Sample Preparation of Posaconazole Oral Suspensions for Identification of the Crystal Form of the Active Pharmaceutical Ingredient
| Autor: | Michail Lykouras, Malvina G. Orkoula, Stefani Fertaki, Christos G. Kontoyannis |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Posaconazole
oral suspension Materials science Chemistry Pharmaceutical Antifungal drug Administration Oral Pharmaceutical Science 02 engineering and technology XRPD 01 natural sciences Article Analytical Chemistry polymorphism lcsh:QD241-441 lcsh:Organic chemistry Suspensions Drug Discovery medicine Polymethyl Methacrylate formS Sample preparation Physical and Theoretical Chemistry Volume concentration Active ingredient centrifugation Chromatography sample preparation form-S 010401 analytical chemistry Organic Chemistry Triazoles 021001 nanoscience & nanotechnology equipment and supplies posaconazole 0104 chemical sciences Chemistry (miscellaneous) Oral suspensions Molecular Medicine 0210 nano-technology medicine.drug |
| Zdroj: | Molecules Volume 25 Issue 24 Molecules, Vol 25, Iss 6032, p 6032 (2020) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules25246032 |
| Popis: | Determination of the polymorphic form of an active pharmaceutical ingredient (API) in a suspension could be really challenging because of the water phase and the low concentration of the API in this formulation. Posaconazole is an antifungal drug available also as an oral suspension. The aim of this study was to develop a sample-preparation method for polymorphic identification of the dispersed API by increasing the concentration of the API but with no compromise of polymorph stability. For this purpose, filtration, drying and centrifugation were tested for separating the API from the suspending medium. Centrifugation was selected because it succeeded in separating Posaconazole API with no polymorph transformation during the process. During this study, it was found that Posaconazole in oral suspensions is Form-S. However, when slower scanning rates were used for acquiring an XRPD pattern with better signal/noise ratio, Posaconazole was converted to Form I due to water loss. In order to protect the sample from conversion, different approaches were tested to secure an airtight sample including a commercially available XRPD sample holder with a dome-like transparent cap, standard polymethylmethacrylate (PMMA) sample holders covered with Mylar film, transparent pressure-sensitive tape and a transparent food membrane. Only usage of the transparent food membrane was found to protect the API from conversion for a period of at least two weeks and resulted in a Posaconazole Form-S XRPD pattern with no artificial peaks. |
| Databáze: | OpenAIRE |
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