TY - JOUR
T1 - Unintended and in situ amorphisation of pharmaceuticals
AU - Priemel, P A
AU - Grohganz, H
AU - Rades, T
N1 - Copyright © 2015 Elsevier B.V. All rights reserved.
PY - 2016/5/1
Y1 - 2016/5/1
N2 - Amorphisation of poorly water-soluble drugs is one approach that can be applied to improve their solubility and thus their bioavailability. Amorphisation is a process that usually requires deliberate external energy input. However, amorphisation can happen both unintentionally, as in process-induced amorphisation during manufacturing, or in situ during dissolution, vaporisation, or lipolysis. The systems in which unintended and in situ amorphisation has been observed normally contain a drug and a carrier. Common carriers include polymers and mesoporous silica particles. However, the precise mechanisms by which in situ amorphisation occurs are often not fully understood. In situ amorphisation can be exploited and performed before administration of the drug or possibly even within the gastrointestinal tract, as can be inferred from in situ amorphisation observed during in vitro lipolysis. The use of in situ amorphisation can thus confer the advantages of the amorphous form, such as higher apparent solubility and faster dissolution rate, without the disadvantage of its physical instability.
AB - Amorphisation of poorly water-soluble drugs is one approach that can be applied to improve their solubility and thus their bioavailability. Amorphisation is a process that usually requires deliberate external energy input. However, amorphisation can happen both unintentionally, as in process-induced amorphisation during manufacturing, or in situ during dissolution, vaporisation, or lipolysis. The systems in which unintended and in situ amorphisation has been observed normally contain a drug and a carrier. Common carriers include polymers and mesoporous silica particles. However, the precise mechanisms by which in situ amorphisation occurs are often not fully understood. In situ amorphisation can be exploited and performed before administration of the drug or possibly even within the gastrointestinal tract, as can be inferred from in situ amorphisation observed during in vitro lipolysis. The use of in situ amorphisation can thus confer the advantages of the amorphous form, such as higher apparent solubility and faster dissolution rate, without the disadvantage of its physical instability.
KW - Journal Article
KW - Review
U2 - 10.1016/j.addr.2015.12.014
DO - 10.1016/j.addr.2015.12.014
M3 - Journal article
C2 - 26724250
SN - 0169-409X
VL - 100
SP - 126
EP - 132
JO - Advanced Drug Delivery Reviews
JF - Advanced Drug Delivery Reviews
ER -