TY - JOUR

T1 - Amorphous drugs and dosage forms

AU - Grohganz, Holger

AU - Löbmann, K.

AU - Priemel, P.

AU - Jensen, Katrine Birgitte Tarp

AU - Graeser, K.

AU - Strachan, C.

AU - Rades, T.

PY - 2013/7/1

Y1 - 2013/7/1

N2 - The transformation to an amorphous form is one of the most promising approaches to address the low solubility of drug compounds, the latter being an increasing challenge in the development of new drug candidates. However, amorphous forms are high energy solids and tend to recry stallize. New formulation principles are needed to ensure the stability of amorphous drug forms. The formation of solid dispersions is still the most investigated approach, but additional approaches are desirable to overcome the shortcomings of solid dispersions. Spatial separation by either coating or the use of micro-containers has shown potential to prevent or delay recrystallization. Another recent approach is the formation of co-amorphous mixtures between either two drugs or one drug and one low molecular weight excipient. Molecular interactions between the two molecules provide an energy barrier that has to be overcome before single molecules are available for the formation of crystal nuclei, thus stabilizing the amorphous form.

AB - The transformation to an amorphous form is one of the most promising approaches to address the low solubility of drug compounds, the latter being an increasing challenge in the development of new drug candidates. However, amorphous forms are high energy solids and tend to recry stallize. New formulation principles are needed to ensure the stability of amorphous drug forms. The formation of solid dispersions is still the most investigated approach, but additional approaches are desirable to overcome the shortcomings of solid dispersions. Spatial separation by either coating or the use of micro-containers has shown potential to prevent or delay recrystallization. Another recent approach is the formation of co-amorphous mixtures between either two drugs or one drug and one low molecular weight excipient. Molecular interactions between the two molecules provide an energy barrier that has to be overcome before single molecules are available for the formation of crystal nuclei, thus stabilizing the amorphous form.

UR - http://www.scopus.com/inward/record.url?scp=84881580992&partnerID=8YFLogxK

M3 - Review

AN - SCOPUS:84881580992

VL - 23

SP - 403

EP - 408

JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

SN - 1773-2247

IS - 4

ER -