Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media

Research output: Contribution to journalJournal articlepeer-review

Standard

Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media. / Heikkinen, A. T.; DeClerck, L.; Löbmann, Korbinian; Grohganz, H.; Rades, T.; Laitinen, R.

In: Pharmazie, Vol. 70, No. 7, 07.2015, p. 452-457.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Heikkinen, AT, DeClerck, L, Löbmann, K, Grohganz, H, Rades, T & Laitinen, R 2015, 'Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media', Pharmazie, vol. 70, no. 7, pp. 452-457. <http://www.ingentaconnect.com/contentone/govi/pharmaz/2015/00000070/00000007/art00003?crawler=true>

APA

Heikkinen, A. T., DeClerck, L., Löbmann, K., Grohganz, H., Rades, T., & Laitinen, R. (2015). Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media. Pharmazie, 70(7), 452-457. http://www.ingentaconnect.com/contentone/govi/pharmaz/2015/00000070/00000007/art00003?crawler=true

Vancouver

Heikkinen AT, DeClerck L, Löbmann K, Grohganz H, Rades T, Laitinen R. Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media. Pharmazie. 2015 Jul;70(7):452-457.

Author

Heikkinen, A. T. ; DeClerck, L. ; Löbmann, Korbinian ; Grohganz, H. ; Rades, T. ; Laitinen, R. / Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media. In: Pharmazie. 2015 ; Vol. 70, No. 7. pp. 452-457.

Bibtex

@article{3f96172eb4ef468a8f88266c20d35b5f,
title = "Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media",
abstract = "Co-amorphous formulations, particularly binary drug-amino acid mixtures, have been shown to provide enhanced dissolution for poorly-soluble drugs and improved physical stability of the amorphous state. However, to date the dissolution properties (mainly intrinsic dissolution rate) of the co-amorphous formulations have been tested only in buffers and their supersaturation ability remain unexplored. Consequently, dissolution studies in simulated intestinal fluids need to be conducted in order to better evaluate the potential of these systems in increasing the oral bioavailability of biopharmaceutics classification system class II drugs. In this study, solubility and dissolution properties of the co-amorphous simvastatin-lysine, gibenclamideserine, glibenclamide-threonine and glibenclamide-serine-threonine were studied in phosphate buffer pH 7.2 and biorelevant media (fasted and fed state simulated intestinal fluids (FaSSIF and FeSSIF, respectively)). The co-amorphous formulations were found to provide a long-lasting supersaturation and improve the dissolution of the drugs compared to the crystalline and amorphous drugs alone in buffer. Similar improvement, but in lesser extent, was observed in biorelevant media suggesting that a dissolution advantage observed in aqueous buffers may overestimate the advantage in vivo. However, the results show that, in addition to stability advantage shown earlier, co-amorphous drug-amino acid formulations provide dissolution advantage over crystalline drugs in both aqueous and biorelevant conditions. ",
author = "Heikkinen, {A. T.} and L. DeClerck and Korbinian L{\"o}bmann and H. Grohganz and T. Rades and R. Laitinen",
year = "2015",
month = jul,
language = "English",
volume = "70",
pages = "452--457",
journal = "Die Pharmazie",
issn = "0031-7144",
publisher = "Govi-Verlag Pharmazeutischer Verlag GmbH",
number = "7",

}

RIS

TY - JOUR

T1 - Dissolution properties of co-amorphous drug-amino acid formulations in buffer and biorelevant media

AU - Heikkinen, A. T.

AU - DeClerck, L.

AU - Löbmann, Korbinian

AU - Grohganz, H.

AU - Rades, T.

AU - Laitinen, R.

PY - 2015/7

Y1 - 2015/7

N2 - Co-amorphous formulations, particularly binary drug-amino acid mixtures, have been shown to provide enhanced dissolution for poorly-soluble drugs and improved physical stability of the amorphous state. However, to date the dissolution properties (mainly intrinsic dissolution rate) of the co-amorphous formulations have been tested only in buffers and their supersaturation ability remain unexplored. Consequently, dissolution studies in simulated intestinal fluids need to be conducted in order to better evaluate the potential of these systems in increasing the oral bioavailability of biopharmaceutics classification system class II drugs. In this study, solubility and dissolution properties of the co-amorphous simvastatin-lysine, gibenclamideserine, glibenclamide-threonine and glibenclamide-serine-threonine were studied in phosphate buffer pH 7.2 and biorelevant media (fasted and fed state simulated intestinal fluids (FaSSIF and FeSSIF, respectively)). The co-amorphous formulations were found to provide a long-lasting supersaturation and improve the dissolution of the drugs compared to the crystalline and amorphous drugs alone in buffer. Similar improvement, but in lesser extent, was observed in biorelevant media suggesting that a dissolution advantage observed in aqueous buffers may overestimate the advantage in vivo. However, the results show that, in addition to stability advantage shown earlier, co-amorphous drug-amino acid formulations provide dissolution advantage over crystalline drugs in both aqueous and biorelevant conditions.

AB - Co-amorphous formulations, particularly binary drug-amino acid mixtures, have been shown to provide enhanced dissolution for poorly-soluble drugs and improved physical stability of the amorphous state. However, to date the dissolution properties (mainly intrinsic dissolution rate) of the co-amorphous formulations have been tested only in buffers and their supersaturation ability remain unexplored. Consequently, dissolution studies in simulated intestinal fluids need to be conducted in order to better evaluate the potential of these systems in increasing the oral bioavailability of biopharmaceutics classification system class II drugs. In this study, solubility and dissolution properties of the co-amorphous simvastatin-lysine, gibenclamideserine, glibenclamide-threonine and glibenclamide-serine-threonine were studied in phosphate buffer pH 7.2 and biorelevant media (fasted and fed state simulated intestinal fluids (FaSSIF and FeSSIF, respectively)). The co-amorphous formulations were found to provide a long-lasting supersaturation and improve the dissolution of the drugs compared to the crystalline and amorphous drugs alone in buffer. Similar improvement, but in lesser extent, was observed in biorelevant media suggesting that a dissolution advantage observed in aqueous buffers may overestimate the advantage in vivo. However, the results show that, in addition to stability advantage shown earlier, co-amorphous drug-amino acid formulations provide dissolution advantage over crystalline drugs in both aqueous and biorelevant conditions.

M3 - Journal article

VL - 70

SP - 452

EP - 457

JO - Die Pharmazie

JF - Die Pharmazie

SN - 0031-7144

IS - 7

ER -

ID: 161664873