Development of direct compression Acetazolamide tablet with improved bioavailability in healthy human volunteers enabled by cocrystallization with p-Aminobenzoic acid
Copyright © 2024 Elsevier B.V. All rights reserved..
Pharmaceutical cocrystallization has been widely used to improve physicochemical properties of APIs. However, developing cocrystal formulation with proven clinical success remains scarce. Successful translation of a cocrystal to suitable dosage forms requires simultaneously improvement of several deficient physicochemical properties over the parent API, without deteriorating other properties critical for successful product development. In the present work, we report the successful development of a direct compression tablet product of acetazolamide (ACZ), using a 1:1 cocrystal of acetazolamide with p-aminobenzoic acid (ACZ-PABA). The ACZ-PABA tablet exhibits superior biopharmaceutical performance against the commercial tablet, DIAMOX® (250 mg), in healthy human volunteers, leading to more than 50 % reduction in the required dose.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:652 |
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| Enthalten in: |
International journal of pharmaceutics - 652(2024) vom: 05. Feb., Seite 123793 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Kumari, Nimmy [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 23.02.2024 Date Revised 23.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ijpharm.2024.123793 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright © 2024 Elsevier B.V. All rights reserved. | ||
| 520 | |a Pharmaceutical cocrystallization has been widely used to improve physicochemical properties of APIs. However, developing cocrystal formulation with proven clinical success remains scarce. Successful translation of a cocrystal to suitable dosage forms requires simultaneously improvement of several deficient physicochemical properties over the parent API, without deteriorating other properties critical for successful product development. In the present work, we report the successful development of a direct compression tablet product of acetazolamide (ACZ), using a 1:1 cocrystal of acetazolamide with p-aminobenzoic acid (ACZ-PABA). The ACZ-PABA tablet exhibits superior biopharmaceutical performance against the commercial tablet, DIAMOX® (250 mg), in healthy human volunteers, leading to more than 50 % reduction in the required dose | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Acetazolamide (ACZ) | |
| 650 | 4 | |a Caco-2 cell permeability | |
| 650 | 4 | |a Comparative bioavailability study | |
| 650 | 4 | |a P-aminobenzoic acid (PABA) | |
| 650 | 4 | |a Solubility | |
| 650 | 4 | |a Tabletability | |
| 650 | 7 | |a Acetazolamide |2 NLM | |
| 650 | 7 | |a O3FX965V0I |2 NLM | |
| 650 | 7 | |a 4-Aminobenzoic Acid |2 NLM | |
| 650 | 7 | |a TL2TJE8QTX |2 NLM | |
| 650 | 7 | |a Tablets |2 NLM | |
| 700 | 1 | |a Roy, Parag |e verfasserin |4 aut | |
| 700 | 1 | |a Roy, Sukanta |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Chenguang |e verfasserin |4 aut | |
| 700 | 1 | |a Das, Sourav |e verfasserin |4 aut | |
| 700 | 1 | |a Pandey, Noopur |e verfasserin |4 aut | |
| 700 | 1 | |a Mondal, Susanta Kumar |e verfasserin |4 aut | |
| 700 | 1 | |a Bose, Anirbandeep |e verfasserin |4 aut | |
| 700 | 1 | |a Sun, Changquan Calvin |e verfasserin |4 aut | |
| 700 | 1 | |a Ghosh, Animesh |e verfasserin |4 aut | |
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