Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling

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Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling. / Wang, Yixuan; Rades, Thomas; Grohganz, Holger.

In: Pharmaceutics, Vol. 15, No. 1, 172, 2023.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Wang, Y, Rades, T & Grohganz, H 2023, 'Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling', Pharmaceutics, vol. 15, no. 1, 172. https://doi.org/10.3390/pharmaceutics15010172

APA

Wang, Y., Rades, T., & Grohganz, H. (2023). Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling. Pharmaceutics, 15(1), [172]. https://doi.org/10.3390/pharmaceutics15010172

Vancouver

Wang Y, Rades T, Grohganz H. Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling. Pharmaceutics. 2023;15(1). 172. https://doi.org/10.3390/pharmaceutics15010172

Author

Wang, Yixuan ; Rades, Thomas ; Grohganz, Holger. / Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling. In: Pharmaceutics. 2023 ; Vol. 15, No. 1.

Bibtex

@article{52f2dfef8f8e4479ba2b1526714ac625,
title = "Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling",
abstract = "In non-strongly interacting co-amorphous systems, addition of a polymer, to further stabilize the co-amorphous systems, may influence the phase behavior between the components. In this study, the evolution of the composition of the amorphous phase in the ternary system carvedilol (CAR)-tryptophan (TRP)-hydroxypropylmethyl cellulose (HPMC) was investigated, based upon previously formed and characterized binary systems to which the third component was added (CAR − TRP + HPMC, CAR − HPMC + TRP and TRP − HPMC + CAR). Ball milling was used as the preparation method for all binary and ternary systems. The influence of the milling time on the co-amorphous systems was monitored by DSC and XRPD. Addition of HPMC reduced the miscibility of CAR with TRP due to hydrogen bond formation between CAR and polymer. These bonds became dominant for the interaction pattern. In addition, when CAR or TRP exceeded the miscibility limit in HPMC, phase separation and eventually crystallization of CAR and TRP was observed. All ternary co-amorphous systems eventually reached the same composition, albeit following different paths depending on the initially used binary system.",
keywords = "Gordon-Taylor equation, miscibility, molecular interaction, phase separation, polymer, poorly water-soluble drugs, ternary amorphous system",
author = "Yixuan Wang and Thomas Rades and Holger Grohganz",
note = "Publisher Copyright: {\textcopyright} 2023 by the authors.",
year = "2023",
doi = "10.3390/pharmaceutics15010172",
language = "English",
volume = "15",
journal = "Pharmaceutics",
issn = "1999-4923",
publisher = "MDPI AG",
number = "1",

}

RIS

TY - JOUR

T1 - Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Milling

AU - Wang, Yixuan

AU - Rades, Thomas

AU - Grohganz, Holger

N1 - Publisher Copyright: © 2023 by the authors.

PY - 2023

Y1 - 2023

N2 - In non-strongly interacting co-amorphous systems, addition of a polymer, to further stabilize the co-amorphous systems, may influence the phase behavior between the components. In this study, the evolution of the composition of the amorphous phase in the ternary system carvedilol (CAR)-tryptophan (TRP)-hydroxypropylmethyl cellulose (HPMC) was investigated, based upon previously formed and characterized binary systems to which the third component was added (CAR − TRP + HPMC, CAR − HPMC + TRP and TRP − HPMC + CAR). Ball milling was used as the preparation method for all binary and ternary systems. The influence of the milling time on the co-amorphous systems was monitored by DSC and XRPD. Addition of HPMC reduced the miscibility of CAR with TRP due to hydrogen bond formation between CAR and polymer. These bonds became dominant for the interaction pattern. In addition, when CAR or TRP exceeded the miscibility limit in HPMC, phase separation and eventually crystallization of CAR and TRP was observed. All ternary co-amorphous systems eventually reached the same composition, albeit following different paths depending on the initially used binary system.

AB - In non-strongly interacting co-amorphous systems, addition of a polymer, to further stabilize the co-amorphous systems, may influence the phase behavior between the components. In this study, the evolution of the composition of the amorphous phase in the ternary system carvedilol (CAR)-tryptophan (TRP)-hydroxypropylmethyl cellulose (HPMC) was investigated, based upon previously formed and characterized binary systems to which the third component was added (CAR − TRP + HPMC, CAR − HPMC + TRP and TRP − HPMC + CAR). Ball milling was used as the preparation method for all binary and ternary systems. The influence of the milling time on the co-amorphous systems was monitored by DSC and XRPD. Addition of HPMC reduced the miscibility of CAR with TRP due to hydrogen bond formation between CAR and polymer. These bonds became dominant for the interaction pattern. In addition, when CAR or TRP exceeded the miscibility limit in HPMC, phase separation and eventually crystallization of CAR and TRP was observed. All ternary co-amorphous systems eventually reached the same composition, albeit following different paths depending on the initially used binary system.

KW - Gordon-Taylor equation

KW - miscibility

KW - molecular interaction

KW - phase separation

KW - polymer

KW - poorly water-soluble drugs

KW - ternary amorphous system

U2 - 10.3390/pharmaceutics15010172

DO - 10.3390/pharmaceutics15010172

M3 - Journal article

C2 - 36678800

AN - SCOPUS:85146462877

VL - 15

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 1

M1 - 172

ER -

ID: 334647893