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dc.contributor.author
Real, Daniel Andres
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dc.contributor.author
Orzan, Lucas
dc.contributor.author
Leonardi, Darío
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dc.contributor.author
Salomon, Claudio Javier
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dc.date.available
2020-10-15T18:50:34Z
dc.date.issued
2020-01
dc.identifier.citation
Real, Daniel Andres; Orzan, Lucas; Leonardi, Darío; Salomon, Claudio Javier; Improving the dissolution of Triclabendazole from stable crystalline solid dispersions formulated for oral delivery; Springer; AAPS Pharmscitech; 21; 16; 1-2020; 1-13
dc.identifier.issn
1530-9932
dc.identifier.uri
http://hdl.handle.net/11336/115993
dc.description.abstract
Triclabendazole belongs to the class II/IV of the Biopharmaceuticals Classification System, and its low aqueous solubility represents a major drawback during the development of effective dosage forms. Therefore, the goal of this study was to elucidate whether polymeric solid dispersions would represent a suitable approach to overcome such disadvantage. Due to the lack of information on triclabendazole release, four different dissolution media were evaluated to analyze drug dissolution rate. The polymeric solid dispersions were characterized by X-ray diffraction and Fourier transform infrared spectroscopy. The selected final formulations were further stored for 24 months, and their physical stability was evaluated by means of X-ray diffraction and drug dissolution assays. Drug solubility studies indicated that poloxamer 407 (P407) solubilized a higher amount of drug than polyethylene glycol 6000. Drug-to-carrier ratio, nature of the selected carriers, and the type of dissolution media were important factors for increasing dissolution. By infrared spectroscopy, there were no specific interactions between the drug and polymers. The physicochemical characterization of the systems showed a detectable evidence of drug amorphization by increasing the carrier ratio. Micromeritic studies indicated that raw triclabendazole, physical mixtures, and reference formulation showed poor flow properties, in contrast to the triclabendazole:P407 solid dispersion sample. Both the crystalline properties and dissolution rate of selected samples were very similar after 24 months at room temperature. Thus, considering physical stability and dissolution studies, the development of the solid dispersion is a very suitable methodology to improve triclabendazole dissolution and, potentially, its biopharmaceutical performance.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
CAPSULES
dc.subject
DISSOLUTION
dc.subject
FASCIOLIASIS
dc.subject
SOLID DISPERSION
dc.subject
TRICLABENDAZOLE
dc.subject.classification
Otras Ciencias de la Salud
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dc.subject.classification
Ciencias de la Salud
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dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
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dc.title
Improving the dissolution of Triclabendazole from stable crystalline solid dispersions formulated for oral delivery
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-06-23T15:12:59Z
dc.journal.volume
21
dc.journal.number
16
dc.journal.pagination
1-13
dc.journal.pais
Alemania
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dc.description.fil
Fil: Real, Daniel Andres. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
dc.description.fil
Fil: Orzan, Lucas. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; Argentina
dc.description.fil
Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
dc.description.fil
Fil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
dc.journal.title
AAPS Pharmscitech
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1208/s12249-019-1551-4
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://link.springer.com/athens-shibboleth-login?previousUrl=https%3A%2F%2Flink.springer.com%2Farticle%2F10.1208%2Fs12249-019-1551-4
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