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

Research output: Contribution to journalJournal articlepeer-review

Standard

Amorphization within the tablet : Using microwave irradiation to form a glass solution in situ. / Doreth, Maria; Hussein, Murtadha Abdul; Priemel, Petra A.; Grohganz, Holger; Holm, René; Lopez de Diego, Heidi; Rades, Thomas; Löbmann, Korbinian.

In: International Journal of Pharmaceutics, Vol. 519, No. 1-2, 15.03.2017, p. 343-351.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Doreth, M, Hussein, MA, Priemel, PA, Grohganz, H, Holm, R, Lopez de Diego, H, Rades, T & Löbmann, K 2017, 'Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ', International Journal of Pharmaceutics, vol. 519, no. 1-2, pp. 343-351. https://doi.org/10.1016/j.ijpharm.2017.01.035

APA

Doreth, M., Hussein, M. A., Priemel, P. A., Grohganz, H., Holm, R., Lopez de Diego, H., Rades, T., & Löbmann, K. (2017). Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ. International Journal of Pharmaceutics, 519(1-2), 343-351. https://doi.org/10.1016/j.ijpharm.2017.01.035

Vancouver

Doreth M, Hussein MA, Priemel PA, Grohganz H, Holm R, Lopez de Diego H et al. Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ. International Journal of Pharmaceutics. 2017 Mar 15;519(1-2):343-351. https://doi.org/10.1016/j.ijpharm.2017.01.035

Author

Doreth, Maria ; Hussein, Murtadha Abdul ; Priemel, Petra A. ; Grohganz, Holger ; Holm, René ; Lopez de Diego, Heidi ; Rades, Thomas ; Löbmann, Korbinian. / Amorphization within the tablet : Using microwave irradiation to form a glass solution in situ. In: International Journal of Pharmaceutics. 2017 ; Vol. 519, No. 1-2. pp. 343-351.

Bibtex

@article{7216b485771a454e931ebec60351ecf3,
title = "Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ",
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 90 kJ. 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.",
keywords = "Amorphization, Glass solution, In situ, Microwave radiation, Recrystallization, Tablet",
author = "Maria Doreth and Hussein, {Murtadha Abdul} and Priemel, {Petra A.} and Holger Grohganz and Ren{\'e} Holm and {Lopez de Diego}, Heidi and Thomas Rades and Korbinian L{\"o}bmann",
year = "2017",
month = mar,
day = "15",
doi = "10.1016/j.ijpharm.2017.01.035",
language = "English",
volume = "519",
pages = "343--351",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

RIS

TY - JOUR

T1 - Amorphization within the tablet

T2 - Using microwave irradiation to form a glass solution in situ

AU - Doreth, Maria

AU - Hussein, Murtadha Abdul

AU - Priemel, Petra A.

AU - Grohganz, Holger

AU - Holm, René

AU - Lopez de Diego, Heidi

AU - Rades, Thomas

AU - Löbmann, Korbinian

PY - 2017/3/15

Y1 - 2017/3/15

N2 - 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 90 kJ. 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.

AB - 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 90 kJ. 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.

KW - Amorphization

KW - Glass solution

KW - In situ

KW - Microwave radiation

KW - Recrystallization

KW - Tablet

U2 - 10.1016/j.ijpharm.2017.01.035

DO - 10.1016/j.ijpharm.2017.01.035

M3 - Journal article

C2 - 28115260

AN - SCOPUS:85010695842

VL - 519

SP - 343

EP - 351

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 176884529