使用煅烧的镁铝水滑石提高塞来昔布无定形形式的稳定性。

Use of calcined Mg-Al-hydrotalcite to enhance the stability of celecoxib in the amorphous form.

作者信息

Ambrogi Valeria, Perioli Luana, Marmottini Fabio, Rossi Carlo

机构信息

Dipartimento di Chimica e Tecnologia del Farmaco, University of Perugia, Perugia, Italy.

出版信息

Eur J Pharm Biopharm. 2007 May;66(2):253-9. doi: 10.1016/j.ejpb.2006.10.006. Epub 2006 Oct 17.

DOI:10.1016/j.ejpb.2006.10.006

PMID:17123798

Abstract

The use of compound in amorphous forms is a promising approach to improve solubility of poorly water-soluble drugs. However, during storage, amorphous state can spontaneously transform to the lower energy crystalline form and this is a limiting factor for a large commercial use of drugs. In this paper, calcined hydrotalcite was employed to support amorphous celecoxib and several preparations at different weight drug/carrier ratio were prepared. Solubility of celecoxib from the prepared systems was evaluated and its physical stability during storage at different conditions was examined as well. The results show that HTlc-calc can be used as a support of amorphous celecoxib with consequent improvement of drug solubility and physical stability.

摘要

使用无定形形式的化合物是提高难溶性药物溶解度的一种有前景的方法。然而，在储存过程中，无定形状态会自发转变为能量较低的结晶形式，这是药物大规模商业应用的一个限制因素。在本文中，采用煅烧水滑石来负载无定形塞来昔布，并制备了几种不同药物/载体重量比的制剂。评估了所制备体系中塞来昔布的溶解度，并考察了其在不同条件下储存期间的物理稳定性。结果表明，煅烧水滑石可作为无定形塞来昔布的载体，从而提高药物的溶解度和物理稳定性。