Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions

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Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions. / Löbmann, Korbinian; Strachan, Clare; Grohganz, Holger; Rades, Thomas; Korhonen, Ossi; Laitinen, Riikka.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 81, No. 1, 2012, p. 159-69.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Löbmann, K, Strachan, C, Grohganz, H, Rades, T, Korhonen, O & Laitinen, R 2012, 'Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions', European Journal of Pharmaceutics and Biopharmaceutics, vol. 81, no. 1, pp. 159-69. https://doi.org/10.1016/j.ejpb.2012.02.004

APA

Löbmann, K., Strachan, C., Grohganz, H., Rades, T., Korhonen, O., & Laitinen, R. (2012). Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions. European Journal of Pharmaceutics and Biopharmaceutics, 81(1), 159-69. https://doi.org/10.1016/j.ejpb.2012.02.004

Vancouver

Löbmann K, Strachan C, Grohganz H, Rades T, Korhonen O, Laitinen R. Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions. European Journal of Pharmaceutics and Biopharmaceutics. 2012;81(1):159-69. https://doi.org/10.1016/j.ejpb.2012.02.004

Author

Löbmann, Korbinian ; Strachan, Clare ; Grohganz, Holger ; Rades, Thomas ; Korhonen, Ossi ; Laitinen, Riikka. / Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions. In: European Journal of Pharmaceutics and Biopharmaceutics. 2012 ; Vol. 81, No. 1. pp. 159-69.

Bibtex

@article{3d5464d8826541dd83da1ffe6bd54bad,
title = "Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions",
abstract = "The objective of this study was to prepare a co-amorphous drug/drug combination between two BCS class II drugs, simvastatin (SVS) and glipizide (GPZ). This pharmacologically relevant combination of two drugs could produce a promising candidate for formulations intended for combination therapy of metabolic disorders. The co-amorphous SVS-GPZ mixtures (molar ratios 2:1, 1:1 and 1:2) were prepared by mechanical activation (ball milling or cryomilling) and characterized with respect to their thermal properties, possible molecular interactions, dissolution properties and physical stability, and compared to the behaviour of pure amorphous forms and their physical mixtures. It was found that even though a molecular mixture was achieved with all SVS-GPZ mixture ratios, no molecular interactions between the drugs could be detected. By formation of co-amorphous single-phase mixtures, only the dissolution rate of GPZ could be improved. The co-amorphous mixtures showed improved stability compared to the pure amorphous forms and the amorphous physical mixtures. It was concluded that this was attributable to the molecular level mixing of SVS with GPZ upon milling, and GPZ is acting as an anti-plasticizer in these mixtures.",
keywords = "Drug Combinations, Drug Compounding, Drug Incompatibility, Drug Stability, Glipizide, Hypoglycemic Agents, Hypolipidemic Agents, Simvastatin, Solubility",
author = "Korbinian L{\"o}bmann and Clare Strachan and Holger Grohganz and Thomas Rades and Ossi Korhonen and Riikka Laitinen",
note = "Copyright {\circledC} 2012 Elsevier B.V. All rights reserved.",
year = "2012",
doi = "10.1016/j.ejpb.2012.02.004",
language = "English",
volume = "81",
pages = "159--69",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",
number = "1",

}

RIS

TY - JOUR

T1 - Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions

AU - Löbmann, Korbinian

AU - Strachan, Clare

AU - Grohganz, Holger

AU - Rades, Thomas

AU - Korhonen, Ossi

AU - Laitinen, Riikka

N1 - Copyright © 2012 Elsevier B.V. All rights reserved.

PY - 2012

Y1 - 2012

N2 - The objective of this study was to prepare a co-amorphous drug/drug combination between two BCS class II drugs, simvastatin (SVS) and glipizide (GPZ). This pharmacologically relevant combination of two drugs could produce a promising candidate for formulations intended for combination therapy of metabolic disorders. The co-amorphous SVS-GPZ mixtures (molar ratios 2:1, 1:1 and 1:2) were prepared by mechanical activation (ball milling or cryomilling) and characterized with respect to their thermal properties, possible molecular interactions, dissolution properties and physical stability, and compared to the behaviour of pure amorphous forms and their physical mixtures. It was found that even though a molecular mixture was achieved with all SVS-GPZ mixture ratios, no molecular interactions between the drugs could be detected. By formation of co-amorphous single-phase mixtures, only the dissolution rate of GPZ could be improved. The co-amorphous mixtures showed improved stability compared to the pure amorphous forms and the amorphous physical mixtures. It was concluded that this was attributable to the molecular level mixing of SVS with GPZ upon milling, and GPZ is acting as an anti-plasticizer in these mixtures.

AB - The objective of this study was to prepare a co-amorphous drug/drug combination between two BCS class II drugs, simvastatin (SVS) and glipizide (GPZ). This pharmacologically relevant combination of two drugs could produce a promising candidate for formulations intended for combination therapy of metabolic disorders. The co-amorphous SVS-GPZ mixtures (molar ratios 2:1, 1:1 and 1:2) were prepared by mechanical activation (ball milling or cryomilling) and characterized with respect to their thermal properties, possible molecular interactions, dissolution properties and physical stability, and compared to the behaviour of pure amorphous forms and their physical mixtures. It was found that even though a molecular mixture was achieved with all SVS-GPZ mixture ratios, no molecular interactions between the drugs could be detected. By formation of co-amorphous single-phase mixtures, only the dissolution rate of GPZ could be improved. The co-amorphous mixtures showed improved stability compared to the pure amorphous forms and the amorphous physical mixtures. It was concluded that this was attributable to the molecular level mixing of SVS with GPZ upon milling, and GPZ is acting as an anti-plasticizer in these mixtures.

KW - Drug Combinations

KW - Drug Compounding

KW - Drug Incompatibility

KW - Drug Stability

KW - Glipizide

KW - Hypoglycemic Agents

KW - Hypolipidemic Agents

KW - Simvastatin

KW - Solubility

U2 - 10.1016/j.ejpb.2012.02.004

DO - 10.1016/j.ejpb.2012.02.004

M3 - Journal article

C2 - 22353489

VL - 81

SP - 159

EP - 169

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

IS - 1

ER -

ID: 43944734