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结肠特异性给药系统的体内评价:大鼠体内偶氮聚合物包衣胶囊中茶碱的吸收研究。

In vivo evaluation of a colon-specific drug delivery system: an absorption study of theophylline from capsules coated with azo polymers in rats.

作者信息

Van den Mooter G, Samyn C, Kinget R

机构信息

Lab. Galenische en Klinische farmacie, K. U. Leuven, Belgium.

出版信息

Pharm Res. 1995 Feb;12(2):244-7. doi: 10.1023/a:1016283027139.

Abstract

Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from capsules coated with the azo polymers was examined in the proximal part of the small intestine and the cecum of male Wistar rats. The capsules were surgically inserted in the region of interest. The plasma concentration of the drug was higher when the capsules were inserted in the cecum as compared to the small intestine. The appearance of theophylline in the plasma when capsules were administered in the small intestine can be attributed to simple diffusion of the drug through the swollen polymer coating. Release and absorption from the cecum is the combined results of diffusion and degradation of the azo polymer coatings by bacterial azo reductase.

摘要

以甲基丙烯酸2-羟乙酯、甲基丙烯酸甲酯和甲基丙烯酸为基础,并含有N,N'-双[(甲基丙烯酰氧基乙基)氧基(羰基氨基)]偶氮苯作为偶氮芳香剂的偶氮聚合物,作为结肠特异性药物递送的包衣进行了体内评估。在雄性Wistar大鼠的小肠近端和盲肠中,研究了用偶氮聚合物包衣的胶囊中茶碱的胃肠道吸收情况。通过手术将胶囊插入感兴趣的区域。与小肠相比,当胶囊插入盲肠时,药物的血浆浓度更高。当在小肠中给药胶囊时,血浆中茶碱的出现可归因于药物通过肿胀的聚合物包衣的简单扩散。从盲肠的释放和吸收是偶氮聚合物包衣被细菌偶氮还原酶扩散和降解的综合结果。

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