The role of pH and dose/solubility ratio on cocrystal dissolution, drug supersaturation and precipitation

The role of pH and dose/solubility ratio on cocrystal dissolution, drug supersaturation and precipitation

•Cocrystal dissolution interfacial pH mitigates drug dissolution-pH dependence.•Cocrystal to drug conversion occurs via surface nucleation of metastable polymorph.•σmax and AUC decrease with decreasing do as dissolution media pH increase.•When Do>>SA, drug supersaturation is sustained for very...

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Veröffentlicht in:European journal of pharmaceutical sciences 2020-09, Vol.152, p.105422-105422, Article 105422
Hauptverfasser: Machado, Tatiane Cogo, Kuminek, Gislaine, Cardoso, Simone Gonçalves, Rodríguez-Hornedo, Naír
Format: Artikel
Sprache:eng
Schlagworte:
Cocrystal
Disproportionation
Dose number
Interfacial pH
Precipitation
Supersaturation
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Zusammenfassung:•Cocrystal dissolution interfacial pH mitigates drug dissolution-pH dependence.•Cocrystal to drug conversion occurs via surface nucleation of metastable polymorph.•σmax and AUC decrease with decreasing do as dissolution media pH increase.•When Do>>SA, drug supersaturation is sustained for very long times.•When DoSA, the cocrystal solubility is not sufficient to dissolve the dose so that a dissolution-precipitation quasi-equilibrium state is able to sustain supersaturation for the extent of the experiment (24 h). When Do
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2020.105422