TY - JOUR
T1 - Emerging trends in the stabilization of amorphous drugs
AU - Laitinen, Riikka
AU - Löbmann, Korbinian
AU - Strachan, Clare J.
AU - Grohganz, Holger
AU - Rades, Thomas
N1 - Copyright © 2012 Elsevier B.V. All rights reserved.
PY - 2013/8/30
Y1 - 2013/8/30
N2 - The number of active pharmaceutical substances having high therapeutic potential but low water solubility is constantly increasing, making it difficult to formulate these compounds as oral dosage forms. The solubility and dissolution rate, and thus potentially the bioavailability, of these poorly water-soluble drugs can be increased by the formation of stabilized amorphous forms. Currently, formulation as solid polymer dispersions is the preferred method to enhance drug dissolution and to stabilize the amorphous form of a drug. The purpose of this review is to highlight emerging alternative methods to amorphous polymer dispersions for stabilizing the amorphous form of drugs. First, an overview of the properties and stabilization mechanisms of amorphous forms is provided. Subsequently, formulation approaches such as the preparation of co-amorphous small-molecule mixtures and the use of mesoporous silicon and silica-based carriers are presented as potential means to increase the stability of amorphous pharmaceuticals.
AB - The number of active pharmaceutical substances having high therapeutic potential but low water solubility is constantly increasing, making it difficult to formulate these compounds as oral dosage forms. The solubility and dissolution rate, and thus potentially the bioavailability, of these poorly water-soluble drugs can be increased by the formation of stabilized amorphous forms. Currently, formulation as solid polymer dispersions is the preferred method to enhance drug dissolution and to stabilize the amorphous form of a drug. The purpose of this review is to highlight emerging alternative methods to amorphous polymer dispersions for stabilizing the amorphous form of drugs. First, an overview of the properties and stabilization mechanisms of amorphous forms is provided. Subsequently, formulation approaches such as the preparation of co-amorphous small-molecule mixtures and the use of mesoporous silicon and silica-based carriers are presented as potential means to increase the stability of amorphous pharmaceuticals.
U2 - 10.1016/j.ijpharm.2012.04.066
DO - 10.1016/j.ijpharm.2012.04.066
M3 - Journal article
C2 - 22569230
SN - 0378-5173
VL - 453
SP - 65
EP - 79
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1
ER -