性与蛋白结合的关系(作者译)
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Relationship between the inotropy speeds in guinea-pig myocardium and lipophilic character of cardenolides and ericaceous toxins.豚鼠心肌收缩性速度与强心甾类化合物和杜鹃花毒素亲脂性之间的关系。
Jpn J Pharmacol. 1984 Oct;36(2):205-15. doi: 10.1254/jjp.36.205.
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[Synthesis and characterization of some cardenolide glucuronides and sulphates (author's transl)].某些强心苷葡萄糖醛酸苷和硫酸盐的合成与表征(作者译)
Arzneimittelforschung. 1977;27(3):642-9.
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A quantitative concept of the mechanism of intestinal lymphatic transfer of lipophilic molecules.
Pharm Res. 1994 Apr;11(4):508-12. doi: 10.1023/a:1018954213469.
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[ABSORPTION AND DEGRADATION OF CARDIAC GLYCOSIDES. 3. CHEMICAL DETERMINATION OF ENTERAL ABSORPTION OF CARDENOLIDE GLYCOSIDES IN CATS].[强心苷的吸收与降解。3. 猫体内强心甾糖苷肠吸收的化学测定]
Arzneimittelforschung. 1963 Sep;13:764-7.
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Rm values of steroids as an expression of their lipophilic character in structure-activity studies.在构效关系研究中,甾体类化合物的分配系数(Rm值)作为其亲脂性特征的一种表达。
J Med Chem. 1975 Sep;18(9):873-83. doi: 10.1021/jm00243a003.
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Gastrointestinal absorption of the strongly acidic drug proxicromil.强酸性药物丙酰半胱氨酸的胃肠道吸收。
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[Estimation of the effects of cardenolides. 1. Relation between molecular physical parameters and parameters of action of cardenolides].[强心甾类化合物作用的评估。1. 分子物理参数与强心甾类化合物作用参数之间的关系]
Pharmazie. 1984 Mar;39(3):173-6.

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