Péter-Haraszti, Anna and Záhonyi, Petra and Farkas, Attila and Csontos, István and Nagy, Zsombor Kristóf and Szabó, Edina and Van den Mooter, Guy and Marosi, György (2024) Thermal investigation of relaxations of interacting and non-interacting amorphous solid dispersions. JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY, 149. pp. 8067-8083. ISSN 1388-6150
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Abstract
In the present research, thermal investigation of amorphous solid dispersions (ASDs) was performed in order to compare their relaxation transitions. Two different active pharmaceutical ingredients (APIs), namely naproxen (NAP) and spironolactone (SPIR), were used as model drugs and combined with polyvinylpyrrolidone vinyl acetate (PVPVA64) copolymer to form stable ASDs. The reason for the API selection was their different interacting potentials based on the presence (in the case of NAP) and the lack of H-bond donor group (in the case of SPIR). Determination of both Tg and sub-Tg transitions suggested that ASDs containing NAP and PVPVA64 are ‘interacting’ systems with respect to the H-bonding. Besides, temperature-dependent Raman spectroscopic experiments confirmed that the naphthalene ring of the NAP has a significant role in the sub-Tg relaxations. In contrast, SPIR-PVPVA64 systems proved to be ‘non-interacting’ ASDs according to the MDSC, TSDC, and Raman measurements. This study highlights that the combination of the results of different thermoanalytical investigations with spectroscopic methods helps to understand the molecular background of the relaxations in ASDs and thus contributes to the conscious design of stable amorphous pharmaceuticals in the early stage of development. © The Author(s) 2024.
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| Additional Information: | Department of Organic Chemistry and Technology, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3, Budapest, 1111, Hungary Department of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, Leuven, 3000, Belgium Export Date: 28 June 2024 CODEN: JTACF Correspondence Address: Szabó, E.; Department of Organic Chemistry and Technology, Műegyetem rkp. 3, Hungary; email: szabo.edina@vbk.bme.hu Correspondence Address: den Mooter, G.V.; Department of Pharmaceutical and Pharmacological Sciences, Campus Gasthuisberg ON2, Herestraat 49 b921, Belgium; email: guy.vandenmooter@kuleuven.be Funding details: European Commission, EC Funding details: Magyar Tudományos Akadémia, MTA Funding details: Nemzeti Kutatási, Fejlesztési és Innovaciós Alap, NKFIA Funding details: ÚNKP-23-3-II-BME-242, CELSA/19/028, ÚNKP-23-5-BME-421 Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH, K 143039 Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH Funding text 1: Project no. RRF-2.3.1\\u201321\\u20132022\\u201300015 has been implemented with the support provided by the European Union. This paper was supported by the J\\u00E1nos Bolyai Research Scholarship of the Hungarian Academy of Science. This research was supported from grants by the National Research, Development, and Innovation Office of Hungary (grant numbers: K 143039). Support of CELSA Research Fund is kindly acknowledged for grant CELSA/19/028. This project was supported by the \\u00DANKP-23-3-II-BME-242 and \\u00DANKP-23-5-BME-421 New National Excellence Program of the Ministry for Culture and Innovation from the source of the National Research, Development, and Innovation Fund. The scientific research publicized in this article was reached with the sponsorship of Gedeon Richter Talentum Foundation in framework of Gedeon Richter Excellence PhD Scholarship of Gedeon Richter. The authors are thoroughly grateful to K\\u00E1lm\\u00E1n Marossy for his useful advice relating to the TSDC method. Eszter G\\u00E1l is acknowledged for her pre-experiments relating to the TSDC measurements. The assistance provided by Erzs\\u00E9bet T\\u00F3th with the TSDC measurements is also appreciated. |
| Uncontrolled Keywords: | STABILITY; Molecular mobility; Amorphous solid dispersion; Intermolecular hydrogen bond; Relaxation transitions; |
| Subjects: | Q Science / természettudomány > QD Chemistry / kémia Q Science / természettudomány > QH Natural history / természetrajz > QH301 Biology / biológia > QH3011 Biochemistry / biokémia R Medicine / orvostudomány > RM Therapeutics. Pharmacology / terápia, gyógyszertan |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 20 Sep 2024 09:45 |
| Last Modified: | 20 Sep 2024 09:45 |
| URI: | https://real.mtak.hu/id/eprint/205319 |
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