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dc.contributor.author
Chiappetta, Diego Andrés
dc.contributor.author
Carcaboso, Ángel M.
dc.contributor.author
Bregni, Carlos
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Rubio, Modesto Carlos
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Bramuglia, Guillermo Federico
dc.contributor.author
Sosnik, Alejandro Dario
dc.date.available
2024-08-12T12:47:32Z
dc.date.issued
2009-01
dc.identifier.citation
Chiappetta, Diego Andrés; Carcaboso, Ángel M.; Bregni, Carlos; Rubio, Modesto Carlos; Bramuglia, Guillermo Federico; et al.; Indinavir-Loaded pH-Sensitive Microparticles for Taste Masking: Toward Extemporaneous Pediatric Anti-HIV/AIDS Liquid Formulations with Improved Patient Compliance; Springer; AAPS Pharmscitech; 10; 1; 1-2009; 1-6
dc.identifier.issn
1530-9932
dc.identifier.uri
http://hdl.handle.net/11336/242262
dc.description.abstract
The aim of this work was to develop indinavir pediatric anti-HIV/AIDS formulations enabling convenient dose adjustment, ease of oral administration, and improved organoleptic properties by means of the generation of drug-loaded microparticles made of a polymer that is insoluble under intake conditions and dissolves fast in the stomach in order to completely release the active agent. Indinavirloaded microparticles made of a pH-dependent polymeric excipient soluble at pH<5, Eudragit E100, were prepared using a double emulsion solvent diffusion technique and the in vitro release profiles characterized. Finally, taste masking properties were evaluated in blind randomized sensory experiments by ten healthy human volunteers. The use of a w/o/o emulsion system resulted in indinavir loads around 90%. Thermal analysis of the microparticles by differential scanning calorimetry revealed that indinavir appeared mainly dispersed at the molecular level. Concentrations of residual organic solvents as determined by gas chromatography were below the upper limits specified by the European Pharmacopeia for pharmaceutical oral formulations. Then, the behavior of drug-containing microparticles in aqueous media at different pH values was assessed. While they selectively dissolved in gastriclike medium, in tap water (intake conditions), the matrix remained almost unchanged and efficiently prevented drug dissolution. Finally, sensoring taste tests performed by volunteers indicated that systems with indinavir loads ∼15% displayed acceptable taste. This work explored the production of indinavircontaining microparticles based on a common pharmaceutical excipient as a means for the improvement of medicines of drugs involved in the treatment of HIV/AIDS. For systems containing about 15% drug, taste studies confirmed the acceptability of the formulation. In pediatric regimes, this composition would require an acceptable amount of formulation (0.7–1.5 g).
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
BITTERNESS MASKING
dc.subject
EXTEMPORANEOUS PEDIATRIC LIQUID FORMULATIONS
dc.subject
INDINAVIR-LOADED MICROPARTICLES
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PATIENT COMPLIANCE AND TREATMENT ADHERENCE
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PEDIATRIC HIV/AIDS
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Otras Ciencias Químicas
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Indinavir-Loaded pH-Sensitive Microparticles for Taste Masking: Toward Extemporaneous Pediatric Anti-HIV/AIDS Liquid Formulations with Improved Patient Compliance
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2024-08-07T15:24:27Z
dc.journal.volume
10
dc.journal.number
1
dc.journal.pagination
1-6
dc.journal.pais
Alemania
dc.description.fil
Fil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Carcaboso, Ángel M.. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
dc.description.fil
Fil: Bregni, Carlos. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
dc.description.fil
Fil: Rubio, Modesto Carlos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
dc.description.fil
Fil: Bramuglia, Guillermo Federico. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
dc.description.fil
Fil: Sosnik, Alejandro Dario. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title
AAPS Pharmscitech
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://link.springer.com/article/10.1208/s12249-008-9168-z
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1208/s12249-008-9168-z
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