Physicochemical Properties of Bosentan and Selected PDE-5 Inhibitors in the Design of Drugs for Rare Diseases

作者: Anna Krupa , Dorota Majda , Włodzimierz Mozgawa , Jakub Szlęk , Renata Jachowicz

DOI: 10.1208/S12249-016-0599-7

关键词:

摘要: The study provides the physicochemical characteristic of bosentan (BOS) in comparison to tadalafil (TA) and sildenafil citrate (SIL). Despite some reports dealing with thermal SIL TA, properties BOS have not been investigated so far. Recent clinical indicated that combination PDE-5 inhibitor can improve effectiveness pharmacotherapy pulmonary arterial hypertension (PAH). However, order design personalized medicines for therapy chronic rare diseases, detailed information on behaviour solubility each drug is indispensable. Thus, XRD, DSC TGA-QMS analyses were applied compare drugs, their stability as well identify products degradation. dehydration started at 70°C was followed by chemical degradation onset 290°C. highest stated which decomposed ca. 320°C, whereas lowest decomposition process SIL, i.e. 190°C. identified. FT-FIR intra- intermolecular interactions between molecules. FT-MIR Raman spectroscopy used examine structure drugs. Chemoinformatic tools predict polar surface area, pKa, or logP Their results line dissolution studies.

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