Characterization of the mechanism of interaction in ibuprofen-Eudragit RL100® coevaporates

被引:20
作者
Pignatello, R
Spadaro, D
Vandelli, MA
Forni, F
Puglisi, G
机构
[1] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy
[2] Univ Modena & Reggio Emilia, Dipartimento Sci Farmaceut, Modena, Italy
关键词
ibuprofen; Eudragit; bioavailability; coevaporates; solid dispersion;
D O I
10.1081/DDC-120030421
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The present study is a preliminary exploration of the affinity between a carboxylic model drug, the nonsteroidal anti inflammatory agent ibuprofen (IBU) and Eudragit RL100 (RL) polymer. Due to the presence of a variable amount of quaternary ammonium groups in this matrix, physical and chemical interaction with the carboxylic drug can occur, which reinforces its scant mechanical dispersion in the polymer network and can ultimately affect its release profile in vitro and in vivo. To study these aspects, IBU was mixed at increasing weight ratios and in different chemical forms (free acid, sodium salt, and n-butyl ester), to investigate further the role of the carboxylic group in the interaction with the RL polymer. Therefore, IBU-RL solid dispersions (coevaporates) were obtained and fully characterized in the solid state through spectroscopic, calorimetric, and x-ray diffractometric analyses. The in vitro release pattern of the drug, in the different chemical states, was studied for the coevaporates, compared with drug-RL physical mixtures, along with drug adsorption profiles from aqueous solutions on the surface of the polymer granules.
引用
收藏
页码:277 / 288
页数:12
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