Abstract：
:In situ amorphization is a concept that allows to amorphize a given drug in its final dosage form right before administration. Hence, this approach can potentially be used to circumvent recrystallization issues that other amorphous formulation approaches are facing during storage. In this study, the feasibility of microwave irradiation to prepare amorphous solid dispersions (glass solutions) in situ was investigated. Indomethacin (IND) and polyvinylpyrrolidone K12 (PVP) were tableted at a 1:2 (w/w) ratio. In order to study the influence of moisture content and energy input on the degree of amorphization, tablet formulations were stored at different relative humidity (32, 43 and 54% RH) and subsequently microwaved using nine different power-time combinations up to a maximum energy input of 90kJ. XRPD results showed that up to 80% (w/w) of IND could be amorphized within the tablet. mDSC measurements revealed that with increasing microwaving power and time, the fractions of crystalline IND and amorphous PVP reduced, whereas the amount of in situ formed IND-PVP glass solution increased. Intrinsic dissolution showed that the dissolution rate of the microwaved solid dispersion was similar to that of a quench cooled, fully amorphous glass solution even though the microwaved samples contained residual crystalline IND.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Doreth M,Hussein MA,Priemel PA,Grohganz H,Holm R,Lopez de Diego H,Rades T,Löbmann Kdoi
10.1016/j.ijpharm.2017.01.035subject
Has Abstractpub_date
2017-03-15 00:00:00pages
343-351issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(17)30044-3journal_volume
519pub_type
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