Gordijo Cláudia R, Barbosa César A S, Da Costa Ferreira Ana M, Constantino Vera R L, de Oliveira Silva Denise
Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, CP 26077, CEP 05513-900, São Paulo, SP, Brazil.
J Pharm Sci. 2005 May;94(5):1135-48. doi: 10.1002/jps.20336.
The immobilization of the NSAID ibuprofen (Hibp) and the Cu(II)-ibp compound on magnesium-aluminum layered double hydroxides (Mg3Al-LDH) is described. Ibuprofen was intercalated on LDHs by three routes (ion exchange, co-precipitation, and reconstruction). The organic drug and the Cu(II)-ibp were also immobilized by adsorption on LDH external surfaces. Materials were characterized by elemental analysis, UV/VIS, FTIR, and Raman spectroscopies, powder X-ray diffractometry (XRD), thermogravimetry, and electronic paramagnetic resonance (EPR). Mg3Al-(ibp)(cop) (30% w/w of drug/material) and Mg3Al-(ibp)(ie) (33%) materials exhibit bilayer arrangements of ibp anions intercalated between the host layers. Mg3Al-(ibp)(rec) and Mg3Al-(ibp)(ads) contain 13% and 6.2% of ibuprofenate, respectively. Mg3Al-(Cu-ibp)(ads) exhibits two Cu centers in different environments interacting with host layers. Pharmacological potential of materials are compared considering the amounts of immobilized drugs and their buffering properties. Mg3Al-(ibp)(ie) and Mg3Al-(ibp)(cop) exhibit poor buffering property, but contain high ibp amounts. Mg3Al-(ibp)(ads) despite having buffering property, contains low amount of ibuprofen. Mg3Al-(ibp)(rec) combines significant amount of immobilized ibp with good buffering property. Mg3Al-(Cu-ibp)(ads), due to the buffering property, may be an interesting new formulation aiming to decrease gastric irritation.
本文描述了非甾体抗炎药布洛芬(Hibp)和铜(II)-布洛芬化合物在镁铝层状双氢氧化物(Mg3Al-LDH)上的固定化。布洛芬通过三种途径(离子交换、共沉淀和重构)插层到层状双氢氧化物中。有机药物和铜(II)-布洛芬也通过吸附固定在层状双氢氧化物的外表面。通过元素分析、紫外/可见光谱、傅里叶变换红外光谱、拉曼光谱、粉末X射线衍射(XRD)、热重分析和电子顺磁共振(EPR)对材料进行了表征。Mg3Al-(ibp)(cop)(药物/材料质量比为30%)和Mg3Al-(ibp)(ie)(33%)材料在主体层之间呈现出插层的ibp阴离子双层排列。Mg3Al-(ibp)(rec)和Mg3Al-(ibp)(ads)分别含有13%和6.2%的布洛芬盐。Mg3Al-(Cu-ibp)(ads)在不同环境中表现出两个与主体层相互作用的铜中心。考虑到固定化药物的量及其缓冲性能,对材料的药理潜力进行了比较。Mg3Al-(ibp)(ie)和Mg3Al-(ibp)(cop)缓冲性能较差,但含有大量的ibp。Mg3Al-(ibp)(ads)尽管具有缓冲性能,但布洛芬含量较低。Mg3Al-(ibp)(rec)结合了大量固定化的ibp和良好的缓冲性能。Mg3Al-(Cu-ibp)(ads)由于具有缓冲性能,可能是一种旨在减少胃部刺激的新型有趣制剂。