无定形态药物结晶行为的研究进展

Recent progress on crystallizations of amorphous pharmaceutical solids

无定形态药物与其晶态形式相比较,通常具有更高的溶解度和更快的溶出速率,并有效地改善部分难溶性药物的口服生物利用度。但由于无定形态药物处于热力学不稳定的高自由能状态,容易自发转变为其热力学稳定的晶态形式,从而丧失其原有优势。本文简述了无定形态药物中存在的多种快速结晶行为,并介绍近几年来该领域的研究进展。通过对无定形药物结晶内在机制的研究,有助于人们更好地理解、控制和预测无定形态药物的物理稳定性,为合理有效的开发无定形药物制剂提供理论基础。

Compared to their crystalline form,amorphous drugs exhibit higher solubility and faster dissolution rate and thus enhancing oral bioavailability of poorly water soluble drugs.However,since the amorphous form is thermodynamically unstable relative to the crystalline form,amorphous solids tend to crystallize over time and subsequently negate their advantages.This review briefly describes fundamental aspects of amorphous substances and highlights the recent advances of fast crystallization behaviors.Understanding the inherent crystallization mechanisms of amorphous materials is of utmost importance in order to control the physical stability and lead to efficient formulation development of amorphous pharmaceutical solids.