Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ

作者: Maria Doreth , Murtadha Abdul Hussein , Petra A. Priemel , Holger Grohganz , René Holm

DOI: 10.1016/J.IJPHARM.2017.01.035

关键词:

摘要: In situ amorphization is a concept that allows to amorphize given drug in its final dosage form right before administration. Hence, this approach can potentially be used circumvent recrystallization issues other amorphous formulation approaches are facing during storage. study, the feasibility of microwave irradiation prepare solid dispersions (glass solutions) was investigated. Indomethacin (IND) and polyvinylpyrrolidone K12 (PVP) were tableted at 1:2 (w/w) ratio. order study influence moisture content energy input on degree amorphization, tablet formulations stored different relative humidity (32, 43 54% RH) subsequently microwaved using nine power-time combinations up maximum 90kJ. XRPD results showed 80% IND could amorphized within tablet. mDSC measurements revealed with increasing microwaving power time, fractions crystalline PVP reduced, whereas amount formed IND-PVP glass solution increased. Intrinsic dissolution rate dispersion similar quench cooled, fully even though samples contained residual IND.

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