Solubility analysis of venlafaxine hydrochloride polymorphs by shake-flask method and real time monitoring
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Tartalom: https://www.aph-hsps.hu/acta/index.php/aph/article/view/11
Archívum: Acta Pharmaceutica
Gyűjtemény: Original Research Articles
Cím:
Solubility analysis of venlafaxine hydrochloride polymorphs by shake-flask method and real time monitoring
Létrehozó:
Takács-Novák, Krisztina
Tempfli, Dóra
Csicsák, Dóra
Völgyi, Gergely
Borbás, Enikő
Nagy, Zsombor K.
Sinkó, Bálint
Kiadó:
Hungarian Society for Pharmaceutical Sciences
Dátum:
2019-08-01
Téma:
solubility-pH profile, polymorphs, shake-flask method, µDISS Profiler, venlafaxine
pharmaceutical chemistry
physico-chemical profiling
solubility
Tartalmi leírás:
Aims: The aqueous solubility of two polymorphic forms of venlafaxine hydrochloride was investigated. Methods: The pH-dependent solubility (SpH) over a wide pH range was measured by saturation shake-flask (SSF) method at 25 °C. The solubility of the free base form was depicted by the intrinsic solubility (So). To identify the solid form present at the solubility equilibrium, X-ray powder diffraction (XRPD) and Raman spectroscopy was carried out. The dissolution was studied using real time concentration monitoring applying fiber optic UV probes. Results: No difference was found in the SpH values of Form I and Form II, in the pH range 7.5-12. Solid phase isolated from pH 10-12 suspensions was identified as free base by XRPD and Raman spectroscopy. Precipitates separated from pH 7-8 samples were also identical product. The transition of polymorphs to the free base was supported by the real time dissolution analysis. Conclusion: In this study we demonstrated a good agreement of equilibrium solubility measured by SSF method and in-situ UV fiber optic method. µDISS ProfilerTM has the advantage to provide much more information about dissolution process; with this approach the dissolution kinetic, the supersaturation and the time needed to reach the equilibrium can be easily monitored.  
Nyelv:
angol
Típus:
info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
Formátum:
application/pdf
Azonosító:
Forrás:
Acta Pharmaceutica Hungarica; Vol. 89 No. 2 (2019); 88-96
1587-1495
0001-6659
Kapcsolat:
Létrehozó:
Copyright (c) 2019 Acta Pharmaceutica Hungarica