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dc.contributor.author
Fandaruff, Cinira
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dc.contributor.author
Quirós Fallas, María Isabel
dc.contributor.author
Vega Baudrit, José Roberto
dc.contributor.author
Navarro Hoyos, Mirtha
dc.contributor.author
Lamas, Diego German
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dc.contributor.author
Araya Sibaja, Andrea Mariela
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dc.date.available
2024-03-01T10:56:11Z
dc.date.issued
2023-10
dc.identifier.citation
Fandaruff, Cinira; Quirós Fallas, María Isabel; Vega Baudrit, José Roberto; Navarro Hoyos, Mirtha; Lamas, Diego German; et al.; Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile; Multidisciplinary Digital Publishing Institute; Pharmaceutics; 15; 10; 10-2023; 1-15
dc.identifier.issn
1999-4923
dc.identifier.uri
http://hdl.handle.net/11336/229044
dc.description.abstract
The dissolution rate of the anti-HIV drug saquinavir base (SQV), a poorly water-soluble and extremely low absolute bioavailability drug, was improved through a eutectic mixture formation approach. A screening based on a liquid-assisted grinding technique was performed using a 1:1 molar ratio of the drug and the coformers sodium saccharinate, theobromine, nicotinic acid, nicotinamide, vanillin, vanillic acid, and piperine (PIP), followed by differential scanning calorimetry (DSC). Given that SQV-PIP was the only resulting eutectic system from the screening, both the binary phase and the Tammann diagrams were adapted to this system using DSC data of mixtures prepared from 0.1 to 1.0 molar ratios in order to determine the exact eutectic composition. The SQV-PIP system formed a eutectic at a composition of 0.6 and 0.40, respectively. Then, a solid-state characterization through DSC, powder X-ray diffraction (PXRD), including small-angle X-ray scattering (SAXS) measurements to explore the small-angle region in detail, Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and a powder dissolution test were performed. The conventional PXRD analyses suggested that the eutectic mixture did not exhibit structural changes; however, the small-angle region explored through the SAXS instrument revealed a change in the crystal structure of one of their components. FT-IR spectra showed no molecular interaction in the solid state. Finally, the dissolution profile of SQV in the eutectic mixture was different from the dissolution of pure SQV. After 45 min, approximately 55% of the drug in the eutectic mixture was dissolved, while, for pure SQV, 42% dissolved within this time. Hence, this study concludes that the dissolution rate of SQV can be effectively improved through the approach of using PIP as a coformer.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Multidisciplinary Digital Publishing Institute
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
DISSOLUTION ENHANCEMENT
dc.subject
EUTECTIC MIXTURES
dc.subject
PIPERINE
dc.subject
POWDER DIFFRACTION
dc.subject
SAQUINAVIR
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SMALL-ANGLE X-RAY SCATTERING
dc.subject
SOLID-STATE CHARACTERIZATION
dc.subject.classification
Farmacología y Farmacia
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dc.subject.classification
Medicina Básica
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dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
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dc.title
Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2024-02-29T12:45:45Z
dc.journal.volume
15
dc.journal.number
10
dc.journal.pagination
1-15
dc.journal.pais
Suiza
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dc.description.fil
Fil: Fandaruff, Cinira. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Tecnologías Emergentes y Ciencias Aplicadas. - Universidad Nacional de San Martin. Instituto de Tecnologías Emergentes y Ciencias Aplicadas; Argentina
dc.description.fil
Fil: Quirós Fallas, María Isabel. Universidad de Costa Rica; Costa Rica
dc.description.fil
Fil: Vega Baudrit, José Roberto. No especifíca;
dc.description.fil
Fil: Navarro Hoyos, Mirtha. Universidad de Costa Rica; Costa Rica
dc.description.fil
Fil: Lamas, Diego German. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Instituto de Tecnologias Emergentes y Ciencias Aplicadas. - Universidad Nacional de San Martin. Instituto de Tecnologias Emergentes y Ciencias Aplicadas.; Argentina
dc.description.fil
Fil: Araya Sibaja, Andrea Mariela. No especifíca;
dc.journal.title
Pharmaceutics
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3390/pharmaceutics15102446
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