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壳聚糖与尤特奇L100和尤特奇L100-55形成的聚电解质复合物作为口服控释药物潜在载体的比较评价

Comparative evaluation of interpolyelectrolyte complexes of chitosan with Eudragit L100 and Eudragit L100-55 as potential carriers for oral controlled drug delivery.

作者信息

Moustafine Rouslan I, Margulis Evgeniya B, Sibgatullina Liliya F, Kemenova Vera A, Van den Mooter Guy

机构信息

Department of Pharmaceutical, Toxicological and Analytical Chemistry, State Medical University of Kazan, Tatarstan, Russian Federation.

出版信息

Eur J Pharm Biopharm. 2008 Sep;70(1):215-25. doi: 10.1016/j.ejpb.2008.04.008. Epub 2008 Apr 22.

Abstract

With a view to the application in oral controlled drug delivery systems, the formation of interpolyelectrolyte complexes (IPEC) between chitosan (CS) and Eudragit L100 (L100) or Eudragit L100-55 (L100-55) was investigated at pH 6.0, using elementary analysis. The interaction or binding ratio of a unit molecule of CS with Eudragit L copolymers depends on the molecular weight of CS, and changes from 1:0.85 to 1:1.22 (1.17<phi<0.82) for L100 and from 1:1.69 to 1:1.26 (0.60<phi<0.79) for L100-55, respectively. Based on the results of FT-IR, the structure of the IPECs can change substantially as a function of pH (from 5.8 till 7.4). Swelling behavior of physical mixtures (PM) is definitely different, and potential interactions between the two polyelectrolytes were not observed. The release of the model drug diclofenac sodium (DS) was significantly delayed from tablets made up of the IPEC and can be modified by two ways: choosing Eudragit L copolymer types and/or changing the molecular weight of CS in the IPECs composition.

摘要

为了应用于口服控释给药系统,在pH 6.0条件下,采用元素分析方法研究了壳聚糖(CS)与丙烯酸树脂L100(L100)或丙烯酸树脂L100-55(L100-55)之间形成的聚电解质络合物(IPEC)。CS的一个单位分子与丙烯酸树脂L共聚物的相互作用或结合比取决于CS的分子量,对于L100,该比值从1:0.85变化到1:1.22(1.17<φ<0.82),对于L100-55,该比值分别从1:1.69变化到1:1.26(0.60<φ<0.79)。基于傅里叶变换红外光谱(FT-IR)的结果,IPEC的结构会随pH值(从5.8到7.4)发生显著变化。物理混合物(PM)的溶胀行为明显不同,且未观察到两种聚电解质之间的潜在相互作用。由IPEC制成的片剂中模型药物双氯芬酸钠(DS)的释放明显延迟,并且可以通过两种方式进行调节:选择丙烯酸树脂L共聚物类型和/或改变IPEC组成中CS的分子量。

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