Unintended and in situ amorphisation of pharmaceuticals.

Abstract:

: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.

journal_name

Adv Drug Deliv Rev

authors

Priemel PA,Grohganz H,Rades T

doi

10.1016/j.addr.2015.12.014

subject

Has Abstract

pub_date

2016-05-01 00:00:00

pages

126-32

eissn

0169-409X

issn

1872-8294

pii

S0169-409X(15)30020-X

journal_volume

100

pub_type

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