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Water-soluble quaternary amine polymers as controlled release carriers

机译:水溶性季胺聚合物作为控释载体

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New bioerodible materials, which are noncrosslinked and water-soluble copolymers of quaternary amines, and alkyl (meth) acrylate were synthesized and then bound with anionic drugs (sodium sulfathiazole and diclofenac sodium) to form water-insoluble complexes. Sodium sulfathiazole was bound to the copolymers more strongly than diclofenac sodium. As the quaternary amine content of the copolymer was increased, the degree of binding of diclofenac sodium to the polymer increased (from 79.9 to 96.2%). Compressed tablets were prepared from the drug-polymer complexes, and their release profiles were well described by the dissociation/erosion mechanism. The release rate constant increased with increasing quaternary amine content of the polymer and decreased as longer alkyl methacrylates were used in the copolymer. The release kinetics were also dependent on the structures of the quaternary amines used (trimethylaminoethyl methacrylate chloride, trimethylaminoethyl acrylate chloride, and methacrylamidopropyltrimethylammonium chloride). Drug release from these systems were found to be independent of the ionic strength (0.05-0.2M NaCl) of the release medium. (C) 1998 John Wiley & Sons, Inc. [References: 11]
机译:合成了新的可生物蚀解的材料,它们是季胺的非交联且水溶性的共聚物,以及(甲基)丙烯酸烷基酯,然后与阴离子药物(磺胺噻唑钠和双氯芬酸钠)结合形成不溶于水的复合物。磺胺噻唑钠比双氯芬酸钠更牢固地结合到共聚物上。随着共聚物中季胺含量的增加,双氯芬酸钠与聚合物的结合度增加(从79.9%增至96.2%)。由药物-聚合物复合物制备压制片剂,并且其解离曲线通过解离/侵蚀机理得到了很好的描述。释放速率常数随聚合物中季胺含量的增加而增加,并随着在共聚物中使用更长的甲基丙烯酸烷基酯而降低。释放动力学还取决于所用的季胺的结构(甲基丙烯酸三甲基氨基乙基氯,甲基丙烯酸三甲基氨基乙基氯和甲基丙烯酰胺基丙基三甲基氯化铵)。发现从这些系统释放的药物与释放介质的离子强度(0.05-0.2M NaCl)无关。 (C)1998 John Wiley&Sons,Inc. [参考:11]

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