Ambrogi Valeria, Fardella Giuseppe, Grandolini Giuliano, Perioli Luana, Tiralti Maria Cristina
Dipartimento di Chimica e Tecnologia del Farmaco, University of Perugia, Perugia, Italy.
AAPS PharmSciTech. 2002;3(3):E26. doi: 10.1208/pt030326.
The purpose of this study was to investigate whether hydrotalcite is able to intercalate diclofenac, a nonsteroidal anti-inflammatory drug, and release it in a controlled manner. Layered Mg-Al hydrotalcite in the chloride form was used as a host, and the intercalation compound was prepared by Cl-/diclofenac anionic exchange. Drug release from the intercalation compound was performed in vitro in simulated intestinal fluid at pH 7.5 according to USP 24 and in a pH 7.0 solution designed to mimic the ionic conditions of the small intestine. Results from the intercalation process show that hydrotalcite is able to intercalate diclofenac with a simple procedure and with a good drug loading (55% wt/wt). The in vitro drug release was remarkably lower than that from the corresponding physical mixture at both pH 7.5 and pH 7.0. In the latter case, the release was not complete at 24 hours. The kinetic analysis shows the importance of the diffusion through the particle in controlling the drug release rate. The obtained results show that hydrotalcite may be used to prepare modified release formulations.
本研究的目的是调查水滑石是否能够插层非甾体抗炎药双氯芬酸，并以可控方式释放它。以氯化物形式存在的层状Mg-Al水滑石用作主体，通过Cl⁻/双氯芬酸阴离子交换制备插层化合物。根据美国药典24，在pH 7.5的模拟肠液中以及在旨在模拟小肠离子条件的pH 7.0溶液中，对插层化合物进行体外药物释放实验。插层过程的结果表明，水滑石能够通过简单的程序插层双氯芬酸，并且具有良好的载药量（55%重量/重量）。在pH 7.5和pH 7.0条件下，体外药物释放均明显低于相应物理混合物的释放。在后一种情况下，24小时时释放不完全。动力学分析表明，通过颗粒的扩散对控制药物释放速率很重要。所得结果表明，水滑石可用于制备缓释制剂。
