Understanding the pH Dependence of Supersaturation State-A Case Study of Telmisartan.
dimerization
solubility
supersaturation
telmisartan
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
05 Aug 2022
05 Aug 2022
Historique:
received:
14
07
2022
revised:
29
07
2022
accepted:
02
08
2022
entrez:
26
8
2022
pubmed:
27
8
2022
medline:
27
8
2022
Statut:
epublish
Résumé
Creating supersaturating drug delivery systems to overcome the poor aqueous solubility of active ingredients became a frequent choice for formulation scientists. Supersaturation as a solution phenomenon is, however, still challenging to understand, and therefore many recent publications focus on this topic. This work aimed to investigate and better understand the pH dependence of supersaturation of telmisartan (TEL) at a molecular level and find a connection between the physicochemical properties of the active pharmaceutical ingredient (API) and the ability to form supersaturated solutions of the API. Therefore, the main focus of the work was the pH-dependent thermodynamic and kinetic solubility of the model API, TEL. Based on kinetic solubility results, TEL was observed to form a supersaturated solution only in the pH range 3-8. The experimental thermodynamic solubility-pH profile shows a slight deviation from the theoretical Henderson-Hasselbalch curve, which indicates the presence of zwitterionic aggregates in the solution. Based on p
Identifiants
pubmed: 36015261
pii: pharmaceutics14081635
doi: 10.3390/pharmaceutics14081635
pmc: PMC9412861
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : János Bolyai Research Scholarship
ID : of the Hungarian Academy of Sciences
Organisme : Bolyai +
ID : New National Excellence Program of the Ministry for Innovation and Technology
Organisme : GITDA
ID : Governmental Information-Technology Development Agency, Hungary
Organisme : Ministry for Innovation and Technology
ID : ÚNKP-21-4
Organisme : National Research, Development, and Innovation Fund of Hungary
ID : TKP2021-EGA-02
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