Rapid screening of ternary amorphous formulations by a spray drying robot
Copyright © 2023 Elsevier B.V. All rights reserved..
Spray drying is commonly used for producing amorphous solid dispersions to improve drug solubility. The development of such formulations typically relies on comprehensive excipient and composition screening, which requires the preparation of many spray-dried powder samples. This is both labour-intensive and time-consuming when carried out manually. In the present work, the formulation screening task was automated by coupling a laboratory spray dryer operated in a semi-continuous mode with custom-made add-ons, allowing for rapid, computer-controlled production of formulation samples with systematically varying composition. The practical use of the spray drying robot in formulation development was demonstrated on a case study of poorly water-soluble model drugs simvastatin and ezetimibe. Six different polymers and several drug:polymer ratios were screened for the enhancement of dissolution properties. From a pool of 28 spray-dried samples, ternary compositions containing Eudragit L100-55 were identified as the most suitable ones for further processing and characterisation. The ability to populate the formulation design space rapidly and automatically made it possible to construct maps of physico-chemical properties such as glass transition temperature or dissolution rate. The spray drying robot thus enables the acceleration of early formulation development and a deeper understanding of composition-property relationships for multi-component spray dried powders.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2024 |
|---|---|
| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:651 |
|---|---|
| Enthalten in: |
International journal of pharmaceutics - 651(2024) vom: 15. Feb., Seite 123739 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Klimša, Vojtěch [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
Amorphous solid dispersion |
|---|
| Anmerkungen: |
Date Completed 02.02.2024 Date Revised 02.02.2024 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1016/j.ijpharm.2023.123739 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM366364480 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM366364480 | ||
| 003 | DE-627 | ||
| 005 | 20240202232115.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231227s2024 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1016/j.ijpharm.2023.123739 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1278.xml |
| 035 | |a (DE-627)NLM366364480 | ||
| 035 | |a (NLM)38145780 | ||
| 035 | |a (PII)S0378-5173(23)01161-4 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Klimša, Vojtěch |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Rapid screening of ternary amorphous formulations by a spray drying robot |
| 264 | 1 | |c 2024 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 02.02.2024 | ||
| 500 | |a Date Revised 02.02.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2023 Elsevier B.V. All rights reserved. | ||
| 520 | |a Spray drying is commonly used for producing amorphous solid dispersions to improve drug solubility. The development of such formulations typically relies on comprehensive excipient and composition screening, which requires the preparation of many spray-dried powder samples. This is both labour-intensive and time-consuming when carried out manually. In the present work, the formulation screening task was automated by coupling a laboratory spray dryer operated in a semi-continuous mode with custom-made add-ons, allowing for rapid, computer-controlled production of formulation samples with systematically varying composition. The practical use of the spray drying robot in formulation development was demonstrated on a case study of poorly water-soluble model drugs simvastatin and ezetimibe. Six different polymers and several drug:polymer ratios were screened for the enhancement of dissolution properties. From a pool of 28 spray-dried samples, ternary compositions containing Eudragit L100-55 were identified as the most suitable ones for further processing and characterisation. The ability to populate the formulation design space rapidly and automatically made it possible to construct maps of physico-chemical properties such as glass transition temperature or dissolution rate. The spray drying robot thus enables the acceleration of early formulation development and a deeper understanding of composition-property relationships for multi-component spray dried powders | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Amorphous solid dispersion | |
| 650 | 4 | |a Dissolution rate enhancement | |
| 650 | 4 | |a Eudragit | |
| 650 | 4 | |a Ezetimibe | |
| 650 | 4 | |a Glass transition temperature | |
| 650 | 4 | |a Simvastatin | |
| 650 | 7 | |a Polymers |2 NLM | |
| 700 | 1 | |a Mašková, Lucie |e verfasserin |4 aut | |
| 700 | 1 | |a Kašpar, Ondřej |e verfasserin |4 aut | |
| 700 | 1 | |a Ruphuy, Gabriela |e verfasserin |4 aut | |
| 700 | 1 | |a Štěpánek, František |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t International journal of pharmaceutics |d 1992 |g 651(2024) vom: 15. Feb., Seite 123739 |w (DE-627)NLM07779785X |x 1873-3476 |7 nnns |
| 773 | 1 | 8 | |g volume:651 |g year:2024 |g day:15 |g month:02 |g pages:123739 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.ijpharm.2023.123739 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 651 |j 2024 |b 15 |c 02 |h 123739 | ||