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阳离子型聚丙烯酸树脂®聚合物作为通过溶剂蒸发法制备的微粒的辅料。

Cationic Eudragit® polymers as excipients for microparticles prepared by solvent evaporation method.

作者信息

Vysloužil Jakub, Bavoľárová Jana, Kejdušová Martina, Vetchý David, Dvořáčková Kateřina

出版信息

Ceska Slov Farm. 2013 Dec;62(6):249-54.

Abstract

Three cationic acrylic polymers, i. e. Eudragit® RL, Eudragit® RS and Eudragit® E 100, were evaluated for the purpose of microparticles preparation by the solvent evaporation method. The practically insoluble drug mirtazapine and the freely soluble drug tramadol hydrochloride were selected for encapsulation as extreme limits of drug solubility. The prepared microspheres were analyzed by optical microscopy, drug content analysis and dissolution test. It was observed that Eudragit® RL did not provide microparticles while Eudragit® RS and Eudragit® E 100 yielded spherical microparticles. Samples prepared with mirtazapine showed sustained drug release whereas tramadol hydrochloride samples released the drug in a pattern similar to the immediate release profile. Eudragit® RS was found to be superior to Eudragit® E 100 in its encapsulation efficiency, drug loading and smaller mean size of microparticles.

摘要

为了通过溶剂蒸发法制备微粒,对三种阳离子丙烯酸聚合物,即尤特奇® RL、尤特奇® RS和尤特奇® E 100进行了评估。选择几乎不溶的药物米氮平以及易溶的药物盐酸曲马多作为药物溶解度的极限进行包封。通过光学显微镜、药物含量分析和溶出试验对制备的微球进行分析。观察到尤特奇® RL未形成微粒,而尤特奇® RS和尤特奇® E 100产生了球形微粒。用米氮平制备的样品显示出药物的持续释放,而盐酸曲马多样品以类似于速释曲线的模式释放药物。发现尤特奇® RS在包封效率、载药量和较小的微粒平均尺寸方面优于尤特奇® E 100。

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