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Abstract:

In situ fluidized hot melt granulation (FHMG) for different (ternary) formulations based on glyceryl palmito-stearate as non-conventional meltable binder and ibuprofen as model drug was examined for controlled release applications. The process was robust, lasted only 15. min, and enabled to attain high yields (95-98. wt.%). The obtained granules presented a bimodal size distribution, having the major mode of 200. μm and good flow properties, thus avoiding the necessity to add other lubricants for tablet compaction. The crystalline structure of ibuprofen and of the non meltable excipients was retained, and that of glyceryl palmito-stearate was recovered in the final granules. The resulting ibuprofen tablets had good pharmacotechnical properties. The granulation process did not modify release profiles from the tablets. The main factor influencing the release profiles was the content of glyceryl palmito-stearate in the formulations. A high drug load (50. wt.%), which is particularly important in the case of high dose active pharmaceutical ingredients, was achieved. Glyceryl palmito-stearate performed a triple function in the tablet formulation: as a meltable binder, as a controlled release matrix and as a lubricant. © 2014 Elsevier B.V.

Registro:

Documento: Artículo
Título:In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
Autor:Prado, H.J.; Bonelli, P.R.; Cukierman, A.L.
Filiación:PINMATE, Departamento de Industrias, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, C1428EGA Buenos Aires, Argentina
Cátedra de Tecnología Farmacéutica II, Departamento de Tecnología Farmacéutica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina
Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Av. Rivadavia 1917, C1033AAJ Buenos Aires, Argentina
Palabras clave:Controlled release; Fluidized hot melt granulation; Gelucires; Glyceryl palmito-stearate; Tablets; Binders; Drug products; Fluidization; Lubricants; Controlled release; Fluidized hot melt granulation; Gelucires; Glyceryl palmito-stearate; Tablets; Granulation; glycerol palmitostearate; ibuprofen; lubricating agent; article; controlled release formulation; crystal structure; drug granulation; drug granule; fluidized hot melt granulation; infrared spectroscopy; particle size; phase transition; scanning electron microscopy; tablet compression; tablet formulation; temperature measurement; X ray diffraction
Año:2014
Volumen:264
Página de inicio:498
Página de fin:506
DOI: http://dx.doi.org/10.1016/j.powtec.2014.05.058
Título revista:Powder Technology
Título revista abreviado:Powder Technol.
ISSN:00325910
CODEN:POTEB
CAS:glycerol palmitostearate, 29593-61-1; ibuprofen, 15687-27-1, 79261-49-7, 31121-93-4, 527688-20-6
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00325910_v264_n_p498_Prado

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Citas:

---------- APA ----------
Prado, H.J., Bonelli, P.R. & Cukierman, A.L. (2014) . In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets. Powder Technology, 264, 498-506.
http://dx.doi.org/10.1016/j.powtec.2014.05.058
---------- CHICAGO ----------
Prado, H.J., Bonelli, P.R., Cukierman, A.L. "In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets" . Powder Technology 264 (2014) : 498-506.
http://dx.doi.org/10.1016/j.powtec.2014.05.058
---------- MLA ----------
Prado, H.J., Bonelli, P.R., Cukierman, A.L. "In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets" . Powder Technology, vol. 264, 2014, pp. 498-506.
http://dx.doi.org/10.1016/j.powtec.2014.05.058
---------- VANCOUVER ----------
Prado, H.J., Bonelli, P.R., Cukierman, A.L. In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets. Powder Technol. 2014;264:498-506.
http://dx.doi.org/10.1016/j.powtec.2014.05.058