Development and physicochemical characterization of saquinavir mesylate solid dispersions using Gelucire 44/14 or PEG 4000 as carrier View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2013-05-23

AUTHORS

Thiago Caon, Ricardo Augusto Konig, Ariadne Cristiane Cabral da Cruz, Simone Gonçalves Cardoso, Carlos Eduardo Maduro Campos, Silvia Lucia Cuffini, Letícia Scherer Koester, Cláudia Maria Oliveira Simões

ABSTRACT

Solid dispersions of saquinavir mesylate containing either Gelucire® 44/14 or poly(ethylene glycol) (PEG) 4000, or mixtures of each carrier with Tween 80 or polyvinyl pyrrolidone (PVP) K30 were prepared in order to enhance the drug dissolution rate. These systems were prepared by the melting method and characterized by X-ray powder diffraction, microscopical techniques, and Raman spectroscopy aiming to establish a relationship between physicochemical and dissolution properties under different cooling conditions. Modifications in degree of crystalline order/disorder over time were observed in preparations with both carriers. Overall, formulations cooled and stored at −20 °C showed less variation in dissolution rates than those at 25 °C. Although Tween 80 has enhanced the known self-emulsifying properties of Gelucire® 44/14, its combination with PEG 4000 displayed miscibility problems. The addition of PVP K30 was not the most effective approach in enhancing the dissolution in early steps; however, the drug dissolution was stable after 7 days of storage at 25 °C. The combination of PEG 4000 and PVP K30 maintained the dissolution properties for 60 and 90 days at 25 °C/95 % relative humidity and 40 °C/75 % (f2 values >50), respectively. More... »

PAGES

1113-1125

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s12272-013-0142-2

DOI

http://dx.doi.org/10.1007/s12272-013-0142-2

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1045702436

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/23700292


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71 mesylate solid dispersions
72 method
73 microscopical techniques
74 miscibility problem
75 mixture
76 modification
77 order
78 order/disorder
79 physicochemical characterization
80 polyvinyl pyrrolidone K30
81 powder diffraction
82 preparation
83 problem
84 properties
85 pyrrolidone K30
86 rate
87 ray powder diffraction
88 relationship
89 relative humidity
90 saquinavir
91 saquinavir mesylate solid dispersions
92 self-emulsifying properties
93 solid dispersions
94 spectroscopy
95 step
96 storage
97 system
98 technique
99 time
100 variation
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