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 Revjournal_title
Advanced drug delivery reviewsauthors
Priemel PA,Grohganz H,Rades Tdoi
10.1016/j.addr.2015.12.014subject
Has Abstractpub_date
2016-05-01 00:00:00pages
126-32eissn
0169-409Xissn
1872-8294pii
S0169-409X(15)30020-Xjournal_volume
100pub_type
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